Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 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
164616580 184745 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4859651 184745 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
17754443 179672 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at GPR40 expressed in CHO cells by FLIPR assayAgonist activity at GPR40 expressed in CHO cells by FLIPR assay
ChEMBL 370 3 1 3 4.7 O=C(O)[C@@H]1[C@H]2c3ccc(Oc4ccc(C(F)(F)F)cc4Cl)cc3O[C@H]21 10.1016/j.bmcl.2008.10.085
CHEMBL475027 179672 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at GPR40 expressed in CHO cells by FLIPR assayAgonist activity at GPR40 expressed in CHO cells by FLIPR assay
ChEMBL 370 3 1 3 4.7 O=C(O)[C@@H]1[C@H]2c3ccc(Oc4ccc(C(F)(F)F)cc4Cl)cc3O[C@H]21 10.1016/j.bmcl.2008.10.085
155551422 173395 0 None -15 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4541658 173395 0 None -15 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
134465732 170909 0 None -1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4463571 170909 0 None -1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
164615766 184426 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1cc(Cl)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4854804 184426 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1cc(Cl)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
134465794 170511 0 None -4 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 170511 0 None -4 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
91827421 148727 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 529 9 1 3 7.0 CC(c1cc(C(F)(F)F)ccc1C(F)(F)F)N1CC(COc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)C1 10.1016/j.bmcl.2016.10.074
CHEMBL3944424 148727 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 529 9 1 3 7.0 CC(c1cc(C(F)(F)F)ccc1C(F)(F)F)N1CC(COc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)C1 10.1016/j.bmcl.2016.10.074
155551422 173395 0 None 15 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4541658 173395 0 None 15 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
134465794 170511 0 None 4 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 170511 0 None 4 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
24857286 1594 66 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
164613862 184023 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1c(Cl)cccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4848974 184023 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1c(Cl)cccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
89671280 146155 0 None 10 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3923877 146155 0 None 10 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmcl.2016.10.074
134465732 170909 0 None 1 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4463571 170909 0 None 1 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
164617551 184729 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c(C)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4859407 184729 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c(C)c1 10.1021/acs.jmedchem.1c00031
142738582 183938 0 None 42 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4847662 183938 0 None 42 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
137333449 167048 3 None 10 2 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165147 167048 3 None 10 2 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301092 167048 3 None 10 2 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
86288852 110766 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265149 110766 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
52936292 181528 23 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
164619456 185567 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1cccc(C)c1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4872298 185567 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1cccc(C)c1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
164610330 184614 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 357 4 2 1 4.9 Cc1cc(Br)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4857550 184614 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 357 4 2 1 4.9 Cc1cc(Br)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
137333449 167048 3 None -10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165147 167048 3 None -10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301092 167048 3 None -10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
118638016 167091 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163182 167091 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301725 167091 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
134465785 175537 0 None -15 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 175537 0 None -15 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
68194465 182724 0 None -3 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 182724 0 None -3 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
118151370 158557 0 None 7 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 158557 0 None 7 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
155549083 173096 0 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4534836 173096 0 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
118623101 167028 0 None -12 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167028 0 None -12 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167028 0 None -12 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
90357232 141720 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884803 141720 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
51049992 145086 4 None -23 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None -23 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
118638009 167092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4160527 167092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301726 167092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
118623101 167028 0 None 12 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167028 0 None 12 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167028 0 None 12 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
15604310 111309 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287571 111309 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
46854655 391 43 None -8 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None -8 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None -8 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
68194476 182305 0 None -6 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182305 0 None -6 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
118638010 167004 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167004 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167004 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
90372613 167183 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167183 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167183 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
90655860 110761 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265144 110761 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
118637996 141638 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 141638 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 141638 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
118637996 141638 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 141638 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 141638 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
162668378 181925 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 181925 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
90372625 167160 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167160 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167160 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
145980154 166084 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 372 9 1 3 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4281133 166084 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 372 9 1 3 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
44572097 188960 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 3 6.1 CC#CC(CC(=O)O)c1ccc(OC2CCc3cc(-c4cccs4)ccc32)cc1 10.1016/j.bmcl.2008.10.085
CHEMBL514337 188960 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 3 6.1 CC#CC(CC(=O)O)c1ccc(OC2CCc3cc(-c4cccs4)ccc32)cc1 10.1016/j.bmcl.2008.10.085
134144239 149934 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 543 8 1 3 7.9 COc1ccc(F)c(-c2ccc(Cc3cccc(N4C[C@H](c5cccc(Cl)c5)C[C@@H]4CC(=O)O)c3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3954235 149934 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 543 8 1 3 7.9 COc1ccc(F)c(-c2ccc(Cc3cccc(N4C[C@H](c5cccc(Cl)c5)C[C@@H]4CC(=O)O)c3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
131986136 163073 0 None 3 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203795 163073 0 None 3 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
3367 1134 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1016/j.bmcl.2009.10.052
46216676 1134 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1016/j.bmcl.2009.10.052
CHEMBL604126 1134 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1016/j.bmcl.2009.10.052
46232307 200879 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C2CC2C(=O)O)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL611821 200879 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C2CC2C(=O)O)cc1 10.1016/j.bmcl.2009.10.052
90644300 111475 0 None 31 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288358 111475 0 None 31 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
23111694 73711 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
CHEMBL2022256 73711 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
68194237 181624 0 None -4 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 181624 0 None -4 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
131986401 163432 0 None 1 2 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4208095 163432 0 None 1 2 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
134140733 146631 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 358 8 1 3 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCCOc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3927863 146631 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 358 8 1 3 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCCOc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2016.10.074
134137874 152448 0 None 1995 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISAAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152448 0 None 1995 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISAAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152448 0 None 1995 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISAAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
44409843 139875 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380884 139875 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
57706620 163332 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 11 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)CC4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4206969 163332 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 11 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)CC4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
57707179 163953 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 534 10 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4214632 163953 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 534 10 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
46854655 391 43 None -8 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/jm2005699
6485 391 43 None -8 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/jm2005699
CHEMBL1829173 391 43 None -8 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/jm2005699
1050 1871 86 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2009.10.052
11595431 1871 86 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2009.10.052
CHEMBL207881 1871 86 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2009.10.052
122185437 122162 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 11 1 5 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OCOC)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604043 122162 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 11 1 5 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OCOC)c2)cc1 10.1016/j.bmc.2015.07.028
121294359 179006 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 14 1 7 6.4 COc1ccc(C(=O)N(CC(C)(C)OC)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4742099 179006 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 14 1 7 6.4 COc1ccc(C(=O)N(CC(C)(C)OC)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
121294251 179377 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 536 11 1 5 6.1 COc1ccc(C(=O)N(C)CC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4746614 179377 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 536 11 1 5 6.1 COc1ccc(C(=O)N(C)CC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
90151370 155374 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 525 7 1 6 5.6 COc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4060840 155374 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 525 7 1 6 5.6 COc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
145987015 166489 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#CC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4288867 166489 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#CC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
54583582 61835 0 None -2 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777872 61835 0 None -2 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
44409728 74702 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.4 CC(Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)C(=O)O 10.1016/j.bmcl.2006.01.007
CHEMBL203520 74702 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.4 CC(Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)C(=O)O 10.1016/j.bmcl.2006.01.007
44409670 75609 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 461 8 2 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205263 75609 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 461 8 2 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
20331242 87398 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL233835 87398 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2006.12.084
58319107 86120 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 326 4 1 1 4.8 O=C(O)CCc1ccc(C#Cc2ccccc2-c2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315546 86120 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 326 4 1 1 4.8 O=C(O)CCc1ccc(C#Cc2ccccc2-c2ccccc2)cc1 10.1021/jm301470a
71562312 86131 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 4 1 1 3.5 O=C(O)CCCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315557 86131 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 4 1 1 3.5 O=C(O)CCCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
146314511 180039 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 508 13 1 5 6.0 COc1ccc(CN(C)CC(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4754718 180039 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 508 13 1 5 6.0 COc1ccc(CN(C)CC(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
23136477 58522 3 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL1688455 58522 3 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL4213909 58522 3 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
137643339 157499 0 None -26 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4085843 157499 0 None -26 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
46232308 199401 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL602867 199401 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
134130696 141605 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 141605 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
142738543 161558 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 349 5 2 2 4.8 O=C(O)CCc1ccc2[nH]c(-c3ccccc3OC(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4161206 161558 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 349 5 2 2 4.8 O=C(O)CCc1ccc2[nH]c(-c3ccccc3OC(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
127046664 139296 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 453 9 1 5 6.0 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC2CCCC2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798992 139296 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 453 9 1 5 6.0 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC2CCCC2)c1 10.1016/j.ejmech.2016.03.054
155549391 173265 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 466 7 1 5 5.0 O=C(O)CC1(c2ccc(OC[C@H]3COc4ccc(-c5ccc(Cl)cc5)cc4O3)cc2)COC1 10.1016/j.bmcl.2019.01.014
CHEMBL4538821 173265 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 466 7 1 5 5.0 O=C(O)CC1(c2ccc(OC[C@H]3COc4ccc(-c5ccc(Cl)cc5)cc4O3)cc2)COC1 10.1016/j.bmcl.2019.01.014
145970056 164221 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 475 9 2 5 5.3 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccccc3F)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4218014 164221 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 475 9 2 5 5.3 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccccc3F)s2)cc1 10.1016/j.ejmech.2017.09.019
137643339 157499 0 None -26 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4085843 157499 0 None -26 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
122193743 123454 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 1 5 5.2 COCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628763 123454 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 1 5 5.2 COCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
145969681 164437 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 392 6 1 5 4.2 Cc1nn(C)c(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4225643 164437 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 392 6 1 5 4.2 Cc1nn(C)c(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
145984886 165886 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 415 7 1 6 4.2 O=C(O)CC(c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1)c1cnco1 10.1016/j.bmc.2018.10.019
CHEMBL4277516 165886 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 415 7 1 6 4.2 O=C(O)CC(c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1)c1cnco1 10.1016/j.bmc.2018.10.019
168290747 191326 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 420 10 1 5 4.9 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)cc3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5200259 191326 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 420 10 1 5 4.9 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)cc3)c2)cc1 10.1016/j.ejmech.2021.114061
90356885 166974 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 166974 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 166974 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
53248847 61818 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 61818 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
134150245 151713 0 None -117 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 374 7 1 3 5.1 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3968947 151713 0 None -117 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 374 7 1 3 5.1 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
118638016 167091 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163182 167091 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301725 167091 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
71612894 89550 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 408 3 1 4 4.1 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381292 89550 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 408 3 1 4 4.1 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
122193737 123452 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 438 10 1 4 5.9 CCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628757 123452 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 438 10 1 4 5.9 CCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
57521809 75911 0 None -13 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL2058520 75911 0 None -13 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL4210970 75911 0 None -13 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmc.2017.10.040
145971234 162531 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 453 7 1 3 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4176612 162531 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 453 7 1 3 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)cc2)cc1 10.1016/j.ejmech.2018.04.023
127051302 139786 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3806208 139786 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3)s2)cc1 10.1016/j.bmc.2016.04.065
127049498 139711 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(Cl)c3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805377 139711 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(Cl)c3)s2)cc1 10.1016/j.bmc.2016.04.065
131986147 164227 0 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218110 164227 0 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
25150121 184599 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1ccc(C#Cc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm8010178
CHEMBL485738 184599 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1ccc(C#Cc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm8010178
75511303 121940 4 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(F)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600997 121940 4 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(F)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
54757735 65014 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 341 4 1 2 4.5 Cc1ccccc1-c1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
CHEMBL1829163 65014 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 341 4 1 2 4.5 Cc1ccccc1-c1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
54582150 61481 0 None 22 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773259 61481 0 None 22 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
54582630 61829 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 61829 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
131986297 163653 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210878 163653 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
122189677 122839 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616657 122839 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
46231436 198715 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 5 1 3 3.4 O=C1NC(=O)C(Cc2ccc(CCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598040 198715 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 5 1 3 3.4 O=C1NC(=O)C(Cc2ccc(CCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
46231655 199429 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccnc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL603065 199429 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccnc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
145951164 162244 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 473 8 2 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172250 162244 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 473 8 2 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
122193972 123460 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 2 5 4.9 Cc1cc(OCCCO)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3629046 123460 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 2 5 4.9 Cc1cc(OCCCO)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
57521917 75922 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL2058530 75922 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1 10.1021/jm300215x
168298569 192078 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1cccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)c1 10.1016/j.ejmech.2022.114645
CHEMBL5219055 192078 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1cccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)c1 10.1016/j.ejmech.2022.114645
25150113 171068 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 265 3 2 2 2.7 Nc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL446575 171068 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 265 3 2 2 2.7 Nc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
54757515 64997 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 296 4 1 4 2.4 O=C(O)CCc1ccc(C#Cc2ncccc2[N+](=O)[O-])cc1 10.1021/jm2005699
CHEMBL1829147 64997 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 296 4 1 4 2.4 O=C(O)CCc1ccc(C#Cc2ncccc2[N+](=O)[O-])cc1 10.1021/jm2005699
146314448 179547 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 507 12 1 4 7.3 COc1ccc(CCCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4748702 179547 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 507 12 1 4 7.3 COc1ccc(CCCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
134538585 163083 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4203974 163083 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
15603842 111308 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287570 111308 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
91809187 146591 7 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 146591 7 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
118645715 180905 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764729 180905 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
162668241 181924 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4787007 181924 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
67087041 181789 0 None -14 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 181789 0 None -14 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183003 0 None -10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183003 0 None -10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194237 181624 0 None -4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 181624 0 None -4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
45107312 118628 3 None -2 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427712 118628 3 None -2 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
118642390 162134 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4170346 162134 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
155544661 174373 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
CHEMBL4565467 174373 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
127045659 139163 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1ccc(F)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798044 139163 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1ccc(F)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
71613520 89547 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381289 89547 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
57706778 80385 25 None 8 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL2152070 80385 25 None 8 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
147329931 174829 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 409 9 2 4 5.3 CCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4575598 174829 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 409 9 2 4 5.3 CCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
134137874 152448 0 None 1995 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152448 0 None 1995 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152448 0 None 1995 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
168273613 189674 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 468 6 1 5 5.6 O=C(O)C[C@@H]1COc2cc(OCc3ccc4nc(-c5ccc(C(F)(F)F)cc5)cn4c3)ccc21 10.1016/j.bmcl.2021.127969
CHEMBL5175525 189674 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 468 6 1 5 5.6 O=C(O)C[C@@H]1COc2cc(OCc3ccc4nc(-c5ccc(C(F)(F)F)cc5)cn4c3)ccc21 10.1016/j.bmcl.2021.127969
57705555 163048 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 518 11 1 3 8.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4203561 163048 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 518 11 1 3 8.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
57400637 69680 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939650 69680 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.10.118
137644989 157969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 391 7 1 4 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C#N)CC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4091211 157969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 391 7 1 4 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C#N)CC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
132606863 157281 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157281 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218709 157872 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
CHEMBL4090240 157872 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
90151764 156460 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 526 7 1 7 5.0 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4073270 156460 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 526 7 1 7 5.0 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
77845055 159238 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4105324 159238 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
145990980 166206 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)ccc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4283655 166206 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)ccc3O2)cc1 10.1016/j.bmc.2018.10.019
122193742 123453 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 396 7 2 4 4.9 Cc1cc(O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628762 123453 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 396 7 2 4 4.9 Cc1cc(O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
23136315 58523 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccccc2Oc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688456 58523 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccccc2Oc2ccccc2)cc1 10.1021/jm101405t
25261464 80386 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152071 80386 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
57395404 69667 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 286 7 1 3 3.3 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939637 69667 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 286 7 1 3 3.3 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
58218607 155399 0 None -7 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4061093 155399 0 None -7 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137661475 158911 0 None 1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4101348 158911 0 None 1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
137651153 156662 0 None -1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.7 CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4076004 156662 0 None -1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.7 CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
90644294 111469 0 None -13 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288352 111469 0 None -13 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
124011385 166307 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4285594 166307 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
137635388 155283 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4059947 155283 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
137646043 157245 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 385 6 1 2 5.4 Cc1ccccc1Cc1ccc(N2CC[C@H](c3ccccc3)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4082975 157245 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 385 6 1 2 5.4 Cc1ccccc1Cc1ccc(N2CC[C@H](c3ccccc3)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145985122 165355 0 None -17 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 456 11 1 4 5.5 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4250132 165355 0 None -17 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 456 11 1 4 5.5 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
1049 360 70 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
4618 360 70 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
5280934 360 70 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
CHEMBL8739 360 70 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
DB00132 360 70 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
71613515 89542 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381283 89542 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
86803185 121949 6 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601006 121949 6 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
137629942 160478 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1 10.1016/j.ejmech.2017.01.005
CHEMBL4071849 160478 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1 10.1016/j.ejmech.2017.01.005
CHEMBL4116363 160478 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1 10.1016/j.ejmech.2017.01.005
54757626 65008 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
CHEMBL1829157 65008 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
24825481 75572 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205090 75572 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
134141270 146277 0 None -35 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 334 8 1 3 4.6 CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3924759 146277 0 None -35 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 334 8 1 3 4.6 CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
15605424 198882 3 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccccc2Oc2ccccc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599067 198882 3 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccccc2Oc2ccccc2)S1 10.1016/j.bmcl.2009.10.052
53248847 61818 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 61818 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
145950728 162220 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4171827 162220 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
86803196 121950 3 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601007 121950 3 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)cc1 10.1016/j.bmcl.2015.06.018
145966017 163791 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1C 10.1016/j.ejmech.2017.09.019
CHEMBL4212573 163791 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1C 10.1016/j.ejmech.2017.09.019
145954950 161096 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccc(C(F)(F)F)cc3)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4130213 161096 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccc(C(F)(F)F)cc3)cc2)S1 10.1016/j.bmcl.2018.03.051
145953265 162077 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccnc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4169459 162077 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccnc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
54580625 61836 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777873 61836 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
127045658 139249 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 437 7 1 4 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(C(F)(F)F)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798642 139249 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 437 7 1 4 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(C(F)(F)F)c1 10.1016/j.ejmech.2016.03.054
145958971 161637 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 500 8 1 4 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4162561 161637 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 500 8 1 4 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
44409702 140455 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 1 3 5.6 O=C(CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)N1CCCC1 10.1016/j.bmcl.2006.01.007
CHEMBL382341 140455 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 1 3 5.6 O=C(CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)N1CCCC1 10.1016/j.bmcl.2006.01.007
137630875 160575 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4091587 160575 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4117177 160575 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
57521813 75915 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 400 7 1 2 6.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1 10.1021/jm300215x
CHEMBL2058524 75915 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 400 7 1 2 6.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1 10.1021/jm300215x
23346507 87860 1 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/jm300215x
CHEMBL234834 87860 1 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/jm300215x
3893 2255 92 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
4642 2255 92 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
5534 2255 92 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
CHEMBL108766 2255 92 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
DB03017 2255 92 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
643684 107029 59 None -8 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 298 15 2 2 5.1 CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O 10.1039/C7MD00130D
CHEMBL3186422 107029 59 None -8 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 298 15 2 2 5.1 CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O 10.1039/C7MD00130D
122189680 122841 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 8 2 4 3.4 CC(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616660 122841 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 8 2 4 3.4 CC(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
127025284 137221 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 417 6 1 4 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
CHEMBL3759212 137221 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 417 6 1 4 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
82051616 158910 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
CHEMBL4101323 158910 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
134130823 153901 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3890182 153901 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990066 153901 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
118129974 156652 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 156652 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
145994052 166801 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 425 7 1 5 4.6 O=C(O)CC(c1ccncc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294582 166801 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 425 7 1 5 4.6 O=C(O)CC(c1ccncc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145966485 163798 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 9 2 6 3.9 CCc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4212664 163798 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 9 2 6 3.9 CCc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
1051 1427 56 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
4289 1427 56 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
445580 1427 56 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
57417355 1427 56 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
CHEMBL367149 1427 56 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
DB03756 1427 56 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
127030730 138285 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1cccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)c1 10.1016/j.ejmech.2016.02.040
CHEMBL3781145 138285 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1cccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)c1 10.1016/j.ejmech.2016.02.040
90151568 157029 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 7 1 5 5.5 CCc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4080516 157029 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 7 1 5 5.5 CCc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
137633536 155754 0 None -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based 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 -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based 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
46231549 198813 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598674 198813 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
91809187 146591 7 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3927519 146591 7 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1016/j.bmcl.2016.10.074
127050768 139759 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805903 139759 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
131986116 163272 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206318 163272 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58173002 122155 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1F 10.1016/j.bmc.2015.07.028
CHEMBL3604037 122155 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1F 10.1016/j.bmc.2015.07.028
122185439 122166 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604047 122166 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)cc2)cc1 10.1016/j.bmc.2015.07.028
45107317 122180 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 8 1 3 4.9 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(CC)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604061 122180 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 8 1 3 4.9 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(CC)cccc32)cc1 10.1016/j.bmc.2015.07.028
122185451 122181 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.4 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C(C)C)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604062 122181 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.4 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C(C)C)cccc32)cc1 10.1016/j.bmc.2015.07.028
127046961 139527 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 383 7 1 4 5.0 Cc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3800362 139527 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 383 7 1 4 5.0 Cc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
90479828 182502 5 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4794409 182502 5 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
57413288 75470 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048614 75470 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
51357276 181425 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194127 182613 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 182613 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
52936292 181528 23 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
131986179 164245 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218348 164245 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
11245322 76789 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL207753 76789 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
162646017 178892 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4740846 178892 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
11773976 74432 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 2 3 5.7 CC(C)NC(=O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL203126 74432 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 2 3 5.7 CC(C)NC(=O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
46941175 61483 20 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL1773261 61483 20 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
44409878 140328 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 419 7 2 4 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(N)=O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL381958 140328 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 419 7 2 4 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(N)=O)cc1 10.1016/j.bmcl.2006.01.007
51350270 58531 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
CHEMBL1688463 58531 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
51350274 58551 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1021/jm101405t
CHEMBL1688483 58551 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1021/jm101405t
57705851 163232 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1F 10.1021/acsmedchemlett.8b00213
CHEMBL4205882 163232 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1F 10.1021/acsmedchemlett.8b00213
155516879 169532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 446 7 1 4 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4443509 169532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 446 7 1 4 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
155522406 170059 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 456 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4c(C)cccc4C)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4451050 170059 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 456 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4c(C)cccc4C)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
46231597 198511 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 352 4 1 5 3.9 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc(C)c1C#N 10.1016/j.bmcl.2009.10.052
CHEMBL596667 198511 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 352 4 1 5 3.9 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc(C)c1C#N 10.1016/j.bmcl.2009.10.052
57398937 69671 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 340 8 1 3 4.8 COc1ccc(COc2ccc(C(C=C(C)C)CC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939641 69671 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 340 8 1 3 4.8 COc1ccc(COc2ccc(C(C=C(C)C)CC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
122185450 122179 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 341 7 1 5 4.5 CCO[C@@H](CC(=O)O)c1ccc(Oc2noc3c(C)cccc23)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604060 122179 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 341 7 1 5 4.5 CCO[C@@H](CC(=O)O)c1ccc(Oc2noc3c(C)cccc23)cc1 10.1016/j.bmc.2015.07.028
90644298 111473 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 391 8 1 4 4.6 COC(Cc1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1)C(=O)O 10.1016/j.bmcl.2014.04.065
CHEMBL3288356 111473 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 391 8 1 4 4.6 COC(Cc1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1)C(=O)O 10.1016/j.bmcl.2014.04.065
121294346 179544 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.6 COCC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4748658 179544 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.6 COCC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
146314488 180559 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 451 10 1 4 6.1 COc1ccc(C(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4760668 180559 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 451 10 1 4 6.1 COc1ccc(C(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
67085761 156483 0 None 12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4073525 156483 0 None 12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
58218640 158376 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4095599 158376 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145979171 165974 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4279126 165974 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
54757737 65016 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1F 10.1021/jm2005699
CHEMBL1829165 65016 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1F 10.1021/jm2005699
51350273 58550 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688482 58550 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
71613094 89556 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381298 89556 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
75511307 121951 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3Cl)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601008 121951 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3Cl)no2)cc1 10.1016/j.bmcl.2015.06.018
71460190 80252 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2)c1 10.1021/ml300133f
CHEMBL2151292 80252 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2)c1 10.1021/ml300133f
71454737 80263 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 512 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)c4ccccc4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151302 80263 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 512 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)c4ccccc4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
1050 1871 86 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1871 86 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1871 86 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
57391958 69672 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 326 7 1 3 4.5 COc1ccc(COc2ccc(C(CC(=O)O)=C(C)C)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939642 69672 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 326 7 1 3 4.5 COc1ccc(COc2ccc(C(CC(=O)O)=C(C)C)cc2)cc1 10.1016/j.bmcl.2011.10.118
57391960 69681 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939651 69681 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
130253300 158565 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4097617 158565 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
137659366 158884 0 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 391 5 1 4 5.1 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4101071 158884 0 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 391 5 1 4 5.1 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12 10.1021/acs.jmedchem.7b00210
145946817 167032 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4248694 167032 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4300846 167032 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
118642390 162134 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4170346 162134 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
142738575 162435 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 283 4 2 1 4.0 O=C(O)CCc1ccc2[nH]c(-c3ccccc3F)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4175260 162435 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 283 4 2 1 4.0 O=C(O)CCc1ccc2[nH]c(-c3ccccc3F)cc2c1 10.1021/acsmedchemlett.7b00460
46231546 198923 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c(C)c1 10.1016/j.bmcl.2009.10.052
CHEMBL599280 198923 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c(C)c1 10.1016/j.bmcl.2009.10.052
118719473 115036 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 498 12 1 6 4.8 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353261 115036 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 498 12 1 6 4.8 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
122189682 122842 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 375 7 2 4 3.6 CC(C)(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616662 122842 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 375 7 2 4 3.6 CC(C)(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
137642174 160671 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4091100 160671 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117940 160671 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
90372616 141701 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
71615467 89559 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 538 9 1 7 4.9 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381301 89559 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 538 9 1 7 4.9 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
1646307 94561 12 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 385 7 1 4 4.7 O=C(O)CCCCCN1C(=O)/C(=C\c2cccc3ccccc23)SC1=S 10.1021/jm7012425
CHEMBL254859 94561 12 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 385 7 1 4 4.7 O=C(O)CCCCCN1C(=O)/C(=C\c2cccc3ccccc23)SC1=S 10.1021/jm7012425
118623088 141595 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883407 141595 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
134130352 141613 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 141613 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
58319098 86115 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1ccc(C)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315541 86115 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1ccc(C)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
145976935 163359 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 434 7 1 4 6.2 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)SCC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4207283 163359 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 434 7 1 4 6.2 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)SCC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
127029851 138333 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
CHEMBL3781779 138333 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
24825489 86895 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 317 6 2 2 4.6 O=C(O)Cc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL233223 86895 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 317 6 2 2 4.6 O=C(O)Cc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
46231485 198632 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccccc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL597436 198632 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccccc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
53248848 61839 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 61839 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
54580625 61836 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777873 61836 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
54586485 61828 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777865 61828 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
71615470 89562 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)ccc2F)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381304 89562 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)ccc2F)c(Cl)c1 10.1016/j.bmcl.2013.03.060
145976845 163179 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 484 11 1 6 4.4 COCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4205241 163179 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 484 11 1 6 4.4 COCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
54583099 61482 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccc(-c2cccc(CNc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
CHEMBL1773260 61482 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccc(-c2cccc(CNc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
44409699 139813 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.7 CC(CC(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380719 139813 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.7 CC(CC(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
134130859 141651 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 416 6 1 2 6.9 CC1(C)CCC=C1c1cccc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883983 141651 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 416 6 1 2 6.9 CC1(C)CCC=C1c1cccc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)c1 10.1021/acsmedchemlett.6b00443
24825505 147743 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 285 7 2 3 3.3 COc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL393661 147743 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 285 7 2 3 3.3 COc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
10131213 178749 3 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 252 3 1 2 2.6 O=C(O)COc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
CHEMBL473459 178749 3 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 252 3 1 2 2.6 O=C(O)COc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
137633536 155754 0 None -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based 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 -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based 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
137647721 157288 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4083440 157288 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
82051616 158910 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
CHEMBL4101323 158910 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
54584097 61472 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 382 6 1 2 3.9 O=C(O)CCc1ccc(OCc2ccccc2)c(I)c1 10.1021/ml100106c
CHEMBL1773250 61472 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 382 6 1 2 3.9 O=C(O)CCc1ccc(OCc2ccccc2)c(I)c1 10.1021/ml100106c
75511312 121988 4 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 402 7 1 5 4.1 O=C(O)CCc1ccc(OCc2nc(-c3cccc(Br)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601049 121988 4 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 402 7 1 5 4.1 O=C(O)CCc1ccc(OCc2nc(-c3cccc(Br)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
137629014 160438 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4063785 160438 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116078 160438 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
54580624 61823 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777860 61823 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
118623101 167028 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167028 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167028 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
118642344 141590 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883380 141590 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
91801188 169008 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4435837 169008 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
134151755 153914 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3976110 153914 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990146 153914 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137630599 160546 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1 10.1016/j.ejmech.2017.01.005
CHEMBL4072869 160546 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1 10.1016/j.ejmech.2017.01.005
CHEMBL4116895 160546 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1 10.1016/j.ejmech.2017.01.005
131986090 163740 0 None 5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4212041 163740 0 None 5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145967994 164236 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 399 7 1 5 3.5 Cc1ccc(C)n1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4218236 164236 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 399 7 1 5 3.5 Cc1ccc(C)n1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
127048827 139753 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 371 6 2 5 3.6 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccc(F)cc3)c2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805879 139753 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 371 6 2 5 3.6 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccc(F)cc3)c2)s1 10.1016/j.bmc.2016.04.065
142738582 183938 0 None 42 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4847662 183938 0 None 42 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
46854655 391 43 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.ejmech.2018.09.071
6485 391 43 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.ejmech.2018.09.071
CHEMBL1829173 391 43 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.ejmech.2018.09.071
46854655 391 43 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2016.10.074
6485 391 43 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2016.10.074
CHEMBL1829173 391 43 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2016.10.074
57706778 80385 25 None -8 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
CHEMBL2152070 80385 25 None -8 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
24857285 75267 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047157 75267 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
131986027 163386 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207592 163386 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986061 163564 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209834 163564 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
67058307 122119 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3cc(C(F)(F)F)ccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3603843 122119 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3cc(C(F)(F)F)ccc32)cc1 10.1016/j.bmc.2015.07.028
67058222 122171 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(F)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604052 122171 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(F)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
122185447 122176 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604057 122176 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2F)cc1 10.1016/j.bmc.2015.07.028
45107324 122182 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 366 8 1 3 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C4CC4)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604063 122182 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 366 8 1 3 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C4CC4)cccc32)cc1 10.1016/j.bmc.2015.07.028
1050 1871 86 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
11595431 1871 86 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
CHEMBL207881 1871 86 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
134138870 147139 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 491 9 2 5 5.2 Cc1cc(OCCC(C)O)cc(C)c1-c1ccc(F)c(COc2cc3c(cn2)[C@@H]2C(C(=O)O)[C@@H]2C3)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3931755 147139 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 491 9 2 5 5.2 Cc1cc(OCCC(C)O)cc(C)c1-c1ccc(F)c(COc2cc3c(cn2)[C@@H]2C(C(=O)O)[C@@H]2C3)c1 10.1016/j.bmcl.2016.10.074
57413290 75473 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048617 75473 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
46854655 391 43 None 1 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
6485 391 43 None 1 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
CHEMBL1829173 391 43 None 1 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
145947998 167155 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167155 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167155 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
11245322 76789 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL207753 76789 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
71575419 89541 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381282 89541 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
54584572 61841 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777878 61841 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
90644292 111467 0 None 10 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288350 111467 0 None 10 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
145983698 165867 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 382 7 1 5 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4277181 165867 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 382 7 1 5 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC)cc3O2)cc1 10.1016/j.bmc.2018.10.019
67087160 181762 0 None -6 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 181762 0 None -6 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
90644293 111468 0 None -13 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
CHEMBL3288351 111468 0 None -13 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
90644301 111476 0 None -9 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288359 111476 0 None -9 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
57706778 80385 25 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL2152070 80385 25 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
57706778 80385 25 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
CHEMBL2152070 80385 25 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
134157016 153900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3985181 153900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990065 153900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137655619 158152 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 340 6 1 4 4.0 CN(C)c1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4093180 158152 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 340 6 1 4 4.0 CN(C)c1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
87265393 158734 0 None -4 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4099410 158734 0 None -4 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
58218699 158869 0 None 2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4100898 158869 0 None 2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
137631654 155759 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 449 8 1 5 5.7 O=C(O)CCc1ccc(-c2ccc3c(OCc4ccccc4)nn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
CHEMBL4065429 155759 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 449 8 1 5 5.7 O=C(O)CCc1ccc(-c2ccc3c(OCc4ccccc4)nn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
137641734 157498 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4085805 157498 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
142738556 162218 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 333 4 2 1 4.9 O=C(O)CCc1ccc2[nH]c(-c3ccccc3C(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4171817 162218 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 333 4 2 1 4.9 O=C(O)CCc1ccc2[nH]c(-c3ccccc3C(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
71458348 80261 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 9 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151300 80261 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 9 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
75511315 121997 5 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601058 121997 5 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
137647721 157288 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4083440 157288 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
44634022 64993 1 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccn2)cc1 10.1021/jm2005699
CHEMBL1829143 64993 1 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccn2)cc1 10.1021/jm2005699
71615671 89574 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cc(C)cc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381316 89574 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cc(C)cc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
122189737 122876 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 7 2 4 3.3 Cc1ccc(OC(C)C(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1C 10.1016/j.bmc.2015.09.010
CHEMBL3616719 122876 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 7 2 4 3.3 Cc1ccc(OC(C)C(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1C 10.1016/j.bmc.2015.09.010
145956160 161946 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 522 8 1 5 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(Cl)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167397 161946 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 522 8 1 5 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(Cl)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
145972020 162575 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 457 8 2 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)o2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4177506 162575 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 457 8 2 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)o2)cc1 10.1016/j.ejmech.2018.04.023
118637974 161489 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4160127 161489 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
131986164 164067 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216016 164067 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
51049992 145086 4 None -23 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL3915620 145086 4 None -23 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
54757738 65017 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 299 3 1 2 3.5 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
CHEMBL1829166 65017 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 299 3 1 2 3.5 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
23136411 58524 0 None 11 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
CHEMBL1688457 58524 0 None 11 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
90151518 156372 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 6 1 5 5.6 Cc1cccc(C)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4072314 156372 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 6 1 5 5.6 Cc1cccc(C)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
46231598 200513 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 4 4.5 O=C1NC(=O)C(Cc2ccc(Oc3cccc4ccccc34)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL609615 200513 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 4 4.5 O=C1NC(=O)C(Cc2ccc(Oc3cccc4ccccc34)cc2)S1 10.1016/j.bmcl.2009.10.052
122189672 122837 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.7 CC(Oc1ccccc1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616652 122837 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.7 CC(Oc1ccccc1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
122189676 122838 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 351 7 2 4 2.8 CC(Oc1ccccc1F)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616656 122838 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 351 7 2 4 2.8 CC(Oc1ccccc1F)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
134149615 148044 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
CHEMBL3939004 148044 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
145973937 164034 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 487 10 2 6 5.2 COc1ccc(C(Cc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c2ccccc2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4215600 164034 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 487 10 2 6 5.2 COc1ccc(C(Cc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c2ccccc2)cc1 10.1016/j.ejmech.2017.09.019
145980455 166159 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 365 6 2 4 3.7 O=C(O)CCc1ccc(NCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4282779 166159 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 365 6 2 4 3.7 O=C(O)CCc1ccc(NCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
20993091 61819 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 310 5 1 2 4.8 O=C(O)CCc1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777856 61819 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 310 5 1 2 4.8 O=C(O)CCc1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
54584572 61841 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777878 61841 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
134149615 148044 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
CHEMBL3939004 148044 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
127033820 138249 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780713 138249 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
118637996 141638 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 141638 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 141638 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
145949955 162360 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccn4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4173953 162360 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccn4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
71562317 86112 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
CHEMBL2315538 86112 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
71562423 86117 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 298 3 1 1 4.1 Cc1cc(Cl)ccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315543 86117 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 298 3 1 1 4.1 Cc1cc(Cl)ccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
145972304 163992 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 423 8 2 6 3.9 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc4c(c3)CCC4)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4215103 163992 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 423 8 2 6 3.9 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc4c(c3)CCC4)s2)cc1 10.1016/j.ejmech.2017.09.019
118637996 141638 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 141638 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 141638 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
46231843 198821 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 5 1 6 4.4 COc1cc(Oc2ncc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL598732 198821 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 5 1 6 4.4 COc1cc(Oc2ncc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
134130352 141613 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 141613 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
134143899 149706 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 5 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
CHEMBL3952316 149706 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 5 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
24857286 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
6484 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
CHEMBL1829174 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
DB12491 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
146948845 185298 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 522 11 1 5 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CCc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4868224 185298 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 522 11 1 5 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CCc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/acs.jmedchem.1c00031
57414539 75268 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047158 75268 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
24857286 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
6484 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
CHEMBL1829174 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
DB12491 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
24857286 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
6484 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
CHEMBL1829174 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
DB12491 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
90644301 111476 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288359 111476 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
11190525 75472 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048616 75472 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
162667620 181975 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 181975 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
162644059 181242 0 None 45 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None 45 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
67087100 182016 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182016 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
145952952 161941 0 None 1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167323 161941 0 None 1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
131986027 163386 0 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207592 163386 0 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986112 163865 0 None 3 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213548 163865 0 None 3 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986072 163900 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213937 163900 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
134131511 141626 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 141626 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
24857286 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
6484 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
CHEMBL1829174 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
DB12491 1594 66 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
44409843 139875 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380884 139875 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
51350138 58541 0 None 660 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL1688473 58541 0 None 660 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
46941175 61483 20 None -1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61483 20 None -1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
60195037 81310 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 495 12 2 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
CHEMBL2163925 81310 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 495 12 2 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
44409676 74653 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 7 3 4 4.7 O=C(NO)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL203297 74653 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 7 3 4 4.7 O=C(NO)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
57705749 164300 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4218995 164300 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
121294749 182159 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 542 11 1 5 6.2 COc1ccc(C(=O)N(C)c2ccccc2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4789994 182159 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 542 11 1 5 6.2 COc1ccc(C(=O)N(C)c2ccccc2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
58218607 155399 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4061093 155399 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57325842 73758 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022580 73758 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
58230598 182537 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 182537 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
122189683 122843 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 389 7 2 4 4.0 CC(Oc1cccc(C(C)(C)C)c1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616663 122843 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 389 7 2 4 4.0 CC(Oc1cccc(C(C)(C)C)c1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
137649555 156788 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4077507 156788 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
90644292 111467 0 None -10 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288350 111467 0 None -10 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
137658391 159101 0 None -1 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
CHEMBL4103681 159101 0 None -1 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
54586485 61828 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777865 61828 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
46231842 198820 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 397 5 1 5 4.7 COc1cc(Oc2ccc(Cl)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL598731 198820 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 397 5 1 5 4.7 COc1cc(Oc2ccc(Cl)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
66562389 89936 0 None 58 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 286 3 1 1 3.4 O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
CHEMBL2386360 89936 0 None 58 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 286 3 1 1 3.4 O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
145965968 163694 0 None -4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4211335 163694 0 None -4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
137656526 159206 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4105013 159206 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
127046662 139510 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 10 1 5 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC(C)C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3800255 139510 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 10 1 5 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC(C)C)c1 10.1016/j.ejmech.2016.03.054
46231779 199194 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 350 4 1 5 3.9 O=C1NC(=O)C(Cc2ccc(Oc3cc4ccccc4cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL601420 199194 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 350 4 1 5 3.9 O=C1NC(=O)C(Cc2ccc(Oc3cc4ccccc4cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
145962064 161687 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 474 8 2 5 5.1 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4163436 161687 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 474 8 2 5 5.1 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
71562316 86111 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.3 O=C(O)[C@H]1C[C@@H]1c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315537 86111 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.3 O=C(O)[C@H]1C[C@@H]1c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
66562390 89934 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 10.1021/ml4000673
CHEMBL2386358 89934 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 10.1021/ml4000673
44409929 76072 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 345 7 2 3 5.2 O=C(O)/C=C/c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205960 76072 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 345 7 2 3 5.2 O=C(O)/C=C/c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
127033352 138491 0 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 272 8 1 1 4.4 CCCCCCCC#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3785789 138491 0 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 272 8 1 1 4.4 CCCCCCCC#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
66562387 89942 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386366 89942 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
71613096 89558 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381300 89558 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
168278906 190437 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 438 10 1 4 5.9 Cc1ccc(OCC(C)C)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5186963 190437 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 438 10 1 4 5.9 Cc1ccc(OCC(C)C)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
2214962 94223 8 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 283 7 2 3 3.6 C=CCOc1ccc(CNc2cccc(C(=O)O)c2)cc1 10.1021/jm7012425
CHEMBL252528 94223 8 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 283 7 2 3 3.6 C=CCOc1ccc(CNc2cccc(C(=O)O)c2)cc1 10.1021/jm7012425
91824140 150544 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 425 7 1 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(-c3ccccc3C)cn3ncnc23)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3958983 150544 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 425 7 1 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(-c3ccccc3C)cn3ncnc23)cc1 10.1016/j.bmcl.2016.10.074
118623101 167028 0 None -12 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167028 0 None -12 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167028 0 None -12 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
90357232 141720 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884803 141720 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
122185446 122175 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1cccc(OCc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmc.2015.07.028
CHEMBL3604056 122175 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1cccc(OCc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmc.2015.07.028
122189685 122813 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 349 8 2 5 2.3 COc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616479 122813 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 349 8 2 5 2.3 COc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
6483 3823 49 None -13 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assayAgonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3823 49 None -13 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assayAgonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3823 49 None -13 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assayAgonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
145987974 166525 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 362 7 1 5 3.1 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CO2 10.1016/j.bmc.2018.10.019
CHEMBL4289597 166525 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 362 7 1 5 3.1 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CO2 10.1016/j.bmc.2018.10.019
137655393 158188 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4093521 158188 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
137529979 163623 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 473 6 3 4 5.2 CNC(=O)c1cc(C)c(-c2ccc(F)c3c2CC[C@H]3Nc2ccc([C@H]3C[C@@H]3C(=O)O)nc2)c(C)c1 10.1021/acsmedchemlett.8b00343
CHEMBL4210588 163623 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 473 6 3 4 5.2 CNC(=O)c1cc(C)c(-c2ccc(F)c3c2CC[C@H]3Nc2ccc([C@H]3C[C@@H]3C(=O)O)nc2)c(C)c1 10.1021/acsmedchemlett.8b00343
122189678 122840 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1ccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1 10.1016/j.bmc.2015.09.010
CHEMBL3616658 122840 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1ccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1 10.1016/j.bmc.2015.09.010
137629795 160636 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4063221 160636 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117645 160636 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
137633561 155810 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(COc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4065921 155810 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(COc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
54582631 61830 0 None -1 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777867 61830 0 None -1 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
54581633 61832 0 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777869 61832 0 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
131986072 163900 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213937 163900 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986179 164245 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218348 164245 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
57413289 75471 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048615 75471 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11398822 75479 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048624 75479 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
46854655 391 43 None -8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None -8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None -8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
118145140 174813 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4575265 174813 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
145967748 162959 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 496 12 1 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4202452 162959 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 496 12 1 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
118645526 182398 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4793322 182398 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
155569585 175635 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 419 7 2 3 5.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4593950 175635 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 419 7 2 3 5.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1F 10.1016/j.ejmech.2019.06.087
127047527 139342 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1Cl 10.1016/j.ejmech.2016.03.054
CHEMBL3799274 139342 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1Cl 10.1016/j.ejmech.2016.03.054
155527415 170658 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 453 7 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C#N)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4459626 170658 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 453 7 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C#N)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
57706778 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
CHEMBL2152070 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
162674275 182409 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 491 10 1 4 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4793427 182409 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 491 10 1 4 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1021/acs.jmedchem.0c00843
58218740 155904 0 None 45 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4067052 155904 0 None 45 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
137646482 157209 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082459 157209 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218551 158501 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4096887 158501 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137633394 155883 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 541 8 1 6 5.4 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4066815 155883 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 541 8 1 6 5.4 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
90151501 158209 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 510 7 1 7 4.5 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(F)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4093944 158209 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 510 7 1 7 4.5 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(F)cn1 10.1021/acs.jmedchem.7b00982
145980470 166183 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 420 6 1 4 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4283222 166183 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 420 6 1 4 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
156703595 191316 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 438 10 1 5 5.1 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5200141 191316 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 438 10 1 5 5.1 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
58172971 122153 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 8 1 3 5.4 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(C)c1 10.1016/j.bmc.2015.07.028
CHEMBL3604035 122153 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 8 1 3 5.4 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(C)c1 10.1016/j.bmc.2015.07.028
67085761 156483 0 None -12 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4073525 156483 0 None -12 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137651358 156601 0 None -2 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 375 5 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4075162 156601 0 None -2 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 375 5 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12 10.1021/acs.jmedchem.7b00210
118144953 175075 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2ccc3c(n2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4581212 175075 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2ccc3c(n2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
58319121 86121 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 284 3 1 1 3.8 O=C(O)CCc1ccc(C#Cc2ccccc2Cl)cc1 10.1021/jm301470a
CHEMBL2315547 86121 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 284 3 1 1 3.8 O=C(O)CCc1ccc(C#Cc2ccccc2Cl)cc1 10.1021/jm301470a
1855223 94198 15 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 404 8 1 7 4.8 COc1ccc(CSc2nnc(SCc3ccc(C(=O)O)cc3)s2)cc1 10.1021/jm7012425
CHEMBL252330 94198 15 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 404 8 1 7 4.8 COc1ccc(CSc2nnc(SCc3ccc(C(=O)O)cc3)s2)cc1 10.1021/jm7012425
71257551 150060 18 None -14 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3955132 150060 18 None -14 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1016/j.bmcl.2016.10.074
127051660 139737 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccccc1NC(=O)c1nnc(COc2ccc(CCC(=O)O)cc2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805668 139737 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccccc1NC(=O)c1nnc(COc2ccc(CCC(=O)O)cc2)s1 10.1016/j.bmc.2016.04.065
145975293 163034 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccccc1OCc1nnc(C(=O)Nc2ccc(CCC(=O)O)cc2)s1 10.1016/j.ejmech.2017.09.019
CHEMBL4203402 163034 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccccc1OCc1nnc(C(=O)Nc2ccc(CCC(=O)O)cc2)s1 10.1016/j.ejmech.2017.09.019
118719717 115162 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.1 Cc1cc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)ccc1OCC(=O)O 10.1016/j.bmc.2014.11.016
CHEMBL3353738 115162 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.1 Cc1cc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)ccc1OCC(=O)O 10.1016/j.bmc.2014.11.016
168276115 189679 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 450 10 1 4 6.0 Cc1ccc(OCC2CCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5175597 189679 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 450 10 1 4 6.0 Cc1ccc(OCC2CCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
145977707 163404 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(C)c(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
CHEMBL4207787 163404 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(C)c(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
90372616 141701 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
51349861 58521 0 None 77 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
CHEMBL1688454 58521 0 None 77 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
25150119 185804 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 274 3 1 1 3.1 C#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL487570 185804 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 274 3 1 1 3.1 C#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
137636167 155446 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
CHEMBL4061630 155446 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
145954794 161973 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 9 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(Cc4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167766 161973 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 9 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(Cc4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
155561223 175109 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2cc3c(cc2F)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4581859 175109 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2cc3c(cc2F)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
54582631 61830 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777867 61830 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
145968322 164468 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 380 6 1 4 5.3 Cc1ccsc1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4226029 164468 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 380 6 1 4 5.3 Cc1ccsc1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
145976267 163037 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4203431 163037 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
54583581 61831 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777868 61831 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
24825487 152744 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 345 8 2 2 5.4 O=C(O)CCCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL397776 152744 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 345 8 2 2 5.4 O=C(O)CCCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
137636167 155446 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
CHEMBL4061630 155446 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
137657972 159057 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4103243 159057 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
137656526 159206 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4105013 159206 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
24857286 1594 66 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
6484 1594 66 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
CHEMBL1829174 1594 66 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
DB12491 1594 66 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
57414267 75259 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047149 75259 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
23642299 75277 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047168 75277 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857375 75278 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047169 75278 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
131986051 163331 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206968 163331 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
155526793 170628 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4459220 170628 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
15603946 111167 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
CHEMBL3286409 111167 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
118129998 156781 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 156781 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
71613518 89545 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381287 89545 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
131986147 164227 0 None 6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218110 164227 0 None 6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
90644290 111465 0 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288348 111465 0 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
118642384 141633 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883790 141633 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
155551584 173427 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4542487 173427 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
164611439 184651 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1ccc(Cl)cc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4858086 184651 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1ccc(Cl)cc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
51350272 58533 0 None 107 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL1688465 58533 0 None 107 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
66562386 89939 0 None 562 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 3 1 2 3.4 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386363 89939 0 None 562 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 3 1 2 3.4 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
122184685 121937 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2coc(-c3cccc(Cl)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600994 121937 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2coc(-c3cccc(Cl)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
57706778 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.1c00031
CHEMBL2152070 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.1c00031
57706778 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL2152070 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
57706778 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152070 80385 25 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
155533810 171299 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 428 7 1 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4469136 171299 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 428 7 1 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
121294307 179837 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 610 13 1 7 6.6 COc1ccc(C(=O)N(CC(C)(C)C#N)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4752289 179837 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 610 13 1 7 6.6 COc1ccc(C(=O)N(CC(C)(C)C#N)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
24857286 1594 66 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
86803191 121941 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2ncc(-c3ccccc3)o2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600998 121941 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2ncc(-c3ccccc3)o2)cc1 10.1016/j.bmcl.2015.06.018
122185434 122150 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 2 3 3.8 CCOC(CC(=O)O)c1ccc(NC(=O)c2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604032 122150 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 2 3 3.8 CCOC(CC(=O)O)c1ccc(NC(=O)c2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
818213 154938 9 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 345 5 2 3 3.9 O=C(O)c1ccc(NC(=O)c2ccc(C(=O)c3ccccc3)cc2)cc1 10.1021/jm7012425
CHEMBL404008 154938 9 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 345 5 2 3 3.9 O=C(O)c1ccc(NC(=O)c2ccc(C(=O)c3ccccc3)cc2)cc1 10.1021/jm7012425
58319138 86124 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2ccccc2O)cc1 10.1021/jm301470a
CHEMBL2315550 86124 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2ccccc2O)cc1 10.1021/jm301470a
134130696 141605 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 141605 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
155516498 169555 0 None -3 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4443853 169555 0 None -3 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
137657972 159057 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4103243 159057 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
46231654 199999 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cccc(C(F)(F)F)n3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL606213 199999 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cccc(C(F)(F)F)n3)cc2)S1 10.1016/j.bmcl.2009.10.052
127052270 139703 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 343 6 2 6 3.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccco3)c2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805303 139703 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 343 6 2 6 3.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccco3)c2)s1 10.1016/j.bmc.2016.04.065
118637973 162193 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171391 162193 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
54585039 61474 5 None 17 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/jm300215x
CHEMBL1773252 61474 5 None 17 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/jm300215x
24825482 87562 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 7 2 3 5.3 CC(C(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234268 87562 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 7 2 3 5.3 CC(C(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
127027729 137165 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.5 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3Cl)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758719 137165 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.5 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3Cl)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
127025867 137252 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 395 6 1 6 4.1 CC(C)n1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
CHEMBL3759448 137252 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 395 6 1 6 4.1 CC(C)n1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
797771 94221 14 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 312 6 0 7 3.1 COC(=O)CSc1nnc(SCc2ccccc2)s1 10.1021/jm7012425
CHEMBL252526 94221 14 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 312 6 0 7 3.1 COC(=O)CSc1nnc(SCc2ccccc2)s1 10.1021/jm7012425
1201156 154587 16 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 297 5 1 5 2.3 O=C(O)CCCN1C(=O)/C(=C\c2ccco2)SC1=S 10.1021/jm7012425
CHEMBL402053 154587 16 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 297 5 1 5 2.3 O=C(O)CCCN1C(=O)/C(=C\c2ccco2)SC1=S 10.1021/jm7012425
46854655 391 43 None -8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
6485 391 43 None -8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL1829173 391 43 None -8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
145965455 163590 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 546 12 1 7 4.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4210139 163590 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 546 12 1 7 4.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
127048843 139726 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 387 6 2 5 4.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3cccc(Cl)c3)c2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805558 139726 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 387 6 2 5 4.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3cccc(Cl)c3)c2)s1 10.1016/j.bmc.2016.04.065
118623088 141595 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 141595 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
57414540 75270 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047160 75270 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414676 75272 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047163 75272 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414677 75273 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047164 75273 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857376 75279 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047170 75279 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
121294284 180775 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 613 12 1 6 7.4 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4763105 180775 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 613 12 1 6 7.4 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
121294846 182970 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc(C(CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4800194 182970 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc(C(CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
162664735 181504 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 181504 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
67087041 181789 0 None -14 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 181789 0 None -14 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194159 182479 0 None -4 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 182479 0 None -4 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
162674998 182809 0 None -5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 182809 0 None -5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
118645756 180880 3 None -2 3 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 180880 3 None -2 3 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
60195036 81309 0 None 630 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 481 12 2 5 5.1 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
CHEMBL2163924 81309 0 None 630 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 481 12 2 5 5.1 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
60195040 81382 0 None 5248 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 7 2 2 5.7 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL2164241 81382 0 None 5248 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 7 2 2 5.7 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
51350135 58538 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688470 58538 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cc2)c1 10.1021/jm101405t
51350136 58539 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688471 58539 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cc2)c1 10.1021/jm101405t
145974173 164047 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 490 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4215771 164047 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 490 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
168294830 191635 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
CHEMBL5205109 191635 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
87262743 158235 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4094160 158235 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
145989151 166649 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3c(Cl)cccc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4291567 166649 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3c(Cl)cccc3O2)cc1 10.1016/j.bmc.2018.10.019
51031010 156090 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4069191 156090 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
23082861 58559 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 298 9 1 2 4.1 O=C(O)CCc1ccc(OCCCCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688491 58559 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 298 9 1 2 4.1 O=C(O)CCc1ccc(OCCCCc2ccccc2)cc1 10.1021/jm101405t
23111708 73701 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/ml1000855
CHEMBL2022246 73701 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/ml1000855
122185431 122147 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 338 8 1 5 3.4 CCOC(Cc1nnn[nH]1)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604029 122147 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 338 8 1 5 3.4 CCOC(Cc1nnn[nH]1)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
58218671 156656 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 7 1 4 4.3 CCOc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4075885 156656 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 7 1 4 4.3 CCOc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137661475 158911 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4101348 158911 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
54582629 61827 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 61827 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
145950126 162310 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 511 7 1 4 6.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4173085 162310 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 511 7 1 4 6.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
24825492 149010 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/ml100106c
CHEMBL394666 149010 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/ml100106c
44409698 76402 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 8 1 3 5.1 CN(C)C(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206779 76402 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 8 1 3 5.1 CN(C)C(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
145967263 163893 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 469 11 1 7 3.6 CO/N=C(\COc1ccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2017.07.001
CHEMBL4213829 163893 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 469 11 1 7 3.6 CO/N=C(\COc1ccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2017.07.001
54757736 65015 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
CHEMBL1829164 65015 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
3367 1134 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/ml100106c
46216676 1134 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/ml100106c
CHEMBL604126 1134 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/ml100106c
127049161 139768 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
CHEMBL3806055 139768 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
145963593 160866 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 4.8 COc1ccc(C(OCCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)cc1 10.1016/j.bmcl.2018.03.051
CHEMBL4126802 160866 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 4.8 COc1ccc(C(OCCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)cc1 10.1016/j.bmcl.2018.03.051
155517179 169576 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
CHEMBL4444223 169576 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
1050 1871 86 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1871 86 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1871 86 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
145962072 161818 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 505 7 1 3 6.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4165184 161818 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 505 7 1 3 6.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
127048844 139668 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1nnc(C(=O)Nc2ccc(OCc3ccccc3)cc2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3804883 139668 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1nnc(C(=O)Nc2ccc(OCc3ccccc3)cc2)s1 10.1016/j.bmc.2016.04.065
57414402 75262 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047152 75262 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414543 75271 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
CHEMBL2047162 75271 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
57414679 75275 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
CHEMBL2047166 75275 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
131986115 164163 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4217348 164163 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
46231780 199121 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 415 4 1 4 5.4 Cc1cc(Oc2ccc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL600799 199121 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 415 4 1 4 5.4 Cc1cc(Oc2ccc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
90644299 111474 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288357 111474 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
162667620 181975 0 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 181975 0 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
131986075 163357 0 None 2 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207273 163357 0 None 2 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
11674915 58554 1 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL1688486 58554 1 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
118645715 180905 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764729 180905 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
118623088 141595 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 141595 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
73345869 89931 0 None 75 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 321 5 1 2 3.7 N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386355 89931 0 None 75 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 321 5 1 2 3.7 N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
66562488 89940 0 None 64 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 4 1 1 4.3 O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F 10.1021/ml4000673
CHEMBL2386364 89940 0 None 64 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 4 1 1 4.3 O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F 10.1021/ml4000673
145970463 164624 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
CHEMBL4228406 164624 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
46941175 61483 20 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
CHEMBL1773261 61483 20 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
46941175 61483 20 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61483 20 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
46941175 61483 20 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
CHEMBL1773261 61483 20 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
57402427 69678 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 6 1 2 4.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939648 69678 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 6 1 2 4.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.10.118
121294843 181922 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 543 11 1 6 5.6 COc1ccc(C(=O)N(C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4786992 181922 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 543 11 1 6 5.6 COc1ccc(C(=O)N(C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
137638341 156228 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 544 7 1 7 5.0 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4070721 156228 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 544 7 1 7 5.0 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
23111671 73709 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
CHEMBL2022254 73709 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
58230552 181637 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
853224 94139 11 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94139 11 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
51350134 58537 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 7 1 2 6.3 Cc1cccc(C)c1-c1cccc(CSc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688469 58537 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 7 1 2 6.3 Cc1cccc(C)c1-c1cccc(CSc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
168289957 191033 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 398 13 1 4 5.7 COc1ccc(/C=C/c2cc(OC)cc(OCCCCCCCC(=O)O)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5195742 191033 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 398 13 1 4 5.7 COc1ccc(/C=C/c2cc(OC)cc(OCCCCCCCC(=O)O)c2)cc1 10.1016/j.ejmech.2021.114061
142738583 161804 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 293 5 2 1 4.4 CCc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
CHEMBL4165039 161804 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 293 5 2 1 4.4 CCc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
142738569 162194 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3cccc(Br)c3)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4171403 162194 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3cccc(Br)c3)cc2c1 10.1021/acsmedchemlett.7b00460
1052 2290 81 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2290 81 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2290 81 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2290 81 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2290 81 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
145987969 166516 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 346 4 1 2 4.5 O=C(O)C#Cc1ccc(OCc2cccc(-c3cccc(F)c3)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4289432 166516 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 346 4 1 2 4.5 O=C(O)C#Cc1ccc(OCc2cccc(-c3cccc(F)c3)c2)cc1 10.1016/j.ejmech.2018.08.075
137638355 156287 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4071290 156287 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
60195125 3825 5 None -4 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3825 5 None -4 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3825 5 None -4 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
24825509 87518 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL234057 87518 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
127033353 138621 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 5 1 1 3.7 O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3787151 138621 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 5 1 1 3.7 O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
134134229 142723 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 assessed as induction of IP1 accumulationAgonist activity at human GPR40 assessed as induction of IP1 accumulation
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1021/acsmedchemlett.6b00360
CHEMBL3896657 142723 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 assessed as induction of IP1 accumulationAgonist activity at human GPR40 assessed as induction of IP1 accumulation
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1021/acsmedchemlett.6b00360
134134229 142723 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1016/j.bmcl.2016.10.054
CHEMBL3896657 142723 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1016/j.bmcl.2016.10.054
57706097 163190 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4205339 163190 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
58319126 86090 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 292 4 1 2 3.3 CC(=O)c1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315248 86090 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 292 4 1 2 3.3 CC(=O)c1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
54757734 65013 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 327 4 1 2 4.2 O=C(O)CCc1ccc(C#Cc2ccnc(-c3ccccc3)c2)cc1 10.1021/jm2005699
CHEMBL1829162 65013 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 327 4 1 2 4.2 O=C(O)CCc1ccc(C#Cc2ccnc(-c3ccccc3)c2)cc1 10.1021/jm2005699
54586984 61478 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
CHEMBL1773256 61478 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
23136477 58522 3 None -15 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL1688455 58522 3 None -15 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL4213909 58522 3 None -15 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
37289 165969 14 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCC(O)CCCCC(=O)O 10.1039/C7MD00130D
CHEMBL4279005 165969 14 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCC(O)CCCCC(=O)O 10.1039/C7MD00130D
127051856 140196 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL3817889 140196 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
145956671 161517 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4160566 161517 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
46231715 199264 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 334 4 1 5 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL601850 199264 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 334 4 1 5 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
25766502 122000 3 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 6 1 5 3.6 O=C(O)Cc1ccc(OCc2nc(-c3cccc(Cl)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601061 122000 3 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 6 1 5 3.6 O=C(O)Cc1ccc(OCc2nc(-c3cccc(Cl)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
127027011 137104 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 7 1 6 4.2 CC(C)Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
CHEMBL3758197 137104 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 7 1 6 4.2 CC(C)Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
51350406 58555 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1C 10.1021/jm101405t
CHEMBL1688487 58555 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1C 10.1021/jm101405t
10668 1922 11 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.bmcl.2021.127969
139600331 1922 11 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.bmcl.2021.127969
CHEMBL5169614 1922 11 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.bmcl.2021.127969
44572033 178996 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 548 13 1 5 7.8 O=C(O)CCc1ccc(OCc2ccc(CC(CCc3ccccn3)c3nc(-c4ccccc4)cs3)cc2)cc1 10.1016/j.bmcl.2008.10.085
CHEMBL474195 178996 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 548 13 1 5 7.8 O=C(O)CCc1ccc(OCc2ccc(CC(CCc3ccccn3)c3nc(-c4ccccc4)cs3)cc2)cc1 10.1016/j.bmcl.2008.10.085
90655862 110763 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265146 110763 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
57414680 75276 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047167 75276 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414542 76863 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047161 76863 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2079433 76863 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
131986140 162968 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202612 162968 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
67058227 118629 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427713 118629 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
122185436 122160 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604041 122160 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
67087246 182295 4 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
131986140 162968 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202612 162968 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986132 163307 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206640 163307 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986051 163331 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206968 163331 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118642372 161914 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166943 161914 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
71613314 89566 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381308 89566 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
149454889 169164 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3Cl)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4438440 169164 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3Cl)c2)cc1F 10.1016/j.ejmech.2019.06.087
67072752 86102 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315528 86102 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
67072752 86102 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL2315528 86102 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
58172999 122183 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 356 8 1 4 4.3 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3c(OC)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604064 122183 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 356 8 1 4 4.3 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3c(OC)cccc32)cc1 10.1016/j.bmc.2015.07.028
58218571 156938 0 None 17 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079421 156938 0 None 17 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
90151435 159171 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 554 8 1 7 5.6 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4104467 159171 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 554 8 1 7 5.6 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
162666840 181872 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 181872 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
58172989 111477 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288360 111477 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
71613519 89546 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381288 89546 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
71562770 86103 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315529 86103 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
145965707 163651 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4210871 163651 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
71451164 80251 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3ccc(CCC(=O)O)cc3)cc2)c1 10.1021/ml300133f
CHEMBL2151291 80251 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3ccc(CCC(=O)O)cc3)cc2)c1 10.1021/ml300133f
57706588 80258 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151298 80258 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
137638269 156334 0 None -8 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4071899 156334 0 None -8 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218640 158376 0 None -15 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4095599 158376 0 None -15 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
1202260 94593 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 313 5 1 5 2.8 O=C(O)CCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL255071 94593 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 313 5 1 5 2.8 O=C(O)CCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
25098573 2706 5 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm800970b
5587 2706 5 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm800970b
CHEMBL463785 2706 5 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm800970b
137633489 156059 0 None -9 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
CHEMBL4068825 156059 0 None -9 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
137647888 157176 0 None - 1 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 369 4 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@H]4C(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4082057 157176 0 None - 1 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 369 4 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@H]4C(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
23136477 58522 3 None -15 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
CHEMBL1688455 58522 3 None -15 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
CHEMBL4213909 58522 3 None -15 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
127046834 139129 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1ccnc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797836 139129 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1ccnc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
90151202 156829 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 461 6 1 5 5.0 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4078050 156829 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 461 6 1 5 5.0 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
24825509 87518 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234057 87518 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
145976145 163261 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 412 8 1 5 3.8 COc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4206179 163261 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 412 8 1 5 3.8 COc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
145971779 163920 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 378 7 1 3 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(SCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4214140 163920 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 378 7 1 3 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(SCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
66562388 89943 0 None 33 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386367 89943 0 None 33 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
60195125 3825 5 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3825 5 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3825 5 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
127027726 137303 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 5.2 COc1cccc(O[C@@H](CCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)c1 10.1016/j.ejmech.2015.12.049
CHEMBL3759866 137303 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 5.2 COc1cccc(O[C@@H](CCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)c1 10.1016/j.ejmech.2015.12.049
137641343 156515 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4074009 156515 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
153211729 172331 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 405 9 2 4 5.4 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4516052 172331 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 405 9 2 4 5.4 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
57705575 163600 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4210239 163600 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
134465785 175537 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 175537 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
54586984 61478 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
CHEMBL1773256 61478 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
71562314 86109 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.7 CC(CC(=O)O)c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315535 86109 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.7 CC(CC(=O)O)c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
25149901 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm2005699
CHEMBL488384 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm2005699
127030714 138556 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 254 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2=CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786524 138556 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 254 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2=CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
25149901 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL488384 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
25149901 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml4000673
CHEMBL488384 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml4000673
25149901 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml100106c
CHEMBL488384 186104 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml100106c
24825494 87604 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234468 87604 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2006.12.084
24825493 149320 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 295 6 2 3 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)s2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL394900 149320 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 295 6 2 3 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)s2)cc1 10.1016/j.bmcl.2006.12.084
137638911 156188 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4070298 156188 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
137638355 156287 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4071290 156287 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
137641343 156515 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4074009 156515 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
164626510 185755 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 549 8 1 4 7.1 C[C@H](C(=O)O)[C@@H](c1ccc2c(c1)O[C@@H](C1CCN([C@@H](C)c3cc(F)ccc3OC(F)(F)F)CC1)CC2)C1CC1 10.1021/acs.jmedchem.1c00031
CHEMBL4874972 185755 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 549 8 1 4 7.1 C[C@H](C(=O)O)[C@@H](c1ccc2c(c1)O[C@@H](C1CCN([C@@H](C)c3cc(F)ccc3OC(F)(F)F)CC1)CC2)C1CC1 10.1021/acs.jmedchem.1c00031
134465732 170909 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4463571 170909 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
137529972 164211 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 556 8 3 8 5.2 Cc1cc(-c2nnn(CC(C)(C)O)n2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4217914 164211 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 556 8 3 8 5.2 Cc1cc(-c2nnn(CC(C)(C)O)n2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
118129999 157225 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157225 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
118645685 179288 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4745513 179288 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
118645756 180880 3 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 180880 3 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
131986061 163564 0 None 6 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209834 163564 0 None 6 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
155528372 170751 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4461095 170751 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
67087095 182793 0 None -6 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 182793 0 None -6 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134465730 172234 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4513748 172234 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
162674998 182809 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 182809 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
118637996 141638 0 None 15 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 141638 0 None 15 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 141638 0 None 15 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
164625212 185401 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3c(Cl)cccc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
CHEMBL4869870 185401 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3c(Cl)cccc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
44409722 140485 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382381 140485 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
118645789 179477 0 None 11 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
CHEMBL4747793 179477 0 None 11 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
118623101 167028 0 None -12 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167028 0 None -12 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167028 0 None -12 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
118642344 141590 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883380 141590 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
90356885 166974 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 166974 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 166974 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
68194127 182613 0 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 182613 0 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194465 182724 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 182724 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
51350404 58552 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1021/jm101405t
CHEMBL1688484 58552 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1021/jm101405t
67072752 86102 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315528 86102 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
66562288 138480 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3785637 138480 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
131986401 163432 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4208095 163432 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986050 163934 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4214289 163934 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
45107307 111479 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1021/ml500391n
CHEMBL3288362 111479 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1021/ml500391n
45107307 111479 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3288362 111479 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
122185452 122186 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 395 7 1 4 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
CHEMBL3604067 122186 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 395 7 1 4 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
45107307 111479 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288362 111479 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
155549083 173096 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4534836 173096 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
145952952 161941 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167323 161941 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
23082877 75469 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
CHEMBL2048613 75469 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
162668378 181925 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 181925 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
131986065 163301 0 None 4 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206579 163301 0 None 4 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986050 163934 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4214289 163934 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
66562288 138480 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3785637 138480 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
164618830 185179 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
CHEMBL4866406 185179 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
155519364 169809 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 476 8 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4F)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4447826 169809 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 476 8 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4F)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
145987796 166573 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 464 6 1 4 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Br)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4290397 166573 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 464 6 1 4 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Br)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
118645367 181080 0 None -5 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4776217 181080 0 None -5 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
134153546 152049 0 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 371 6 1 4 4.4 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3971857 152049 0 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 371 6 1 4 4.4 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
137632610 155805 0 None 2 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4065890 155805 0 None 2 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
134139528 154001 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3921121 154001 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990894 154001 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137657027 159033 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 373 7 1 4 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccncc3Cl)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4102878 159033 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 373 7 1 4 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccncc3Cl)c2)s1 10.1021/acs.jmedchem.6b01357
46231486 198660 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL597638 198660 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
145949924 162318 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 507 8 1 6 4.4 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4173246 162318 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 507 8 1 6 4.4 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
51349861 58521 0 None 77 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL1688454 58521 0 None 77 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
44409883 140698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 500 7 3 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCNC2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382884 140698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 500 7 3 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCNC2)cc1 10.1016/j.bmcl.2006.01.007
44409906 76433 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2019.06.087
CHEMBL206880 76433 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2019.06.087
57521814 75916 0 None -10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 362 8 1 3 5.0 COc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058525 75916 0 None -10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 362 8 1 3 5.0 COc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
58319089 86092 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CCO)cc1 10.1021/jm301470a
CHEMBL2315250 86092 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CCO)cc1 10.1021/jm301470a
44409906 76433 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206880 76433 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
71615469 89561 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(F)cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381303 89561 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(F)cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
137630008 160484 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 561 12 1 5 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4077784 160484 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 561 12 1 5 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116425 160484 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 561 12 1 5 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
46231595 198510 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3cc(Cl)cc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL596666 198510 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3cc(Cl)cc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
127031002 138557 0 None 165 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C/C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3786526 138557 0 None 165 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C/C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
10466 166117 72 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 272 15 2 2 4.5 O=C(O)CCCCCCCCCCCCCCCO 10.1039/C7MD00130D
CHEMBL4281719 166117 72 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 272 15 2 2 4.5 O=C(O)CCCCCCCCCCCCCCCO 10.1039/C7MD00130D
46231435 198922 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 309 4 1 3 3.8 O=C1NC(=O)C(Cc2ccc(/C=C/c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599271 198922 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 309 4 1 3 3.8 O=C1NC(=O)C(Cc2ccc(/C=C/c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
45107320 122185 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 396 7 1 4 4.8 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604066 122185 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 396 7 1 4 4.8 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
23111791 73707 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022252 73707 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
67087095 182793 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 182793 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
131986250 163133 0 None 3 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204776 163133 0 None 3 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986130 163873 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213597 163873 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
162652399 179648 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4749949 179648 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
71460547 81308 22 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
CHEMBL2163923 81308 22 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
75511310 121943 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 352 8 1 5 3.9 CCc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601000 121943 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 352 8 1 5 3.9 CCc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
145973329 164183 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(OCc2ccc(-c3cc(OC)ccc3F)c(C3CCCC3(C)C)c2)ccc1F 10.1021/acsmedchemlett.8b00213
CHEMBL4217580 164183 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(OCc2ccc(-c3cc(OC)ccc3F)c(C3CCCC3(C)C)c2)ccc1F 10.1021/acsmedchemlett.8b00213
137648439 157338 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 396 8 1 4 5.8 COC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4083960 157338 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 396 8 1 4 5.8 COC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
137654021 158246 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 404 7 1 3 6.2 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4094216 158246 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 404 7 1 3 6.2 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
58172998 122152 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(F)c1 10.1016/j.bmc.2015.07.028
CHEMBL3604034 122152 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(F)c1 10.1016/j.bmc.2015.07.028
75204360 157075 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 7 1 5 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4081072 157075 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 7 1 5 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
145982132 166016 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 370 6 1 4 3.6 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4279826 166016 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 370 6 1 4 3.6 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145993162 166428 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Br)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4287731 166428 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Br)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145988796 166746 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(F)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4293798 166746 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(F)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
132606863 157281 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157281 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
90644287 111462 0 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288345 111462 0 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
71449363 80262 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 518 9 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151301 80262 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 518 9 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
25261467 80383 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(F)(F)F)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2152068 80383 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(F)(F)F)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
168273292 189939 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 409 7 1 5 5.1 O=C(O)COc1ccc(COc2cccc(-c3nc4ccccc4s3)c2)cc1F 10.1016/j.ejmech.2021.114061
CHEMBL5179638 189939 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 409 7 1 5 5.1 O=C(O)COc1ccc(COc2cccc(-c3nc4ccccc4s3)c2)cc1F 10.1016/j.ejmech.2021.114061
122185441 122169 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 315 8 1 4 3.5 CCOC(CC(=O)O)c1ccc(OCc2cccnc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604050 122169 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 315 8 1 4 3.5 CCOC(CC(=O)O)c1ccc(OCc2cccnc2C)cc1 10.1016/j.bmc.2015.07.028
137637488 155376 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 4.5 O=C(O)C1CCN(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4060859 155376 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 4.5 O=C(O)C1CCN(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
134155480 150719 0 None -38 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 384 5 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3960231 150719 0 None -38 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 384 5 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
145989566 166603 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 377 6 1 5 3.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C#N)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4290886 166603 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 377 6 1 5 3.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C#N)cc3O2)cc1 10.1016/j.bmc.2018.10.019
137651638 156679 0 None -7 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4076190 156679 0 None -7 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
90644297 111472 0 None -32 2 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288355 111472 0 None -32 2 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
25109512 189172 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 382 10 1 5 4.8 O=C(O)CCCc1ccc(OCCN(c2ccccc2)c2nccs2)cc1 10.1021/jm800970b
CHEMBL515995 189172 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 382 10 1 5 4.8 O=C(O)CCCc1ccc(OCCN(c2ccccc2)c2nccs2)cc1 10.1021/jm800970b
127025866 137188 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 7 1 6 3.7 C=CCn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
CHEMBL3758885 137188 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 7 1 6 3.7 C=CCn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
145956069 162147 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4170517 162147 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
145989900 166470 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 360 7 1 4 3.6 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
CHEMBL4288499 166470 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 360 7 1 4 3.6 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
86803188 121989 2 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 356 7 1 5 3.8 Cc1cc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)ccc1F 10.1016/j.bmcl.2015.06.018
CHEMBL3601050 121989 2 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 356 7 1 5 3.8 Cc1cc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)ccc1F 10.1016/j.bmcl.2015.06.018
131986164 164067 0 None -1 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216016 164067 0 None -1 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145966699 163722 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1cc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)ccc1Cl 10.1016/j.ejmech.2017.07.001
CHEMBL4211760 163722 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1cc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)ccc1Cl 10.1016/j.ejmech.2017.07.001
145972079 164014 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 417 7 1 6 3.9 Cc1cccc(-c2nc(C)c(COc3ccc(S(=O)(=O)CC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4215289 164014 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 417 7 1 6 3.9 Cc1cccc(-c2nc(C)c(COc3ccc(S(=O)(=O)CC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.07.001
145960453 160945 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 433 9 1 5 4.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccccc3)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4127972 160945 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 433 9 1 5 4.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccccc3)cc2)S1 10.1016/j.bmcl.2018.03.051
71655225 89932 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)cn1 10.1021/ml4000673
CHEMBL2386356 89932 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)cn1 10.1021/ml4000673
54586010 61469 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(CNc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773247 61469 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(CNc2ccccc2)cc1 10.1021/ml100106c
127045888 139138 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 393 6 1 4 4.4 Cc1noc(C)c1C#Cc1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797889 139138 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 393 6 1 4 4.4 Cc1noc(C)c1C#Cc1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
118145019 173084 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 464 8 1 3 6.7 COc1ccc(F)c(-c2cc(F)c3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4534543 173084 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 464 8 1 3 6.7 COc1ccc(F)c(-c2cc(F)c3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
145976702 163402 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4207755 163402 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
137638911 156188 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4070298 156188 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
46231716 199995 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(C(F)(F)F)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
CHEMBL606207 199995 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(C(F)(F)F)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
24825484 87563 0 None 208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm300215x
CHEMBL234269 87563 0 None 208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm300215x
58319118 86126 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315552 86126 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
71613517 89544 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381286 89544 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
154005 162730 4 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 366 6 1 5 3.6 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL418695 162730 4 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 366 6 1 5 3.6 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
90655863 110765 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265148 110765 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
57414405 75265 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047155 75265 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111781 73702 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022247 73702 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
134465730 172234 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4513748 172234 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
11674915 58554 1 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL1688486 58554 1 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
68194476 182305 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182305 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
134131511 141626 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 141626 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
71655227 89938 0 None 173 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386362 89938 0 None 173 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
155548258 173194 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 399 7 2 3 5.5 Cc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(Cl)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4537190 173194 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 399 7 2 3 5.5 Cc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(Cl)c1 10.1016/j.ejmech.2019.06.087
127047528 139239 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(COc2ccc(CCC(=O)O)c(F)c2)cc1-c1c(C)noc1C 10.1016/j.ejmech.2016.03.054
CHEMBL3798575 139239 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(COc2ccc(CCC(=O)O)c(F)c2)cc1-c1c(C)noc1C 10.1016/j.ejmech.2016.03.054
168269875 189425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 410 9 1 4 5.2 CCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5171641 189425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 410 9 1 4 5.2 CCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
155511380 168989 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4435633 168989 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
155526126 170482 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 429 7 1 5 4.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccnc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4456918 170482 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 429 7 1 5 4.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccnc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
137633101 156037 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 380 6 1 4 4.4 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cn1 10.1021/acs.jmedchem.6b01559
CHEMBL4068606 156037 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 380 6 1 4 4.4 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cn1 10.1021/acs.jmedchem.6b01559
137638269 156334 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4071899 156334 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
90151625 157185 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 523 8 1 6 5.5 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4082133 157185 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 523 8 1 6 5.5 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
155551422 173395 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4541658 173395 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
57706720 80257 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 9 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(C)C)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151297 80257 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 9 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(C)C)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
16738034 85339 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretionAgonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretion
ChEMBL 326 9 1 2 5.1 CCC(CC)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm070130j
CHEMBL229225 85339 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretionAgonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretion
ChEMBL 326 9 1 2 5.1 CCC(CC)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm070130j
1050 1871 86 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1871 86 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1871 86 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
134155847 150570 0 None -63 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 418 5 1 3 5.6 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3959144 150570 0 None -63 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 418 5 1 3 5.6 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 10.1021/acsmedchemlett.6b00394
145985116 165343 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 7 1 4 6.1 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(C(=O)c4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4249862 165343 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 7 1 4 6.1 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(C(=O)c4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
46231484 198631 3 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 283 3 1 3 3.2 O=C1NC(=O)C(Cc2ccc(-c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL597435 198631 3 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 283 3 1 3 3.2 O=C1NC(=O)C(Cc2ccc(-c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
71562527 86128 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2ccccc2OC(F)(F)F)cc1 10.1021/jm301470a
CHEMBL2315554 86128 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2ccccc2OC(F)(F)F)cc1 10.1021/jm301470a
1050 1871 86 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1871 86 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1871 86 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
53248848 61839 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 61839 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
145992642 166342 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3ccc(Br)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4286165 166342 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3ccc(Br)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
149378333 171317 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 370 7 2 5 4.2 Cc1noc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4469534 171317 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 370 7 2 5 4.2 Cc1noc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
1201222 154588 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 325 5 1 4 2.9 O=C(O)CCCN1C(=O)/C(=C\c2ccc(F)cc2)SC1=S 10.1021/jm7012425
CHEMBL402054 154588 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 325 5 1 4 2.9 O=C(O)CCCN1C(=O)/C(=C\c2ccc(F)cc2)SC1=S 10.1021/jm7012425
46231651 197738 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ncccc3C(F)(F)F)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL591214 197738 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ncccc3C(F)(F)F)cc2)S1 10.1016/j.bmcl.2009.10.052
71562313 86108 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.5 Cc1ccccc1C#Cc1ccc(/C=C/C(=O)O)cc1 10.1021/jm301470a
CHEMBL2315534 86108 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.5 Cc1ccccc1C#Cc1ccc(/C=C/C(=O)O)cc1 10.1021/jm301470a
131986057 163103 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204345 163103 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23111704 73699 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022244 73699 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
58172961 122163 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 392 10 1 4 5.6 CCOC(CC(=O)O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604044 122163 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 392 10 1 4 5.6 CCOC(CC(=O)O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmc.2015.07.028
11236925 75475 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048619 75475 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
12002202 75481 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048626 75481 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
67087160 181762 0 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 181762 0 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182404 0 None -13 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182404 0 None -13 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
145952952 161941 0 None -1 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167323 161941 0 None -1 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
46854655 391 43 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
6485 391 43 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
CHEMBL1829173 391 43 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
118637972 161767 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4164618 161767 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
90372616 141701 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
60195039 81381 0 None 181 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 8 2 2 5.7 CCc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL2164240 81381 0 None 181 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 8 2 2 5.7 CCc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
118645392 179529 0 None -2 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4748392 179529 0 None -2 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
90644302 111478 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288361 111478 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
71456495 80247 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
CHEMBL2151287 80247 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
71449362 80250 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 418 8 1 3 5.7 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cc(OC)ccc3F)cc2)cc1 10.1021/ml300133f
CHEMBL2151290 80250 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 418 8 1 3 5.7 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cc(OC)ccc3F)cc2)cc1 10.1021/ml300133f
58218655 155624 0 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4063889 155624 0 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
145955723 161986 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167970 161986 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
127025858 137211 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3ccc(Br)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759133 137211 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3ccc(Br)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
137635513 155569 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2csc(CCC(=O)O)c2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4063167 155569 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2csc(CCC(=O)O)c2)c1 10.1021/acs.jmedchem.6b01357
164609159 183891 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN3CCC4(CCc5ccccc54)CC3)c2)cc1 10.1021/acs.jmedchem.1c00031
CHEMBL4846948 183891 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN3CCC4(CCc5ccccc54)CC3)c2)cc1 10.1021/acs.jmedchem.1c00031
51049992 145086 4 None -23 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3915620 145086 4 None -23 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmcl.2016.10.074
145976748 162996 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 5.7 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(=O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4202936 162996 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 5.7 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(=O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
145976172 163324 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4206875 163324 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
46231922 199655 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 452 4 1 5 5.6 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)c3ccccc23)S1 10.1016/j.bmcl.2009.10.052
CHEMBL604317 199655 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 452 4 1 5 5.6 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)c3ccccc23)S1 10.1016/j.bmcl.2009.10.052
137628912 160433 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 594 12 1 6 7.1 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc5ccccc5n3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4101806 160433 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 594 12 1 6 7.1 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc5ccccc5n3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116012 160433 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 594 12 1 6 7.1 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc5ccccc5n3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
46231652 199427 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cc(C(F)(F)F)ccn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL603063 199427 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cc(C(F)(F)F)ccn3)cc2)S1 10.1016/j.bmcl.2009.10.052
145991968 166284 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 10 1 5 3.6 COCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
CHEMBL4285148 166284 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 10 1 5 3.6 COCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
46231547 200442 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(C)c(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL609034 200442 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(C)c(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
145986696 166661 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)C[C@@H]1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4291932 166661 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)C[C@@H]1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
131986162 164284 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218822 164284 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
24825492 149010 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/jm300215x
CHEMBL394666 149010 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/jm300215x
75511298 121990 3 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.9 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccccc2)no1 10.1016/j.bmcl.2015.06.018
CHEMBL3601051 121990 3 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.9 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccccc2)no1 10.1016/j.bmcl.2015.06.018
145975621 163202 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4205508 163202 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
145974509 164197 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4217742 164197 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
57414401 75261 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047151 75261 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
23111693 73710 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
CHEMBL2022255 73710 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
162676881 183003 0 None -10 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183003 0 None -10 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
131986115 164163 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4217348 164163 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145947998 167155 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167155 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167155 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
149144496 174619 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 9 2 4 5.6 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4570807 174619 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 9 2 4 5.6 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
127045864 139208 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(-c2c(C)noc2C)cc1COc1ccc(CCC(=O)O)c(F)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798341 139208 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(-c2c(C)noc2C)cc1COc1ccc(CCC(=O)O)c(F)c1 10.1016/j.ejmech.2016.03.054
127046960 139461 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799946 139461 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL4227915 139461 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
51350271 58532 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
CHEMBL1688464 58532 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
149231065 174862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4576378 174862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
46231594 199219 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL601504 199219 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
57390188 69682 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939652 69682 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
137648780 157058 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4080911 157058 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
5353640 160944 14 None - 1 Human 6.6 pEC50 = 6.6 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C/C/C=C/C/C=C/CCCCC(=O)O 10.1016/j.bmcl.2018.03.051
CHEMBL4127920 160944 14 None - 1 Human 6.6 pEC50 = 6.6 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C/C/C=C/C/C=C/CCCCC(=O)O 10.1016/j.bmcl.2018.03.051
132606864 157204 0 None 2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157204 0 None 2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
137635715 155535 0 None -9 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4062765 155535 0 None -9 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
132606864 157204 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157204 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
137652992 158103 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(OCc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4092577 158103 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(OCc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
90356885 166974 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 166974 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 166974 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
145976979 163446 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 413 9 2 7 3.4 COc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4208272 163446 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 413 9 2 7 3.4 COc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
145985686 164878 0 None -354 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 358 7 1 3 4.2 COc1cc(F)c(F)c(-c2cc(F)c(OCCCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2018.06.047
CHEMBL4238809 164878 0 None -354 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 358 7 1 3 4.2 COc1cc(F)c(F)c(-c2cc(F)c(OCCCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2018.06.047
54580627 61838 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777875 61838 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
155528372 170751 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4461095 170751 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
54586983 61473 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 266 4 1 2 4.1 O=C(O)CCc1ccc2oc(-c3ccccc3)cc2c1 10.1021/ml100106c
CHEMBL1773251 61473 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 266 4 1 2 4.1 O=C(O)CCc1ccc2oc(-c3ccccc3)cc2c1 10.1021/ml100106c
763016 94594 24 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 271 4 2 4 2.7 O=C(O)c1ccc(NCc2ccc3c(c2)OCO3)cc1 10.1021/jm7012425
CHEMBL255073 94594 24 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 271 4 2 4 2.7 O=C(O)c1ccc(NCc2ccc3c(c2)OCO3)cc1 10.1021/jm7012425
145947998 167155 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167155 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167155 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
54582629 61827 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 61827 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
118637996 141638 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 141638 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 141638 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
118637996 141638 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 141638 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 141638 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
21322577 61822 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 324 5 1 2 5.4 CC(CC(=O)O)c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777859 61822 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 324 5 1 2 5.4 CC(CC(=O)O)c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
53248848 61839 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 61839 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
131986300 163075 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203837 163075 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
57393692 69684 8 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939654 69684 8 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.118
11226058 75477 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048622 75477 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
11203294 75478 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048623 75478 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
145950347 162288 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172828 162288 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
11203294 75478 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
FLIPR functional assay (Ca influx activity of CHO cells)FLIPR functional assay (Ca influx activity of CHO cells)
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 75478 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
FLIPR functional assay (Ca influx activity of CHO cells)FLIPR functional assay (Ca influx activity of CHO cells)
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
90372616 141701 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
127045866 139507 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1F 10.1016/j.ejmech.2016.03.054
CHEMBL3800232 139507 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1F 10.1016/j.ejmech.2016.03.054
71460547 81308 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
CHEMBL2163923 81308 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
127045865 139201 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1F 10.1016/j.ejmech.2016.03.054
CHEMBL3798274 139201 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1F 10.1016/j.ejmech.2016.03.054
162671590 182379 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 479 12 1 4 6.5 COc1ccc(CCCC(C)(C)C)c(N2CC(COc3cccc(C(CC(=O)O)C4CC4)c3)C2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4792979 182379 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 479 12 1 4 6.5 COc1ccc(CCCC(C)(C)C)c(N2CC(COc3cccc(C(CC(=O)O)C4CC4)c3)C2)c1 10.1021/acs.jmedchem.0c00843
90151466 155735 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 529 6 1 5 6.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4065150 155735 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 529 6 1 5 6.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
90644296 111471 0 None -29 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288354 111471 0 None -29 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
90644295 111470 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288353 111470 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
73777156 152183 0 None -18 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 396 4 1 4 4.7 N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 10.1021/acsmedchemlett.6b00360
CHEMBL3973034 152183 0 None -18 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 396 4 1 4 4.7 N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 10.1021/acsmedchemlett.6b00360
134151115 151667 0 None -72 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 336 6 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
CHEMBL3968537 151667 0 None -72 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 336 6 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
24825490 87053 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.6 O=C(O)CCc1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL233402 87053 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.6 O=C(O)CCc1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2006.12.084
24825484 87563 0 None 208 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234269 87563 0 None 208 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
145966632 163609 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 437 7 1 6 4.2 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4210351 163609 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 437 7 1 6 4.2 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54757624 65006 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 256 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccs2)cc1 10.1021/jm2005699
CHEMBL1829155 65006 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 256 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccs2)cc1 10.1021/jm2005699
71655226 89933 0 None 36 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 10.1021/ml4000673
CHEMBL2386357 89933 0 None 36 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 10.1021/ml4000673
118642384 141633 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883790 141633 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
145973781 164181 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c(C)c1 10.1016/j.ejmech.2017.09.019
CHEMBL4217530 164181 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c(C)c1 10.1016/j.ejmech.2017.09.019
90151537 155906 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 479 6 1 5 5.1 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(F)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4067111 155906 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 479 6 1 5 5.1 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(F)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
137645353 160667 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cccnc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4083311 160667 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cccnc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117885 160667 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cccnc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
118642372 161914 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166943 161914 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
145965138 163909 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 400 7 1 4 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4214028 163909 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 400 7 1 4 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1016/j.ejmech.2017.07.001
75511308 121991 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 330 7 1 6 3.4 O=C(O)CCc1ccc(OCc2nc(-c3cccs3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601052 121991 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 330 7 1 6 3.4 O=C(O)CCc1ccc(OCc2nc(-c3cccs3)no2)cc1 10.1016/j.bmcl.2015.06.018
46231781 199122 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 436 4 1 5 5.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
CHEMBL600800 199122 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 436 4 1 5 5.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
121294363 182498 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 599 12 1 6 7.0 COc1ccc(C(=O)N(CC(C)(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4794401 182498 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 599 12 1 6 7.0 COc1ccc(C(=O)N(CC(C)(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
71460547 81308 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
CHEMBL2163923 81308 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
23157282 76867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048628 76867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2079469 76867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
131986182 164069 0 None 3 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216026 164069 0 None 3 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23136411 58524 0 None 11 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688457 58524 0 None 11 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm101405t
51349991 58546 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 10 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCCc3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688478 58546 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 10 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCCc3ccccc3)c2)cc1 10.1021/jm101405t
44572095 14743 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 5 4.0 Cc1cccc(C)c1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2008.10.085
CHEMBL1208013 14743 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 5 4.0 Cc1cccc(C)c1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2008.10.085
CHEMBL475053 14743 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 5 4.0 Cc1cccc(C)c1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2008.10.085
168284831 190698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 8 1 4 4.9 COc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5190883 190698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 8 1 4 4.9 COc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
42603138 69673 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939643 69673 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
137630491 160533 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1cccc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4098843 160533 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1cccc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4116766 160533 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1cccc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
137635715 155535 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4062765 155535 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
137638184 156215 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070619 156215 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
145981983 166116 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4281717 166116 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
118737974 118631 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427715 118631 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
137642248 157608 0 None 1 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
CHEMBL4087308 157608 0 None 1 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
137641818 157662 0 None -10 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 373 6 1 5 4.1 COc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4087992 157662 0 None -10 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 373 6 1 5 4.1 COc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
137643731 157841 0 None -5 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 361 5 1 4 4.2 O=C(O)CCc1ccc(-c2cc(F)c3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
CHEMBL4089919 157841 0 None -5 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 361 5 1 4 4.2 O=C(O)CCc1ccc(-c2cc(F)c3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
90151624 155604 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccn4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4063627 155604 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccn4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
46231714 199336 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
CHEMBL602289 199336 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
71562772 86105 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315531 86105 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
51350272 58533 0 None 107 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58533 0 None 107 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
75511299 121992 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2noc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601053 121992 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2noc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
53248848 61839 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 61839 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
75511306 121993 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 354 8 1 6 3.3 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601054 121993 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 354 8 1 6 3.3 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)c1 10.1016/j.bmcl.2015.06.018
145977404 163295 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 401 7 1 6 3.4 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4206505 163295 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 401 7 1 6 3.4 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
51350272 58533 0 None 107 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688465 58533 0 None 107 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
24857286 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
6484 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
CHEMBL1829174 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
DB12491 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
58172979 122151 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 367 8 2 3 5.2 CCOC(CC(=O)O)c1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604033 122151 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 367 8 2 3 5.2 CCOC(CC(=O)O)c1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
23111704 73699 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022244 73699 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
23111781 73702 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022247 73702 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
145968204 164635 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 379 6 1 5 4.5 Cc1noc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4228620 164635 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 379 6 1 5 4.5 Cc1noc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
24857286 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
6484 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
CHEMBL1829174 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
DB12491 1594 66 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
168271964 189516 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 432 8 1 4 5.7 COc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
CHEMBL5173019 189516 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 432 8 1 4 5.7 COc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
57414403 75263 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047153 75263 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
146314264 181735 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 423 9 1 4 5.3 COc1ccc(C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4784293 181735 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 423 9 1 4 5.3 COc1ccc(C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
58218726 158592 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097951 158592 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
23159839 58547 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 333 7 1 3 4.3 O=C(O)CCc1ccc(OCc2cccc(-c3ccccn3)c2)cc1 10.1021/jm101405t
CHEMBL1688479 58547 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 333 7 1 3 4.3 O=C(O)CCc1ccc(OCc2cccc(-c3ccccn3)c2)cc1 10.1021/jm101405t
23159846 58549 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 339 7 1 4 4.4 O=C(O)CCc1ccc(OCc2cccc(-c3nccs3)c2)cc1 10.1021/jm101405t
CHEMBL1688481 58549 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 339 7 1 4 4.4 O=C(O)CCc1ccc(OCc2cccc(-c3nccs3)c2)cc1 10.1021/jm101405t
57391959 69679 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 362 6 1 2 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939649 69679 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 362 6 1 2 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2011.10.118
137635143 155713 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 7 1 3 6.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4064922 155713 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 7 1 3 6.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)s1 10.1021/acs.jmedchem.6b01357
145977043 163081 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 491 9 2 5 5.8 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4203929 163081 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 491 9 2 5 5.8 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
145979329 166173 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 7 1 6 2.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(S(C)(=O)=O)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4283015 166173 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 7 1 6 2.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(S(C)(=O)=O)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145976136 163243 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4205991 163243 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54757622 65004 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)nc(Cl)n1 10.1021/jm2005699
CHEMBL1829153 65004 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)nc(Cl)n1 10.1021/jm2005699
145990303 166472 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3cccc(-c4ccccc4)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4288513 166472 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3cccc(-c4ccccc4)c3)ccc21 10.1016/j.ejmech.2018.09.071
131986113 164273 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218709 164273 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23111668 73698 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022243 73698 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
23111682 73754 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022576 73754 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23111734 73755 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022577 73755 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
145953365 161911 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166892 161911 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
155549083 173096 0 None -6 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4534836 173096 0 None -6 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
118645789 179477 0 None -11 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
CHEMBL4747793 179477 0 None -11 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
1050 1871 86 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm300215x
11595431 1871 86 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm300215x
CHEMBL207881 1871 86 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm300215x
131842087 164295 23 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 416 7 1 4 4.4 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4218946 164295 23 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 416 7 1 4 4.4 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2017.07.001
1050 1871 86 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
11595431 1871 86 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
CHEMBL207881 1871 86 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
145947987 167173 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4228673 167173 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4302779 167173 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.04.019
134136960 153930 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 543 11 1 5 6.3 COc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3893207 153930 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 543 11 1 5 6.3 COc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990279 153930 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 543 11 1 5 6.3 COc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
90151023 157671 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 538 8 1 7 5.1 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(F)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4088102 157671 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 538 8 1 7 5.1 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(F)cn1 10.1021/acs.jmedchem.7b00982
145993644 166775 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 8 1 5 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(C)C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294274 166775 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 8 1 5 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(C)C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
132578495 182304 2 None -13 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182304 2 None -13 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
71612897 89552 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381294 89552 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
54580626 61837 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777874 61837 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
75202601 157839 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 482 7 1 5 4.7 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4089881 157839 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 482 7 1 5 4.7 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
145988554 166706 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 412 5 1 3 5.3 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4292911 166706 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 412 5 1 3 5.3 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.ejmech.2018.08.075
145987167 166659 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 4 1 2 5.3 Cc1cc(C)c(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4291858 166659 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 4 1 2 5.3 Cc1cc(C)c(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2018.08.075
145975628 163223 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 382 7 1 4 3.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4205774 163223 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 382 7 1 4 3.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
11316164 76436 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 422 7 2 5 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(OCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206881 76436 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 422 7 2 5 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(OCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
1049 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
4618 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
5280934 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
CHEMBL8739 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
DB00132 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
145974295 162475 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 518 9 1 6 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(OC)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4175826 162475 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 518 9 1 6 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(OC)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
57414678 75274 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
CHEMBL2047165 75274 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
131986132 163307 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206640 163307 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
45107318 118625 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1021/ml500391n
CHEMBL3427709 118625 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1021/ml500391n
45107318 118625 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427709 118625 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1016/j.bmc.2015.07.028
121294254 179550 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 585 13 1 6 6.7 COc1ccc(C(=O)N(CC(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4748739 179550 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 585 13 1 6 6.7 COc1ccc(C(=O)N(CC(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
12002201 75482 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048627 75482 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
23111689 73712 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022257 73712 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
90372365 141610 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883504 141610 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
155552554 173488 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 512 8 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4544058 173488 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 512 8 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
57414268 75260 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047150 75260 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57414538 75266 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047156 75266 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
137646830 157463 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4085420 157463 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.6b01559
58172957 111169 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3286417 111169 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
145986046 165359 0 None -19 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 437 10 1 6 4.3 CO[C@H]1C[C@H](Oc2ccc([N+](=O)[O-])c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4250196 165359 0 None -19 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 437 10 1 6 4.3 CO[C@H]1C[C@H](Oc2ccc([N+](=O)[O-])c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
44634024 65010 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2)cc1 10.1021/jm2005699
CHEMBL1829159 65010 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2)cc1 10.1021/jm2005699
134139171 145730 0 None -104 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 6 1 3 5.4 Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3920591 145730 0 None -104 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 6 1 3 5.4 Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 10.1016/j.bmcl.2016.10.054
134130787 141734 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884916 141734 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
71257551 150060 18 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3955132 150060 18 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
91801188 169008 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4435837 169008 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
155565379 174993 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4579146 174993 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
134465794 170511 0 None -4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 170511 0 None -4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
118637996 141638 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 141638 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 141638 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
118637996 141638 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 141638 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 141638 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
59590781 110764 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265147 110764 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
90644286 111461 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288344 111461 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
57706778 80385 25 None -8 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL2152070 80385 25 None -8 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
67087173 181878 0 None -8 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 181878 0 None -8 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
24897670 111312 19 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
CHEMBL3287574 111312 19 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
45107312 118628 3 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427712 118628 3 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
45107312 118628 3 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427712 118628 3 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
90644290 111465 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288348 111465 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
15602772 111311 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
CHEMBL3287573 111311 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
45107282 118619 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
CHEMBL3427703 118619 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
45107282 118619 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427703 118619 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
118144982 169784 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4447353 169784 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
51350139 58542 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
CHEMBL1688474 58542 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
51350140 58543 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
CHEMBL1688475 58543 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
51350405 58553 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 8 1 2 6.1 CC(C)c1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688485 58553 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 8 1 2 6.1 CC(C)c1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
23111734 73755 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2022577 73755 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
131986035 163505 0 None -5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209136 163505 0 None -5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
122185435 122159 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 3 4.0 CCOC(CC(=O)O)c1ccc(OCc2cccc(F)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604040 122159 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 3 4.0 CCOC(CC(=O)O)c1ccc(OCc2cccc(F)c2)cc1 10.1016/j.bmc.2015.07.028
51350138 58541 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL1688473 58541 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
131986057 163103 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204345 163103 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118638001 141588 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883355 141588 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
71613312 89564 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381306 89564 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
71613521 89548 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381290 89548 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
51349860 58520 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm101405t
CHEMBL1688453 58520 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm101405t
51349990 58545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 9 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCc3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688477 58545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 9 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCc3ccccc3)c2)cc1 10.1021/jm101405t
86803193 121944 6 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.6 Cc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601001 121944 6 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.6 Cc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
155569570 175627 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)c(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4593742 175627 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)c(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
75511316 121994 3 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 388 8 1 6 4.0 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601055 121994 3 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 388 8 1 6 4.0 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
1049 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
4618 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
5280934 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
CHEMBL8739 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
DB00132 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
85472225 162211 0 None -64 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 by calcium flux assayAgonist activity at human GPR40 by calcium flux assay
ChEMBL 495 7 1 4 6.5 O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 10.1021/acsmedchemlett.7b00233
CHEMBL4171724 162211 0 None -64 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 by calcium flux assayAgonist activity at human GPR40 by calcium flux assay
ChEMBL 495 7 1 4 6.5 O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 10.1021/acsmedchemlett.7b00233
67085353 158688 0 None -9 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4098892 158688 0 None -9 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
145947309 167116 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 491 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4241974 167116 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 491 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4302072 167116 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 491 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
145965968 163694 0 None 4 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4211335 163694 0 None 4 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
86803219 121998 3 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 426 7 1 5 5.0 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601059 121998 3 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 426 7 1 5 5.0 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
24860552 142756 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 312 8 1 2 4.7 CC[C@H](C)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm2005699
CHEMBL389699 142756 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 312 8 1 2 4.7 CC[C@H](C)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm2005699
11750823 76480 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206942 76480 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
145980573 166038 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 384 8 1 4 4.8 CC(C)(C)c1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
CHEMBL4280212 166038 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 384 8 1 4 4.8 CC(C)(C)c1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
118642391 162412 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)n1 10.1021/acsmedchemlett.8b00149
CHEMBL4174833 162412 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)n1 10.1021/acsmedchemlett.8b00149
53248847 61818 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 61818 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
90151464 155395 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 519 7 1 6 5.6 COc1cc(C)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(C)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4061053 155395 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 519 7 1 6 5.6 COc1cc(C)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(C)c1 10.1021/acs.jmedchem.7b00982
145986662 166620 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1cncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4291179 166620 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1cncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
12830931 200757 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL611065 200757 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
145984906 165839 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)CC1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4276781 165839 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)CC1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
145955179 161860 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 490 8 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)o2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166005 161860 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 490 8 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)o2)cc1 10.1016/j.ejmech.2018.04.023
71562422 86114 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)cc1 10.1021/jm301470a
CHEMBL2315540 86114 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)cc1 10.1021/jm301470a
145974478 164135 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 451 8 2 6 4.4 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(C(F)(F)F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4217082 164135 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 451 8 2 6 4.4 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(C(F)(F)F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
58172986 118621 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1021/ml500391n
CHEMBL3427705 118621 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1021/ml500391n
58172986 118621 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427705 118621 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
54586486 61833 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777870 61833 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
57413375 76866 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2048620 76866 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2079468 76866 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
145950347 162288 0 None -1 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172828 162288 0 None -1 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
118645541 180061 0 None -4 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4754974 180061 0 None -4 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
51349861 58521 0 None 77 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm101405t
CHEMBL1688454 58521 0 None 77 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm101405t
57706502 163763 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4212284 163763 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
67085353 158688 0 None 9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4098892 158688 0 None 9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
87265393 158734 0 None 4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4099410 158734 0 None 4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
90644291 111466 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288349 111466 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
58172988 122154 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 413 9 1 5 5.0 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c([N+](=O)[O-])c1 10.1016/j.bmc.2015.07.028
CHEMBL3604036 122154 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 413 9 1 5 5.0 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c([N+](=O)[O-])c1 10.1016/j.bmc.2015.07.028
90372458 141692 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884347 141692 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
54757739 65018 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 325 5 1 2 3.9 C=CCc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
CHEMBL1829167 65018 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 325 5 1 2 3.9 C=CCc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
24825481 75572 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL205090 75572 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
1049 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
4618 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
5280934 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
CHEMBL8739 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
DB00132 360 70 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
12830934 200711 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3cccc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL610787 200711 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3cccc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
134133675 142730 0 None -22 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 318 8 1 3 4.1 CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3896714 142730 0 None -22 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 318 8 1 3 4.1 CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
51350137 58540 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688472 58540 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cc2)c1 10.1021/jm101405t
25150014 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
3952 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
CHEMBL449588 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
90644288 111463 0 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL3288346 111463 0 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
11489259 75476 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048621 75476 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
162674654 182873 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 182873 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
131986082 163602 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210243 163602 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986378 164029 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4215544 164029 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118645685 179288 0 None -15 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4745513 179288 0 None -15 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
25150014 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
3952 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
CHEMBL449588 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
127046960 139461 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL3799946 139461 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4227915 139461 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
51351414 58536 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 358 7 1 1 5.8 Cc1cccc(C)c1-c1cccc(CCc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688468 58536 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 358 7 1 1 5.8 Cc1cccc(C)c1-c1cccc(CCc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
90161101 158240 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4094183 158240 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
90644300 111475 0 None -31 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288358 111475 0 None -31 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
1622278 94562 10 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 94562 10 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
22036572 164748 66 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 242 5 1 2 3.5 O=C(O)CCc1ccc(Oc2ccccc2)cc1 10.1021/jm101405t
CHEMBL423319 164748 66 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 242 5 1 2 3.5 O=C(O)CCc1ccc(Oc2ccccc2)cc1 10.1021/jm101405t
57397248 69668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 314 8 1 3 4.2 CCC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939638 69668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 314 8 1 3 4.2 CCC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
122185442 122170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 5 2.9 CCOC(CC(=O)O)c1ccc(OCc2cc(C)nn2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604051 122170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 5 2.9 CCOC(CC(=O)O)c1ccc(OCc2cc(C)nn2C)cc1 10.1016/j.bmc.2015.07.028
58218581 158578 0 None -8 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097826 158578 0 None -8 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
137640417 156559 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCn2cc(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4074547 156559 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCn2cc(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
44409697 76368 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 365 8 2 4 5.3 O=C(O)CSc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206572 76368 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 365 8 2 4 5.3 O=C(O)CSc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
168283014 190282 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 393 7 1 5 4.7 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ncoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5184830 190282 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 393 7 1 5 4.7 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ncoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
155527626 170665 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459709 170665 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
145966219 163745 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1cccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
CHEMBL4212106 163745 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1cccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
118638009 167092 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4160527 167092 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301726 167092 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
145948007 167177 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 334 9 1 3 4.2 O=C(O)CCc1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4284549 167177 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 334 9 1 3 4.2 O=C(O)CCc1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4302817 167177 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 334 9 1 3 4.2 O=C(O)CCc1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
23111668 73698 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022243 73698 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
23111766 73713 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022258 73713 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
131986113 164273 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218709 164273 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
66562385 89937 0 None 47 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386361 89937 0 None 47 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
127046962 139406 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(F)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799639 139406 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(F)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
24857286 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
6484 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
CHEMBL1829174 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
DB12491 1594 66 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
118737973 118630 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427714 118630 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
58218651 157774 0 None -4 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4089171 157774 0 None -4 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145965467 163614 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4210415 163614 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54583097 61471 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 270 6 1 2 3.8 CC(Oc1ccc(CCC(=O)O)cc1)c1ccccc1 10.1021/ml100106c
CHEMBL1773249 61471 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 270 6 1 2 3.8 CC(Oc1ccc(CCC(=O)O)cc1)c1ccccc1 10.1021/ml100106c
118145140 174813 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4575265 174813 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
46231545 199385 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1C 10.1016/j.bmcl.2009.10.052
CHEMBL602731 199385 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1C 10.1016/j.bmcl.2009.10.052
85470884 163452 0 None -36 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40Agonist activity at human GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
CHEMBL4208325 163452 0 None -36 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40Agonist activity at human GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
137630696 160553 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 612 12 1 6 6.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(C(F)(F)F)cn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4064196 160553 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 612 12 1 6 6.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(C(F)(F)F)cn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116961 160553 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 612 12 1 6 6.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(C(F)(F)F)cn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
134156096 150915 0 None -100 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 400 8 1 3 6.2 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3961950 150915 0 None -100 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 400 8 1 3 6.2 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
71562526 86123 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2ccccc2C(F)(F)F)cc1 10.1021/jm301470a
CHEMBL2315549 86123 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2ccccc2C(F)(F)F)cc1 10.1021/jm301470a
23136363 58525 0 None 14 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688458 58525 0 None 14 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm101405t
146314300 180858 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 493 11 1 4 6.9 COc1ccc(CCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4764150 180858 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 493 11 1 4 6.9 COc1ccc(CCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
155526793 170628 0 None -2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4459220 170628 0 None -2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
71613516 89543 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381285 89543 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
46941175 61483 20 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61483 20 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
51350138 58541 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL1688473 58541 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
127031412 138198 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 407 7 1 5 4.6 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
CHEMBL3780042 138198 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 407 7 1 5 4.6 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
168283114 190466 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 436 10 1 4 5.6 Cc1ccc(OCC2CC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5187322 190466 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 436 10 1 4 5.6 Cc1ccc(OCC2CC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
58218630 159108 0 None 13 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103729 159108 0 None 13 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
145978975 166010 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4279744 166010 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
58218571 156938 0 None -17 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079421 156938 0 None -17 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
25261464 80386 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152071 80386 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
145992078 166453 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 406 8 1 4 4.2 O=C(O)CC1COc2cc(OCCCOc3cccc(Br)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4288124 166453 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 406 8 1 4 4.2 O=C(O)CC1COc2cc(OCCCOc3cccc(Br)c3)ccc21 10.1016/j.ejmech.2018.09.071
71562315 86110 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 O=C(O)CC1CCc2cc(C#Cc3ccccc3)ccc21 10.1021/jm301470a
CHEMBL2315536 86110 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 O=C(O)CC1CCc2cc(C#Cc3ccccc3)ccc21 10.1021/jm301470a
145983824 165186 0 None 6 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 484 13 1 4 6.3 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4246334 165186 0 None 6 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 484 13 1 4 6.3 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
118642379 141587 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 141587 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
53248847 61818 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 61818 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
23082739 58544 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 396 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2cc(F)c(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
CHEMBL1688476 58544 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 396 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2cc(F)c(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
90644303 111480 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3288363 111480 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmc.2015.07.028
122185440 122168 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 306 8 1 3 4.2 CCOC(CC(=O)O)c1ccc(OCC2CCCCC2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604049 122168 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 306 8 1 3 4.2 CCOC(CC(=O)O)c1ccc(OCC2CCCCC2)cc1 10.1016/j.bmc.2015.07.028
90644303 111480 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288363 111480 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
137333449 167048 3 None -10 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165147 167048 3 None -10 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301092 167048 3 None -10 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
90372616 141701 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
71562773 86106 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 301 3 1 2 3.3 N#CCc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
CHEMBL2315532 86106 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 301 3 1 2 3.3 N#CCc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
66562286 89935 0 None 223 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
CHEMBL2386359 89935 0 None 223 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
71615667 89570 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 420 4 1 4 5.3 Cc1cc(F)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381312 89570 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 420 4 1 4 5.3 Cc1cc(F)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
19705952 58557 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 270 7 1 2 3.3 O=C(O)CCc1ccc(OCCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688489 58557 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 270 7 1 2 3.3 O=C(O)CCc1ccc(OCCc2ccccc2)cc1 10.1021/jm101405t
23082789 58558 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 284 8 1 2 3.7 O=C(O)CCc1ccc(OCCCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688490 58558 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 284 8 1 2 3.7 O=C(O)CCc1ccc(OCCCc2ccccc2)cc1 10.1021/jm101405t
145982616 165193 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 470 12 1 4 5.9 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4246529 165193 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 470 12 1 4 5.9 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
58218699 158869 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4100898 158869 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
85470884 163452 0 None -38 5 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
CHEMBL4208325 163452 0 None -38 5 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
25150011 186107 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 4 1 2 2.9 O=Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL488395 186107 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 4 1 2 2.9 O=Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
44409729 139680 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.0 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CC(C)C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380504 139680 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.0 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CC(C)C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
57521915 75919 0 None -15 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 378 8 1 3 5.7 CSc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058528 75919 0 None -15 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 378 8 1 3 5.7 CSc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
155544661 174373 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
CHEMBL4565467 174373 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
127027659 137145 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3cccc(Br)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758549 137145 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3cccc(Br)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
134157586 153629 0 None -123 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 366 8 1 3 5.5 O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3985509 153629 0 None -123 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 366 8 1 3 5.5 O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
145989198 166693 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
CHEMBL4292598 166693 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
122185453 122187 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 397 7 1 5 4.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
CHEMBL3604068 122187 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 397 7 1 5 4.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
118638009 167092 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4160527 167092 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301726 167092 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
118623088 141595 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 141595 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
155549085 173097 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 425 10 3 5 4.2 Cc1cc(OCCO)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4534840 173097 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 425 10 3 5 4.2 Cc1cc(OCCO)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
145964042 163531 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 4.8 Cc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4209491 163531 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 4.8 Cc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
44409933 75631 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 418 6 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205434 75631 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 418 6 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
71612685 89549 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 352 4 1 4 4.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(C2CC2)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381291 89549 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 352 4 1 4 4.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(C2CC2)c1)O3 10.1016/j.bmcl.2013.03.060
155535186 171442 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 369 7 2 3 4.7 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3F)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4471403 171442 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 369 7 2 3 4.7 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3F)c2)cc1F 10.1016/j.ejmech.2019.06.087
168276253 189859 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
CHEMBL5178528 189859 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
67058186 118620 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
CHEMBL3427704 118620 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
57394144 69508 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 356 6 1 2 5.7 CC#CC(CC(=O)O)c1ccc(Oc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1938409 69508 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 356 6 1 2 5.7 CC#CC(CC(=O)O)c1ccc(Oc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
67058186 118620 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427704 118620 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
58218581 158578 0 None 8 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097826 158578 0 None 8 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
90151400 155594 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4063492 155594 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
90151222 156363 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 6 1 5 5.9 Cc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4072229 156363 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 6 1 5 5.9 Cc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
132578495 182304 2 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182304 2 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
23136477 58522 3 None -15 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688455 58522 3 None -15 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm101405t
CHEMBL4213909 58522 3 None -15 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm101405t
853224 94139 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94139 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
134154473 151842 0 None -218 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 370 6 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3970238 151842 0 None -218 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 370 6 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
1051 1427 56 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
4289 1427 56 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
445580 1427 56 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
57417355 1427 56 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
CHEMBL367149 1427 56 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
DB03756 1427 56 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
90151309 155403 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)cc1F 10.1021/acs.jmedchem.7b00982
CHEMBL4061146 155403 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)cc1F 10.1021/acs.jmedchem.7b00982
145979602 165959 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 466 11 1 6 3.4 CS(=O)(=O)CCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
CHEMBL4278799 165959 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 466 11 1 6 3.4 CS(=O)(=O)CCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
145977668 163327 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1C 10.1016/j.ejmech.2017.07.001
CHEMBL4206915 163327 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1C 10.1016/j.ejmech.2017.07.001
73345870 89945 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386369 89945 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
54586982 61470 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 254 6 1 1 3.5 O=C(O)CCc1ccc(CCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773248 61470 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 254 6 1 1 3.5 O=C(O)CCc1ccc(CCc2ccccc2)cc1 10.1021/ml100106c
145974382 163988 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 367 7 2 5 3.4 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccccc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4215054 163988 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 367 7 2 5 3.4 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccccc3)s2)cc1 10.1016/j.ejmech.2017.09.019
127051975 139763 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(Cl)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805971 139763 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(Cl)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
131986075 163357 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207273 163357 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118645367 181080 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4776217 181080 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
24857286 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
6484 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
CHEMBL1829174 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
DB12491 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
66562289 138490 0 None 707 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(\C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3785764 138490 0 None 707 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(\C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
127046960 139461 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL3799946 139461 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4227915 139461 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
142738567 161992 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4168059 161992 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3)cc2c1 10.1021/acsmedchemlett.7b00460
58380220 110768 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265151 110768 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
57706588 80258 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151298 80258 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
58172957 111169 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3286417 111169 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmc.2015.07.028
58172957 111169 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3286417 111169 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
90151283 158936 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 6 1 6 4.8 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)n1 10.1021/acs.jmedchem.7b00982
CHEMBL4101678 158936 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 6 1 6 4.8 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)n1 10.1021/acs.jmedchem.7b00982
54585512 61834 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777871 61834 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
73348895 89948 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386371 89948 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
25150018 184850 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1016/j.ejmech.2019.06.087
CHEMBL486145 184850 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1016/j.ejmech.2019.06.087
25150018 184850 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1021/jm8010178
CHEMBL486145 184850 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1021/jm8010178
145990731 166467 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 328 4 1 2 4.4 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4288438 166467 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 328 4 1 2 4.4 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
137637576 155522 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4062640 155522 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
23083193 58529 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccccc1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688461 58529 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccccc1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
118645756 180880 3 None 1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40 assessed as increase in intracellular calcium levelAgonist activity at mouse GPR40 assessed as increase in intracellular calcium level
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 180880 3 None 1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40 assessed as increase in intracellular calcium levelAgonist activity at mouse GPR40 assessed as increase in intracellular calcium level
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
90644286 111461 0 None -10 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288344 111461 0 None -10 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
71562639 86094 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315252 86094 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
66562392 89941 0 None 83 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 3 1 1 4.6 O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F 10.1021/ml4000673
CHEMBL2386365 89941 0 None 83 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 3 1 1 4.6 O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F 10.1021/ml4000673
145947987 167173 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmc.2017.12.030
CHEMBL4228673 167173 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmc.2017.12.030
CHEMBL4302779 167173 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmc.2017.12.030
23111781 73702 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
CHEMBL2022247 73702 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
24857286 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
6484 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
CHEMBL1829174 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
DB12491 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
147747458 170014 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 437 10 2 4 6.0 CCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4450552 170014 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 437 10 2 4 6.0 CCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
71615668 89571 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381313 89571 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
127045657 139357 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(Cl)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799341 139357 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(Cl)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
57787398 143219 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 448 9 2 7 3.1 Cc1cc(OCCO)ccc1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3900797 143219 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 448 9 2 7 3.1 Cc1cc(OCCO)ccc1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2016.10.074
67972848 166089 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 356 4 1 2 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4281238 166089 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 356 4 1 2 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
122185432 122148 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 350 8 1 3 4.4 CCOC(c1ccc(OCc2ccccc2C)cc1)C(F)(F)C(=O)O 10.1016/j.bmc.2015.07.028
CHEMBL3604030 122148 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 350 8 1 3 4.4 CCOC(c1ccc(OCc2ccccc2C)cc1)C(F)(F)C(=O)O 10.1016/j.bmc.2015.07.028
137660172 158567 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 C[C@@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O 10.1021/acs.jmedchem.7b00210
CHEMBL4097652 158567 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 C[C@@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O 10.1021/acs.jmedchem.7b00210
71460255 80384 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
CHEMBL2152069 80384 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
118638010 167004 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167004 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167004 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
90372613 167183 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167183 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167183 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
23136401 158589 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4097919 158589 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
145981599 165902 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 370 7 1 4 4.4 CC(C)(C)c1cccc(OCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
CHEMBL4277858 165902 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 370 7 1 4 4.4 CC(C)(C)c1cccc(OCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
137629794 160635 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4093571 160635 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117644 160635 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
145993490 166796 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 429 7 1 7 3.3 Cn1nncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294530 166796 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 429 7 1 7 3.3 Cn1nncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
118144973 174712 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4572891 174712 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
127031569 138654 0 None 26 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 264 4 1 1 3.3 O=C(O)CCc1ccc(C#CCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3787580 138654 0 None 26 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 264 4 1 1 3.3 O=C(O)CCc1ccc(C#CCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
118719474 115037 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OC(C)C(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353262 115037 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OC(C)C(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
54757623 65005 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 257 3 1 3 2.6 O=C(O)CCc1ccc(C#Cc2cncs2)cc1 10.1021/jm2005699
CHEMBL1829154 65005 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 257 3 1 3 2.6 O=C(O)CCc1ccc(C#Cc2cncs2)cc1 10.1021/jm2005699
57414404 75264 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047154 75264 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
131986130 163873 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213597 163873 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145953365 161911 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166892 161911 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
23111666 73708 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
CHEMBL2022253 73708 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
58230552 181637 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
131986136 163073 0 None -3 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203795 163073 0 None -3 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
24857286 1594 66 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
6484 1594 66 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
CHEMBL1829174 1594 66 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
DB12491 1594 66 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
24857286 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
6484 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
CHEMBL1829174 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
DB12491 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
71613313 89565 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381307 89565 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
145988414 164662 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4229006 164662 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
24825485 87600 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 343 6 2 2 5.2 O=C(O)C1CC1c1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234450 87600 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 343 6 2 2 5.2 O=C(O)C1CC1c1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
71562769 86098 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315256 86098 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
44409665 75240 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 388 9 2 3 5.5 CC(C)NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL204671 75240 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 388 9 2 3 5.5 CC(C)NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
168271642 189719 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 486 11 1 4 6.5 Cc1ccc(OCCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5176157 189719 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 486 11 1 4 6.5 Cc1ccc(OCCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
168288738 190813 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 446 9 1 4 6.1 CCOc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
CHEMBL5192621 190813 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 446 9 1 4 6.1 CCOc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
137653172 157987 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 480 6 1 6 4.5 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccc(F)n4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4091456 157987 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 480 6 1 6 4.5 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccc(F)n4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
145955263 161991 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4168048 161991 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
57706778 80385 25 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL2152070 80385 25 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
57706778 80385 25 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
CHEMBL2152070 80385 25 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
137640728 156490 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 8 1 3 6.6 Cc1cccc(C)c1-c1cccc(COc2ccc(C(CC(=O)O)C3CC3)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4073587 156490 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 8 1 3 6.6 Cc1cccc(C)c1-c1cccc(COc2ccc(C(CC(=O)O)C3CC3)s2)c1 10.1021/acs.jmedchem.6b01357
54581633 61832 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777869 61832 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
155530636 170969 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 438 11 2 6 4.3 CO/N=C(\COc1ccc(CNc2ccc(OCC(=O)O)c(F)c2)cc1)c1ccccc1 10.1016/j.ejmech.2019.06.087
CHEMBL4464317 170969 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 438 11 2 6 4.3 CO/N=C(\COc1ccc(CNc2ccc(OCC(=O)O)c(F)c2)cc1)c1ccccc1 10.1016/j.ejmech.2019.06.087
24825480 87561 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1cccc(NCc2cccc(Oc3ccccc3)c2)c1 10.1016/j.bmcl.2006.12.084
CHEMBL234267 87561 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1cccc(NCc2cccc(Oc3ccccc3)c2)c1 10.1016/j.bmcl.2006.12.084
145979123 165913 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 5 1 2 5.5 CC(C)c1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4278085 165913 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 5 1 2 5.5 CC(C)c1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
24825483 76527 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 7 2 3 4.7 O=C(O)Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL206972 76527 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 7 2 3 4.7 O=C(O)Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
24825495 87605 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccccc2Cl)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234469 87605 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccccc2Cl)cc1 10.1016/j.bmcl.2006.12.084
24825496 87606 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 269 6 2 2 3.6 Cc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234470 87606 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 269 6 2 2 3.6 Cc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
137637576 155522 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4062640 155522 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
23136401 158589 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4097919 158589 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
168285919 191078 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 534 9 2 5 6.7 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@@H]2Oc1ccc2c(c1)OC[C@@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
CHEMBL5196447 191078 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 534 9 2 5 6.7 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@@H]2Oc1ccc2c(c1)OC[C@@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
134538585 163083 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4203974 163083 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
145976639 163263 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 523 6 2 5 6.2 Cc1cc(-c2cccc(=O)n2C)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4206195 163263 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 523 6 2 5 6.2 Cc1cc(-c2cccc(=O)n2C)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
131986295 162990 0 None 2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202907 162990 0 None 2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986030 164262 0 None 1 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218596 164262 0 None 1 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
134465785 175537 0 None 15 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 175537 0 None 15 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
162673875 182404 0 None -13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182404 0 None -13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182232 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182232 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
90372625 167160 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167160 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167160 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
44409703 140670 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 431 6 2 4 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(N)=O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382831 140670 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 431 6 2 4 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(N)=O)cc1 10.1016/j.bmcl.2006.01.007
57413373 75474 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048618 75474 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
118645526 182398 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4793322 182398 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
118144973 174712 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4572891 174712 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
67087100 182016 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182016 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
164616320 184462 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
CHEMBL4855306 184462 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
147146439 170719 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 365 7 2 3 4.9 Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4460582 170719 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 365 7 2 3 4.9 Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
44409722 140485 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382381 140485 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
162674654 182873 0 None -9 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 182873 0 None -9 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
134465730 172234 0 None 1 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4513748 172234 0 None 1 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
51349992 58526 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
CHEMBL1688459 58526 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
146840871 168958 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4434996 168958 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
23083189 75466 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
CHEMBL2048610 75466 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
71562638 86093 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315251 86093 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
54669771 65021 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 319 3 1 2 3.8 O=C(O)CCc1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
CHEMBL1829170 65021 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 319 3 1 2 3.8 O=C(O)CCc1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
168285917 191077 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5196445 191077 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
155548030 173107 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4535007 173107 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
75511297 121995 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 7 1 6 4.0 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2cccs2)no1 10.1016/j.bmcl.2015.06.018
CHEMBL3601056 121995 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 7 1 6 4.0 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2cccs2)no1 10.1016/j.bmcl.2015.06.018
71461901 80249 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
CHEMBL2151289 80249 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
145946416 166980 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 9 1 4 6.5 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(CCc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4248812 166980 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 9 1 4 6.5 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(CCc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4300233 166980 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 9 1 4 6.5 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(CCc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
118642379 141587 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 141587 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
137636033 155635 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4063956 155635 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
46232309 199402 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 351 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)O1 10.1016/j.bmcl.2009.10.052
CHEMBL602868 199402 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 351 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)O1 10.1016/j.bmcl.2009.10.052
141747238 165891 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4277653 165891 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.ejmech.2018.08.075
118637972 161767 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4164618 161767 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
118638001 141588 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883355 141588 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
57521918 75923 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 380 7 1 2 5.9 Cc1ccc(-c2ccc(Cl)cc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058531 75923 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 380 7 1 2 5.9 Cc1ccc(-c2ccc(Cl)cc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
54757513 64995 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccncc2)cc1 10.1021/jm2005699
CHEMBL1829145 64995 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccncc2)cc1 10.1021/jm2005699
54582630 61829 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 61829 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
46854655 391 43 None -8 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
6485 391 43 None -8 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
CHEMBL1829173 391 43 None -8 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
146695343 171287 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 10 2 4 5.7 CCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4468987 171287 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 10 2 4 5.7 CCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
145754982 161912 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 510 10 1 6 4.9 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3C(=O)O)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4166922 161912 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 510 10 1 6 4.9 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3C(=O)O)c1 10.1016/j.ejmech.2017.07.001
24857286 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
6484 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
CHEMBL1829174 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
DB12491 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
155515835 169431 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 439 11 2 5 4.9 COCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4442354 169431 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 439 11 2 5 4.9 COCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
132578494 153975 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3941821 153975 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990702 153975 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137643956 157728 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4088797 157728 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
162659927 180800 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 500 12 1 3 8.3 COc1ccc(CCCC(C)(C)C)c(-c2ccc(COc3cccc(C(CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4763356 180800 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 500 12 1 3 8.3 COc1ccc(CCCC(C)(C)C)c(-c2ccc(COc3cccc(C(CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acs.jmedchem.0c00843
127027730 137190 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 443 7 1 6 4.6 O=C1NC(=O)C(Cc2ccc(OCc3nc4ccccc4n3Cc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758919 137190 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 443 7 1 6 4.6 O=C1NC(=O)C(Cc2ccc(OCc3nc4ccccc4n3Cc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
145965797 163833 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 501 9 2 7 4.9 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc4c(c3)OCO4)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4213089 163833 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 501 9 2 7 4.9 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc4c(c3)OCO4)s2)cc1 10.1016/j.ejmech.2017.09.019
90372365 141610 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883504 141610 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
58319139 86116 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1cccc(C)c1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315542 86116 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1cccc(C)c1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
127030715 138469 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.6 C=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3785544 138469 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.6 C=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
24825484 87563 0 None 208 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL234269 87563 0 None 208 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
145959722 161641 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 544 8 1 5 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C(C)(C)C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4162588 161641 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 544 8 1 5 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C(C)(C)C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
134135852 143848 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 502 9 1 8 3.6 CCOc1ccc(F)c(N2CC[C@@H](Oc3cnc(N4CC(OC)[C@@H](C)[C@@H]4CC(=O)O)cn3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3905856 143848 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 502 9 1 8 3.6 CCOc1ccc(F)c(N2CC[C@@H](Oc3cnc(N4CC(OC)[C@@H](C)[C@@H]4CC(=O)O)cn3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
54586484 61825 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 61825 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
145950402 162373 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4174136 162373 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
145953365 161911 0 None -1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166892 161911 0 None -1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
56680363 65023 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 331 2 1 2 4.0 O=C(O)C1CC1c1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
CHEMBL1829172 65023 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 331 2 1 2 4.0 O=C(O)C1CC1c1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
57706642 80259 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 490 9 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151299 80259 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 490 9 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
90644291 111466 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288349 111466 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
168287667 191065 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 466 12 1 5 5.8 CCOc1ccc(/C=C/c2cc(OCC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5196235 191065 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 466 12 1 5 5.8 CCOc1ccc(/C=C/c2cc(OCC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
134142866 145109 0 None -9 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 358 7 1 3 4.6 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3915765 145109 0 None -9 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 358 7 1 3 4.6 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
71562641 86096 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 400 9 1 4 3.3 CS(=O)(=O)CCCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315254 86096 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 400 9 1 4 3.3 CS(=O)(=O)CCCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
145964802 163727 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4211807 163727 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
66562391 138460 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 262 4 2 2 2.1 C/C(C#Cc1ccc(CCC(=O)O)c(F)c1)=C/CO 10.1021/acs.jmedchem.5b01962
CHEMBL3785413 138460 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 262 4 2 2 2.1 C/C(C#Cc1ccc(CCC(=O)O)c(F)c1)=C/CO 10.1021/acs.jmedchem.5b01962
145980608 166091 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3ccc(-c4ccccc4)cc3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4281316 166091 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3ccc(-c4ccccc4)cc3)ccc21 10.1016/j.ejmech.2018.09.071
54757621 64992 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cnc(Cl)nc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
CHEMBL1829142 64992 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cnc(Cl)nc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
46231656 199430 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccnc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL603066 199430 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccnc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
134130696 141605 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 141605 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
118638001 141588 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883355 141588 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
122193975 123461 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3629049 123461 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
25150120 173432 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL454257 173432 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
54757831 65022 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 333 3 1 2 4.1 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)cc(Cl)nc1Cl 10.1021/jm2005699
CHEMBL1829171 65022 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 333 3 1 2 4.1 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)cc(Cl)nc1Cl 10.1021/jm2005699
58218673 156983 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079930 156983 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
853224 94139 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94139 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
127050771 139699 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805246 139699 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
145979252 166095 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 442 7 1 4 5.3 O=C(O)CC(c1ccc(F)cc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4281376 166095 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 442 7 1 4 5.3 O=C(O)CC(c1ccc(F)cc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145962164 160930 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 367 6 1 6 3.0 O=C1NC(=O)C(Cc2ccc(OCCn3cnc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4127761 160930 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 367 6 1 6 3.0 O=C1NC(=O)C(Cc2ccc(OCCn3cnc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
53248846 61824 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 61824 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
46941175 61483 20 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61483 20 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
162659599 180616 0 None -4 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4761101 180616 0 None -4 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
90151205 156744 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4076882 156744 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
162666840 181872 0 None -3 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 181872 0 None -3 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
137638184 156215 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070619 156215 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
134129938 141908 0 None -263 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 414 6 1 4 5.0 COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F 10.1021/acsmedchemlett.6b00394
CHEMBL3890089 141908 0 None -263 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 414 6 1 4 5.0 COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F 10.1021/acsmedchemlett.6b00394
58319127 86125 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm301470a
CHEMBL2315551 86125 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm301470a
54580132 61475 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/ml100106c
CHEMBL1773253 61475 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/ml100106c
57521913 75917 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 9 1 3 5.3 CCOc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058526 75917 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 9 1 3 5.3 CCOc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
142738545 161726 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 279 4 2 1 4.2 Cc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
CHEMBL4164008 161726 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 279 4 2 1 4.2 Cc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
46231713 199351 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc1 10.1016/j.bmcl.2009.10.052
CHEMBL602457 199351 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc1 10.1016/j.bmcl.2009.10.052
51349993 58528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1cccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
CHEMBL1688460 58528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1cccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
24857286 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
6484 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
CHEMBL1829174 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
DB12491 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
24857286 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
6484 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
CHEMBL1829174 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
DB12491 1594 66 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
155550483 173731 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 501 12 2 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4550165 173731 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 501 12 2 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
127046960 139461 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2017.12.030
CHEMBL3799946 139461 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2017.12.030
CHEMBL4227915 139461 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2017.12.030
25150014 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm2005699
3952 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm2005699
CHEMBL449588 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm2005699
25150014 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/ml4000673
3952 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/ml4000673
CHEMBL449588 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/ml4000673
60195125 3825 5 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3825 5 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3825 5 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
145963855 163647 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 476 9 1 3 7.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4210827 163647 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 476 9 1 3 7.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
168285924 191079 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 392 7 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5196452 191079 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 392 7 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
137639817 156263 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 504 10 1 5 6.6 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCC4(C)COC4)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4071066 156263 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 504 10 1 5 6.6 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCC4(C)COC4)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
137653896 157999 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
CHEMBL4091552 157999 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
90151652 158128 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 507 7 1 5 5.7 CCc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4092937 158128 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 507 7 1 5 5.7 CCc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
90151514 159114 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4103854 159114 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
58218630 159108 0 None -13 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103729 159108 0 None -13 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
137637243 155348 0 None -4 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 343 5 1 4 4.1 O=C(O)CCc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
CHEMBL4060517 155348 0 None -4 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 343 5 1 4 4.1 O=C(O)CCc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
134143394 153943 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 545 11 1 7 5.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3nc(C5CC5)no3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3917858 153943 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 545 11 1 7 5.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3nc(C5CC5)no3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990389 153943 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 545 11 1 7 5.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3nc(C5CC5)no3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
53248846 61824 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 61824 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
54580132 61475 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/jm300215x
CHEMBL1773253 61475 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/jm300215x
145966167 163671 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 407 7 1 5 3.7 N#Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4211064 163671 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 407 7 1 5 3.7 N#Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
561372 58519 59 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1688452 58519 59 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
75511317 121996 5 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.3 Cc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601057 121996 5 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.3 Cc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
145955263 161991 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4168048 161991 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
145990715 166444 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4288001 166444 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
25150014 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm301470a
3952 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm301470a
CHEMBL449588 3822 48 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm301470a
162668241 181924 0 None -4 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4787007 181924 0 None -4 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
71612898 89553 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381295 89553 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
71562771 86104 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315530 86104 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
145974495 164173 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 396 7 1 4 4.1 Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4217477 164173 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 396 7 1 4 4.1 Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
127032539 138281 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
CHEMBL3781077 138281 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
155522452 170147 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
CHEMBL4452044 170147 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
137657002 159255 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 3 3.7 Cc1ccccc1C(=O)c1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4105565 159255 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 3 3.7 Cc1ccccc1C(=O)c1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
90372625 167160 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167160 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167160 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
5280933 177646 59 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O 10.1016/j.ejmech.2015.12.049
CHEMBL464982 177646 59 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O 10.1016/j.ejmech.2015.12.049
71562768 86097 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315255 86097 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
127050769 139738 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 413 9 2 7 3.4 COc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
CHEMBL3805670 139738 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 413 9 2 7 3.4 COc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
23083190 58530 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 8 1 3 5.7 Cc1cccc(C)c1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688462 58530 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 8 1 3 5.7 Cc1cccc(C)c1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
156013404 176885 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmcl.2021.127969
CHEMBL4638956 176885 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmcl.2021.127969
131986378 164029 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4215544 164029 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145950347 162288 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172828 162288 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
54586486 61833 0 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777870 61833 0 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayAgonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm8010178
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayAgonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm8010178
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayAgonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm8010178
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm2005699
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm2005699
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm2005699
127031003 138614 0 None 371 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C\C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3787072 138614 0 None 371 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C\C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
3681700 198630 13 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2cccc(Oc3ccccc3)c2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL597424 198630 13 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2cccc(Oc3ccccc3)c2)S1 10.1016/j.bmcl.2009.10.052
9995943 198853 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2011.03.114
CHEMBL598935 198853 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2011.03.114
86803183 121942 2 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(Cl)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600999 121942 2 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(Cl)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
54757733 65012 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 343 5 1 3 4.3 O=C(O)CCc1ccc(C#Cc2ccnc(Oc3ccccc3)c2)cc1 10.1021/jm2005699
CHEMBL1829161 65012 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 343 5 1 3 4.3 O=C(O)CCc1ccc(C#Cc2ccnc(Oc3ccccc3)c2)cc1 10.1021/jm2005699
54582150 61481 0 None 22 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL1773259 61481 0 None 22 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2018.06.047
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2018.06.047
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2018.06.047
11271473 74123 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022584 74123 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2027975 74123 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
54586484 61825 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 61825 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
118645671 180347 0 None -5 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4758060 180347 0 None -5 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
127034370 138312 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3781477 138312 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
44409664 76937 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 360 8 2 3 4.8 CNC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL208175 76937 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 360 8 2 3 4.8 CNC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
71460255 80384 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
CHEMBL2152069 80384 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
168276826 189531 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5173326 189531 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
168278602 190392 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.5 O=C(O)COc1ccc(OCc2cccc(-c3ccc4cc(OCC5CC5)ccc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5186275 190392 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.5 O=C(O)COc1ccc(OCc2cccc(-c3ccc4cc(OCC5CC5)ccc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
9995943 198853 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598935 198853 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
90151529 157226 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 497 6 1 5 5.2 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4082717 157226 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 497 6 1 5 5.2 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
1052 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
3323 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
5280450 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
CHEMBL267476 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
DB14104 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
1052 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
3323 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
5280450 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
CHEMBL267476 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
DB14104 2290 81 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
127030344 138615 0 None 69 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.2 O=C(O)CCc1ccc(C#CC2CCCC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3787110 138615 0 None 69 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.2 O=C(O)CCc1ccc(C#CC2CCCC2)cc1 10.1021/acs.jmedchem.5b01962
51350270 58531 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
CHEMBL1688463 58531 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
11327107 73703 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
CHEMBL2022248 73703 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
122185444 122173 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 7 1 3 5.3 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604054 122173 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 7 1 3 5.3 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
58172989 111477 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288360 111477 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
122193735 123450 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628755 123450 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
168293256 191541 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 464 10 1 4 6.4 Cc1ccc(OCC2CCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5203672 191541 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 464 10 1 4 6.4 Cc1ccc(OCC2CCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
137631853 155771 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4065518 155771 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
132606864 157204 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157204 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
23111708 73701 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/jm2012968
CHEMBL2022246 73701 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/jm2012968
118145020 170502 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4457184 170502 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
127046666 139475 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cncc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3800040 139475 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cncc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
45107311 118627 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1021/ml500391n
CHEMBL3427711 118627 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1021/ml500391n
45107311 118627 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427711 118627 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1016/j.bmc.2015.07.028
68194449 182232 0 None -4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182232 0 None -4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
90356885 166974 0 None 16 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 166974 0 None 16 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 166974 0 None 16 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
90372616 141701 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
45107476 118489 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1021/ml500391n
CHEMBL3425533 118489 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1021/ml500391n
45107476 118489 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3425533 118489 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
73051869 166882 3 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 521 10 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2cc3c(cn2)[C@@H]2[C@@H](C(=O)O)[C@@H]2C3)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4297471 166882 3 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 521 10 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2cc3c(cn2)[C@@H]2[C@@H](C(=O)O)[C@@H]2C3)c1 10.1021/acs.jmedchem.1c00031
51350138 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
CHEMBL1688473 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
51350138 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
CHEMBL1688473 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
51350138 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL1688473 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
6483 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
66553168 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL2386353 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
90372613 167183 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167183 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167183 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.1c00031
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.1c00031
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.1c00031
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00460
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00460
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00460
137653903 158021 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4091723 158021 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
145952673 161886 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 443 7 1 4 4.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)o2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166397 161886 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 443 7 1 4 4.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)o2)cc1 10.1016/j.ejmech.2018.04.023
145990715 166444 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4288001 166444 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
24825479 146734 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 359 7 2 3 5.3 O=C(O)C1CC1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL392869 146734 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 359 7 2 3 5.3 O=C(O)C1CC1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2020.127650
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2020.127650
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2020.127650
51350272 58533 0 None 107 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58533 0 None 107 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
86817649 121945 2 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.5 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccc(Cl)cc2)no1 10.1016/j.bmcl.2015.06.018
CHEMBL3601002 121945 2 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.5 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccc(Cl)cc2)no1 10.1016/j.bmcl.2015.06.018
137636358 155345 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4060499 155345 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
90151428 157507 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 475 6 1 5 5.3 Cc1ccccc1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4085928 157507 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 475 6 1 5 5.3 Cc1ccccc1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
58218709 157872 0 None -4 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
CHEMBL4090240 157872 0 None -4 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
9995943 198853 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Partial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assayPartial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL598935 198853 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Partial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assayPartial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
3514336 45723 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 4.0 O=C(O)C1CC(=O)N(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL1532576 45723 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 4.0 O=C(O)C1CC(=O)N(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
24825486 86373 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1cccc(NCc2ccc(-c3ccccc3)cc2)c1 10.1016/j.bmcl.2006.12.084
CHEMBL232192 86373 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1cccc(NCc2ccc(-c3ccccc3)cc2)c1 10.1016/j.bmcl.2006.12.084
118623088 141595 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 141595 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
57522038 3824 54 None -1995 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assayAgonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
6490 3824 54 None -1995 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assayAgonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
CHEMBL2058533 3824 54 None -1995 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assayAgonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
24825498 152551 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 358 6 2 3 4.4 O=C(O)CCc1ccc(NCc2cc(C(F)(F)F)cnc2Cl)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL397613 152551 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 358 6 2 3 4.4 O=C(O)CCc1ccc(NCc2cc(C(F)(F)F)cnc2Cl)cc1 10.1016/j.bmcl.2006.12.084
24825497 161317 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 273 6 2 2 3.5 O=C(O)CCc1ccc(NCc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL414895 161317 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 273 6 2 2 3.5 O=C(O)CCc1ccc(NCc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.12.084
127033354 138601 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.5 O=C(O)CCc1ccc(C#CC2CC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786964 138601 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.5 O=C(O)CCc1ccc(C#CC2CC2)cc1 10.1021/acs.jmedchem.5b01962
145973087 164149 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 385 7 2 5 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4217225 164149 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 385 7 2 5 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
145987309 166549 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4289942 166549 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
127046665 139230 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)n1 10.1016/j.ejmech.2016.03.054
CHEMBL3798520 139230 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)n1 10.1016/j.ejmech.2016.03.054
145961656 160785 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 400 6 1 5 4.3 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccc(Cl)cc43)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4125720 160785 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 400 6 1 5 4.3 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccc(Cl)cc43)cc2)S1 10.1016/j.bmcl.2018.03.051
46231433 198883 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 315 4 1 4 3.7 O=C1NC(=O)C(Cc2ccc(Sc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599068 198883 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 315 4 1 4 3.7 O=C1NC(=O)C(Cc2ccc(Sc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
54583582 61835 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777872 61835 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
145978511 163117 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 460 9 1 5 4.8 CCOc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4204628 163117 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 460 9 1 5 4.8 CCOc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
44409877 74658 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 346 8 2 3 4.5 NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL203334 74658 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 346 8 2 3 4.5 NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
148485044 174798 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 453 11 2 5 5.2 COCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4574808 174798 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 453 11 2 5 5.2 COCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
155528599 170788 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2ccc(Cl)c(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4461611 170788 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2ccc(Cl)c(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
561372 58519 59 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688452 58519 59 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm101405t
90151297 156658 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4075946 156658 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
57325916 73759 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022581 73759 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
24857286 1594 66 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
6484 1594 66 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
CHEMBL1829174 1594 66 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
DB12491 1594 66 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
57521811 75913 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Cl)cc2)cc1 10.1021/jm300215x
CHEMBL2058522 75913 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Cl)cc2)cc1 10.1021/jm300215x
25150114 184577 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1cccc(C#Cc2ccc(OCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL485713 184577 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1cccc(C#Cc2ccc(OCC(=O)O)cc2)c1 10.1021/jm8010178
54757627 65009 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 269 3 1 2 2.6 O=C(O)CCc1ccc(C#Cc2ccnc(F)c2)cc1 10.1021/jm2005699
CHEMBL1829158 65009 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 269 3 1 2 2.6 O=C(O)CCc1ccc(C#Cc2ccnc(F)c2)cc1 10.1021/jm2005699
127033020 138546 0 None 18 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 256 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786418 138546 0 None 18 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 256 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
118637973 162193 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171391 162193 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
54586484 61825 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 61825 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
90644288 111463 0 None 20 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288346 111463 0 None 20 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
145965661 163546 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 450 7 1 4 4.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4209622 163546 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 450 7 1 4 4.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1 10.1016/j.ejmech.2017.07.001
71613311 89563 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381305 89563 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
23157589 58535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 373 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(CN(C)c2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688467 58535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 373 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(CN(C)c2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
168285003 190929 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 492 11 1 4 7.2 Cc1ccc(OCCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5194153 190929 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 492 11 1 4 7.2 Cc1ccc(OCCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
137658243 159070 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 6 1 4 3.9 COc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103345 159070 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 6 1 4 3.9 COc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
145993621 166829 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cccc(Cl)c3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294975 166829 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cccc(Cl)c3O2)cc1 10.1016/j.bmc.2018.10.019
1049 360 70 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
4618 360 70 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
5280934 360 70 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
CHEMBL8739 360 70 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
DB00132 360 70 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
164616580 184745 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4859651 184745 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
90372613 167183 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167183 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167183 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
57521808 75910 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL2058519 75910 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
71562424 86118 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccc(F)cc2)cc1 10.1021/jm301470a
CHEMBL2315544 86118 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccc(F)cc2)cc1 10.1021/jm301470a
54757732 65011 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 281 4 1 3 2.5 COc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
CHEMBL1829160 65011 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 281 4 1 3 2.5 COc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
54582149 61477 0 None 33 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773255 61477 0 None 33 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
57522038 3824 54 None -1995 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
6490 3824 54 None -1995 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
CHEMBL2058533 3824 54 None -1995 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
24857286 1594 66 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
6484 1594 66 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
CHEMBL1829174 1594 66 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
DB12491 1594 66 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
122185438 122164 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 325 8 1 4 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc(C#N)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604045 122164 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 325 8 1 4 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc(C#N)c2)cc1 10.1016/j.bmc.2015.07.028
54582629 61827 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 61827 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
137646482 157209 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082459 157209 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
127047529 139288 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798881 139288 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
127032539 138281 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL3781077 138281 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
145970371 164481 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 393 6 1 5 4.8 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.bmc.2017.12.030
CHEMBL4226180 164481 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 393 6 1 5 4.8 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.bmc.2017.12.030
54583098 61480 0 None 70 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
CHEMBL1773258 61480 0 None 70 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
44409927 77228 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 535 8 2 4 7.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N[C@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL208783 77228 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 535 8 2 4 7.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N[C@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2006.01.007
23159951 58548 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 338 7 1 3 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3cccs3)c2)cc1 10.1021/jm101405t
CHEMBL1688480 58548 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 338 7 1 3 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3cccs3)c2)cc1 10.1021/jm101405t
75202609 156197 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 7 1 4 5.5 COc1ccc(F)c(N2CCC(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4070443 156197 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 7 1 4 5.5 COc1ccc(F)c(N2CCC(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
46231483 199112 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 4 1 4 2.8 O=C1NC(=O)C(Cc2ccc(C(=O)c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL600658 199112 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 4 1 4 2.8 O=C1NC(=O)C(Cc2ccc(C(=O)c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
145950191 162387 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 460 7 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4174315 162387 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 460 7 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
90372616 141701 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
145947998 167155 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167155 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167155 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
155541840 172488 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 8 2 4 4.6 COc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4519415 172488 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 8 2 4 4.6 COc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
145975522 162989 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc(F)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4202901 162989 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc(F)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
131986112 163865 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213548 163865 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145950447 162436 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4175272 162436 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
155516498 169555 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4443853 169555 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
132606863 157281 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157281 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
122193735 123450 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2018.07.050
CHEMBL3628755 123450 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2018.07.050
142738551 161492 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Cl)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4160141 161492 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Cl)cc2c1 10.1021/acsmedchemlett.7b00460
71612683 89540 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381281 89540 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
1052 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
122184686 121946 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccc(Cl)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601003 121946 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccc(Cl)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
168281295 190209 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc(OCC4CC4)cc3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5183783 190209 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc(OCC4CC4)cc3)c2)cc1F 10.1016/j.bmc.2022.116615
168294961 191819 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5208111 191819 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
23111754 73700 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022245 73700 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
1052 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
90644289 111464 0 None -8 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288347 111464 0 None -8 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
145947764 167141 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4238097 167141 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4302391 167141 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
134153562 152191 0 None -758 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 394 7 1 3 4.9 O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F 10.1016/j.bmcl.2016.10.054
CHEMBL3973101 152191 0 None -758 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 394 7 1 3 4.9 O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F 10.1016/j.bmcl.2016.10.054
118637974 161489 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4160127 161489 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
134130787 141734 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884916 141734 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
155527626 170665 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459709 170665 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
46231844 198852 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 430 4 1 5 5.1 Cc1cc(Oc2ncc(C(F)(F)F)cc2Cl)cc(C)c1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL598934 198852 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 430 4 1 5 5.1 Cc1cc(Oc2ncc(C(F)(F)F)cc2Cl)cc(C)c1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
46231487 200760 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL611084 200760 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1 10.1016/j.bmcl.2009.10.052
118645756 180880 3 None -2 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 180880 3 None -2 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
155527487 170650 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459517 170650 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
561372 58519 59 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm300215x
CHEMBL1688452 58519 59 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm300215x
145978233 163039 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 432 7 2 4 5.6 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4203471 163039 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 432 7 2 4 5.6 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
145976608 163205 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccccc2F)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4205537 163205 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccccc2F)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54585039 61474 5 None 17 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/ml100106c
CHEMBL1773252 61474 5 None 17 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/ml100106c
1052 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2290 81 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
134151151 153983 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 513 10 1 4 6.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3963542 153983 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 513 10 1 4 6.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990756 153983 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 513 10 1 4 6.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
51031010 156090 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4069191 156090 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
51357276 181425 0 None -10 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None -10 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
71612896 89551 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381293 89551 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
46231653 199428 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL603064 199428 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
118642379 141587 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 141587 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
71615468 89560 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2ccc(F)c(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381302 89560 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2ccc(F)c(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
71613316 89568 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381310 89568 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
75511302 121938 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2coc(-c3cccc(F)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600995 121938 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2coc(-c3cccc(F)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
122185445 122174 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 7 1 3 5.8 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604055 122174 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 7 1 3 5.8 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
58218542 156225 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070703 156225 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
122185449 122178 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 1 4 3.7 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3ncccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604059 122178 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 1 4 3.7 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3ncccc32)cc1 10.1016/j.bmc.2015.07.028
58218638 156894 0 None -75 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4078852 156894 0 None -75 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
51350272 58533 0 None 107 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58533 0 None 107 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
11739868 75197 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@@H]1C[C@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL204455 75197 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@@H]1C[C@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
25149900 172054 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 268 3 2 3 2.3 O=C(O)COc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm8010178
CHEMBL449321 172054 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 268 3 2 3 2.3 O=C(O)COc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm8010178
23136363 58525 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL1688458 58525 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2017.01.034
137661929 158959 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4101950 158959 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
145959598 161805 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4165046 161805 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
24857286 1594 66 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
6484 1594 66 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL1829174 1594 66 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
DB12491 1594 66 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
145964820 163750 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 440 8 1 5 4.4 COc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4212170 163750 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 440 8 1 5 4.4 COc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
23136363 58525 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/ml100106c
CHEMBL1688458 58525 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/ml100106c
58218672 156180 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 3 4.6 Cc1ccccc1Sc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070270 156180 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 3 4.6 Cc1ccccc1Sc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57325678 73706 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 387 6 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(n2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022250 73706 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 387 6 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(n2)CCC3CC(=O)O)c1 10.1021/jm2012968
58319142 86091 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CO)cc1 10.1021/jm301470a
CHEMBL2315249 86091 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CO)cc1 10.1021/jm301470a
86803224 121936 18 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 337 7 1 4 4.2 Cc1oc(-c2ccccc2)nc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600993 121936 18 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 337 7 1 4 4.2 Cc1oc(-c2ccccc2)nc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2015.06.018
57398938 69683 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939653 69683 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
134130352 141613 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 141613 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
153213696 174940 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 351 7 2 3 4.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4577954 174940 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 351 7 2 3 4.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
25150118 186108 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 295 4 1 3 3.0 O=C(O)CCc1ccc(C#Cc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm8010178
CHEMBL488396 186108 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 295 4 1 3 3.0 O=C(O)CCc1ccc(C#Cc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm8010178
44409916 138369 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C(C)CC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL378275 138369 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C(C)CC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
57393689 69670 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 380 8 1 3 5.0 COc1ccc(COc2ccc(C(CC(=O)O)c3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939640 69670 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 380 8 1 3 5.0 COc1ccc(COc2ccc(C(CC(=O)O)c3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
137632053 155816 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 386 8 1 4 5.2 COc1ccc(F)c(-c2cccc(COc3ccc(CCC(=O)O)s3)c2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4065959 155816 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 386 8 1 4 5.2 COc1ccc(F)c(-c2cccc(COc3ccc(CCC(=O)O)s3)c2)c1 10.1021/acs.jmedchem.6b01357
122185433 122149 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 391 9 1 5 3.1 CCOC(CC(=O)NS(C)(=O)=O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604031 122149 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 391 9 1 5 3.1 CCOC(CC(=O)NS(C)(=O)=O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
127051658 139756 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3F)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805888 139756 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3F)s2)cc1 10.1016/j.bmc.2016.04.065
127050770 139761 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 419 8 2 6 3.7 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)c(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805952 139761 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 419 8 2 6 3.7 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)c(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
145991380 166432 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1ccnc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4287775 166432 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1ccnc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
155513821 169247 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4439462 169247 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
146763588 173218 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 515 12 2 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4537797 173218 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 515 12 2 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
90151022 157785 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4089313 157785 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
118144976 170688 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4460109 170688 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
54586484 61825 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 61825 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
59541 175762 89 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assay
ChEMBL 168 3 1 2 1.9 O=C(O)CSc1ccccc1 10.1016/j.bmcl.2021.127969
CHEMBL459548 175762 89 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assay
ChEMBL 168 3 1 2 1.9 O=C(O)CSc1ccccc1 10.1016/j.bmcl.2021.127969
90655861 110762 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265145 110762 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
73891117 113764 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3330550 113764 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
6483 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
131986035 163505 0 None 5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209136 163505 0 None 5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
51350138 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2005699
CHEMBL1688473 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2005699
51350138 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL1688473 58541 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
146316684 170999 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4464769 170999 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
68194743 181966 9 None -5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None -5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
6483 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
45107281 118618 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
CHEMBL3427702 118618 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
45107281 118618 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427702 118618 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
67087246 182295 4 None -12 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None -12 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
23157191 58534 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 359 7 2 2 5.6 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688466 58534 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 359 7 2 2 5.6 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
59590895 110767 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265150 110767 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
11674915 58554 1 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL1688486 58554 1 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
118638010 167004 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167004 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167004 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
146316684 170999 0 None 3 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4464769 170999 0 None 3 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
44409677 140700 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 447 6 3 5 5.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NO)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382915 140700 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 447 6 3 5 5.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NO)cc1 10.1016/j.bmcl.2006.01.007
46854655 391 43 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300133f
6485 391 43 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300133f
CHEMBL1829173 391 43 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300133f
155527487 170650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459517 170650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
90150977 155628 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 521 7 1 5 6.2 CC(C)c1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4063905 155628 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 521 7 1 5 6.2 CC(C)c1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
15659413 98272 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL277845 98272 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
57521702 75909 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1ccccc1COc1ccc(CCC(=O)O)cc1 10.1021/jm300215x
CHEMBL2058518 75909 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1ccccc1COc1ccc(CCC(=O)O)cc1 10.1021/jm300215x
57521916 75920 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cc(Cl)ccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL2058529 75920 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cc(Cl)ccc2-c2ccccc2)cc1 10.1021/jm300215x
54757516 64998 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccnc2Cl)cc1 10.1021/jm2005699
CHEMBL1829148 64998 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccnc2Cl)cc1 10.1021/jm2005699
44634023 64994 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2cccnc2)cc1 10.1021/jm2005699
CHEMBL1829144 64994 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2cccnc2)cc1 10.1021/jm2005699
15659413 98272 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL277845 98272 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
122193975 123461 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL3629049 123461 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
67087173 181878 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 181878 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134130696 141605 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 141605 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
127031413 138328 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 421 8 1 5 5.0 CCOc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
CHEMBL3781733 138328 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 421 8 1 5 5.0 CCOc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
145983006 164927 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 499 13 1 7 5.1 Cc1cc(OCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
CHEMBL4240026 164927 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 499 13 1 7 5.1 Cc1cc(OCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
71615669 89572 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 430 4 1 4 5.7 Cc1cc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381314 89572 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 430 4 1 4 5.7 Cc1cc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
86803186 121947 3 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3ccc(C(F)(F)F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601004 121947 3 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3ccc(C(F)(F)F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
168291030 191301 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 424 10 1 4 5.6 CCCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5199948 191301 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 424 10 1 4 5.6 CCCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
145956739 161588 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 468 8 1 5 4.4 O=C(O)CCc1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4161630 161588 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 468 8 1 5 4.4 O=C(O)CCc1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
145986077 165898 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 342 4 1 2 4.7 Cc1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4277789 165898 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 342 4 1 2 4.7 Cc1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
137629985 160477 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccncc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4101306 160477 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccncc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116362 160477 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccncc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
137650498 156780 0 None -2 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 382 5 1 5 4.3 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3C#N)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4077353 156780 0 None -2 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 382 5 1 5 4.3 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3C#N)ccc12 10.1021/acs.jmedchem.7b00210
137640163 156306 0 None -5 2 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 372 5 1 5 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(C(C)CC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
CHEMBL4071523 156306 0 None -5 2 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 372 5 1 5 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(C(C)CC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
127025285 137146 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 457 6 1 4 5.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccc(C(F)(F)F)cc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758553 137146 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 457 6 1 4 5.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccc(C(F)(F)F)cc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
73356514 89944 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386368 89944 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
54757514 64996 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
CHEMBL1829146 64996 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
44319268 106687 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL316370 106687 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
67058273 118624 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1021/ml500391n
CHEMBL3427708 118624 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1021/ml500391n
67058273 118624 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427708 118624 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
121294396 179080 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 603 12 1 7 6.5 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)OC)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4743254 179080 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 603 12 1 7 6.5 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)OC)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
118719721 115164 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353742 115164 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2014.11.016
118719721 115164 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3353742 115164 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
118719721 115164 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3353742 115164 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
57400636 69676 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 294 6 1 2 3.8 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939646 69676 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 294 6 1 2 3.8 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
90151177 159185 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 491 7 1 6 5.0 COc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4104738 159185 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 491 7 1 6 5.0 COc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
57390187 69677 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 7 1 2 3.9 CC#CC(CC(=O)O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939647 69677 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 7 1 2 3.9 CC#CC(CC(=O)O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
137640032 156388 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2[C@@H](C)CC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4072491 156388 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2[C@@H](C)CC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
90151279 157695 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(Cl)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4088375 157695 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(Cl)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
118688890 189650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)[C@H](CC(=O)O)CO3)c1 10.1016/j.bmc.2022.116615
CHEMBL5175124 189650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)[C@H](CC(=O)O)CO3)c1 10.1016/j.bmc.2022.116615
131986297 163653 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210878 163653 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
46231840 198850 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598917 198850 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
118737972 118626 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1021/ml500391n
CHEMBL3427710 118626 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1021/ml500391n
118737972 118626 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427710 118626 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1016/j.bmc.2015.07.028
58172969 122165 3 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 345 9 1 5 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc([N+](=O)[O-])c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604046 122165 3 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 345 9 1 5 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc([N+](=O)[O-])c2)cc1 10.1016/j.bmc.2015.07.028
23136363 58525 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm300215x
CHEMBL1688458 58525 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm300215x
145973478 164040 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 454 9 1 5 4.8 CCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4215675 164040 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 454 9 1 5 4.8 CCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
71612895 89502 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 398 3 1 4 4.3 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2380322 89502 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 398 3 1 4 4.3 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
75204487 158421 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4096102 158421 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
134144929 149916 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 418 5 2 4 6.2 O=C(O)CCc1ccc2oc(Nc3c(Cl)c(Cl)cc(Cl)c3Cl)nc2c1 10.1016/j.bmcl.2016.10.074
CHEMBL3954105 149916 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 418 5 2 4 6.2 O=C(O)CCc1ccc2oc(Nc3c(Cl)c(Cl)cc(Cl)c3Cl)nc2c1 10.1016/j.bmcl.2016.10.074
57521809 75911 0 None -13 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058520 75911 0 None -13 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL4210970 75911 0 None -13 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
57521914 75918 0 None 6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 416 8 1 3 5.8 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300215x
CHEMBL2058527 75918 0 None 6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 416 8 1 3 5.8 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300215x
73777153 142291 0 None -81 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 355 3 1 2 5.2 O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 10.1021/acsmedchemlett.6b00360
CHEMBL3893026 142291 0 None -81 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 355 3 1 2 5.2 O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 10.1021/acsmedchemlett.6b00360
54582148 61468 4 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(COc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773246 61468 4 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(COc2ccccc2)cc1 10.1021/ml100106c
134138318 147487 0 None -23 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 378 9 1 4 5.4 COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3934450 147487 0 None -23 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 378 9 1 4 5.4 COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 10.1016/j.bmcl.2016.10.054
57393691 69675 1 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939645 69675 1 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
118144976 170688 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4460109 170688 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
162652399 179648 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4749949 179648 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
1050 1871 86 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.01.007
11595431 1871 86 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.01.007
CHEMBL207881 1871 86 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.01.007
127034369 138227 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2cccc(F)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780456 138227 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2cccc(F)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
137646308 157329 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 295 4 1 3 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4083913 157329 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 295 4 1 3 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)s1 10.1021/acs.jmedchem.6b01357
145992631 166312 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 392 8 1 5 4.1 CCOC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4285740 166312 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 392 8 1 5 4.1 CCOC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
137635388 155283 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4059947 155283 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
145957539 161691 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4163496 161691 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
46231386 197553 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 3 4.0 O=C1CC(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)C(=O)N1 10.1016/j.bmcl.2009.10.052
CHEMBL589992 197553 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 3 4.0 O=C1CC(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)C(=O)N1 10.1016/j.bmcl.2009.10.052
8852666 192081 21 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
CHEMBL5219102 192081 21 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
57522038 3824 54 None -1995 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
6490 3824 54 None -1995 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
CHEMBL2058533 3824 54 None -1995 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
137658671 158901 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
CHEMBL4101219 158901 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
122185443 122172 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 9 1 3 5.2 CCOC(CC(=O)O)c1ccc(OCCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604053 122172 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 9 1 3 5.2 CCOC(CC(=O)O)c1ccc(OCCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
90644289 111464 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288347 111464 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
90644297 111472 0 None 32 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288355 111472 0 None 32 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
162676686 182904 0 None -11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 182904 0 None -11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
71615666 89569 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 388 4 1 4 4.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381311 89569 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 388 4 1 4 4.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2)c1)O3 10.1016/j.bmcl.2013.03.060
122193736 123451 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628756 123451 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
71449361 80248 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
CHEMBL2151288 80248 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
168282466 190663 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 543 12 1 6 5.4 Cn1nc(COCc2ccccc2F)c2c1CCN(Cc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
CHEMBL5190303 190663 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 543 12 1 6 5.4 Cn1nc(COCc2ccccc2F)c2c1CCN(Cc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
155529599 170890 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(OC)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4463298 170890 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(OC)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
137646337 157385 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 353 5 1 3 5.2 CC(C)(C)c1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4084441 157385 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 353 5 1 3 5.2 CC(C)(C)c1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
44319268 106687 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL316370 106687 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
118638016 167091 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163182 167091 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301725 167091 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
145967091 163565 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 410 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4209845 163565 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 410 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
44409844 74140 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 459 6 1 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL202835 74140 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 459 6 1 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N(C)C)cc1 10.1016/j.bmcl.2006.01.007
71613315 89567 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381309 89567 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
54757518 65001 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
CHEMBL1829150 65001 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
1622278 94562 10 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 94562 10 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
127051659 139685 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805086 139685 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
155565451 175022 7 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
CHEMBL4579901 175022 7 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
131986082 163602 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210243 163602 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58218608 156143 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4069764 156143 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
71613092 89554 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381296 89554 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
44409690 75222 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 420 7 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL204630 75222 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 420 7 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
168272362 190056 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3cccc(OCC4CC4)c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5181439 190056 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3cccc(OCC4CC4)c3)c2)cc1F 10.1016/j.bmc.2022.116615
162657311 180272 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 427 9 1 4 5.1 COc1ccc(F)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4757231 180272 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 427 9 1 4 5.1 COc1ccc(F)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
57393690 69674 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939644 69674 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
134136175 142148 0 None -51 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 388 7 1 3 5.5 Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
CHEMBL3892019 142148 0 None -51 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 388 7 1 3 5.5 Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
131986090 163740 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4212041 163740 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23136411 58524 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
CHEMBL1688457 58524 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
5849 66 39 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
97783 66 39 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
CHEMBL4278254 66 39 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
134134149 142843 0 None -100 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 348 8 1 3 5.4 O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3897776 142843 0 None -100 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 348 8 1 3 5.4 O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2016.10.054
162644059 181242 0 None 45 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None 45 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
127033239 138210 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 387 6 1 6 4.7 Cc1nc(-c2ccsc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780232 138210 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 387 6 1 6 4.7 Cc1nc(-c2ccsc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
75511301 121948 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 342 7 1 5 3.5 O=C(O)CCc1ccc(OCc2nc(-c3ccc(F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601005 121948 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 342 7 1 5 3.5 O=C(O)CCc1ccc(OCc2nc(-c3ccc(F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
57705531 80255 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 464 9 1 3 7.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
CHEMBL2151295 80255 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 464 9 1 3 7.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
137640919 156530 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4074138 156530 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.6b01559
137659517 158712 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 500 6 1 6 5.1 Cc1ccc(C#N)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4099189 158712 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 500 6 1 6 5.1 Cc1ccc(C#N)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
168294722 191872 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 427 7 1 5 5.3 O=C(O)COc1ccc(COc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1F 10.1016/j.ejmech.2021.114061
CHEMBL5208754 191872 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 427 7 1 5 5.3 O=C(O)COc1ccc(COc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1F 10.1016/j.ejmech.2021.114061
1050 1871 86 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1871 86 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1871 86 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
164616580 184745 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4859651 184745 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
54584570 61820 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 344 5 1 2 5.2 O=C(O)CCc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777857 61820 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 344 5 1 2 5.2 O=C(O)CCc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
145983493 164952 0 None -371 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 442 10 1 4 5.1 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4240607 164952 0 None -371 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 442 10 1 4 5.1 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
46231717 199262 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc(C(F)(F)F)c1 10.1016/j.bmcl.2009.10.052
CHEMBL601848 199262 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc(C(F)(F)F)c1 10.1016/j.bmcl.2009.10.052
46231718 199994 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.4 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL606206 199994 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.4 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
118737971 118622 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1021/ml500391n
CHEMBL3427706 118622 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1021/ml500391n
118737971 118622 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427706 118622 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
57325674 73704 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022249 73704 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
127047530 139058 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 413 9 1 5 5.1 CCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797383 139058 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 413 9 1 5 5.1 CCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
145966647 163637 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 468 10 1 5 5.2 CCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4210719 163637 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 468 10 1 5 5.2 CCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
54582145 61464 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 361 8 2 3 5.0 COc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773167 61464 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 361 8 2 3 5.0 COc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
122193736 123451 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL3628756 123451 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
155558174 174194 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 7 3 4 4.6 Cc1cc(O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4561122 174194 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 7 3 4 4.6 Cc1cc(O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
57706031 80256 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 10 1 3 7.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
CHEMBL2151296 80256 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 10 1 3 7.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
145992604 166280 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 362 4 1 2 5.0 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4285071 166280 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 362 4 1 2 5.0 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2018.08.075
58218740 155904 0 None -45 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4067052 155904 0 None -45 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
137529983 163325 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 516 8 2 5 6.2 Cc1cc(OCC2CCOC2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4206879 163325 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 516 8 2 5 6.2 Cc1cc(OCC2CCOC2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
131986294 163289 0 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206445 163289 0 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118623088 141595 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883407 141595 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
10292451 122167 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604048 122167 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
134131511 141626 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 141626 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
162664735 181504 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 181504 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
122185448 122177 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)c(F)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604058 122177 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)c(F)c2)cc1 10.1016/j.bmc.2015.07.028
118645541 180061 0 None 4 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4754974 180061 0 None 4 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
11961321 111307 3 None -4 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287569 111307 3 None -4 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
51350138 58541 0 None 660 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
CHEMBL1688473 58541 0 None 660 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
134131511 141626 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 141626 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
145987484 164658 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
CHEMBL4228985 164658 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
155527805 170705 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4460425 170705 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
137635907 155407 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 527 7 1 6 5.0 COc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4061175 155407 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 527 7 1 6 5.0 COc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
76900387 157003 3 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4080226 157003 3 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
9957245 178407 11 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL470757 178407 11 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
11327107 73703 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
CHEMBL2022248 73703 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
162646017 178892 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4740846 178892 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
58319134 86127 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315553 86127 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
75511304 121939 4 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2coc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600996 121939 4 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2coc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
145990228 166353 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 436 7 1 5 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(F)(F)F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4286382 166353 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 436 7 1 5 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(F)(F)F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
54584571 61840 0 None -1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777877 61840 0 None -1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
54757517 64999 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccc(Cl)nc2)cc1 10.1021/jm2005699
CHEMBL1829149 64999 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccc(Cl)nc2)cc1 10.1021/jm2005699
134153148 152187 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 519 7 1 6 5.5 COc1ccc(C)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3973075 152187 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 519 7 1 6 5.5 COc1ccc(C)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
53248846 61824 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 61824 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
90644287 111462 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288345 111462 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
131986300 163075 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203837 163075 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
57706778 80385 25 None -8 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152070 80385 25 None -8 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
58218608 156143 0 None -10 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4069764 156143 0 None -10 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145963330 161477 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 488 8 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4159848 161477 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 488 8 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
118129981 158920 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 158920 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
68194159 182479 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 182479 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
73354950 89947 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386370 89947 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
46231548 198812 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1C 10.1016/j.bmcl.2009.10.052
CHEMBL598673 198812 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1C 10.1016/j.bmcl.2009.10.052
153272850 171328 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 376 7 2 4 4.4 N#Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4469691 171328 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 376 7 2 4 4.4 N#Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
58218651 157774 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4089171 157774 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
71612681 89576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 406 4 1 4 5.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381318 89576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 406 4 1 4 5.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2F)c1)O3 10.1016/j.bmcl.2013.03.060
127033818 138218 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
CHEMBL3780334 138218 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
155551584 173427 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4542487 173427 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
121294455 180621 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.9 CCOC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4761155 180621 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.9 CCOC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
58218638 156894 0 None 75 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4078852 156894 0 None 75 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
58218694 157925 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4090766 157925 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
25150016 184841 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cc(C)cc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL486139 184841 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cc(C)cc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
145971800 163947 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 424 8 1 4 4.9 CC(C)c1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4214530 163947 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 424 8 1 4 4.9 CC(C)c1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
71655293 89930 0 None 52 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386354 89930 0 None 52 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
71612682 89539 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 456 4 1 4 5.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381280 89539 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 456 4 1 4 5.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
71612680 89575 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 440 4 1 4 5.6 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccc(F)cc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381317 89575 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 440 4 1 4 5.6 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccc(F)cc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
57705719 163917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 520 10 1 3 8.4 CC[C@H](CC(=O)O)c1ccc(F)c(OCc2ccc(-c3cc(OC)ccc3F)c(C3=CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4214121 163917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 520 10 1 3 8.4 CC[C@H](CC(=O)O)c1ccc(F)c(OCc2ccc(-c3cc(OC)ccc3F)c(C3=CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
87262743 158235 0 None -4 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4094160 158235 0 None -4 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
54582149 61477 0 None 33 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL1773255 61477 0 None 33 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
127027727 137288 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.2 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(C(F)(F)F)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759746 137288 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.2 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(C(F)(F)F)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
54584098 61476 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/jm300215x
CHEMBL1773254 61476 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/jm300215x
54757625 65007 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 270 3 1 2 3.5 Cc1ccsc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
CHEMBL1829156 65007 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 270 3 1 2 3.5 Cc1ccsc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
9957245 178407 11 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL470757 178407 11 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
168279392 190546 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 421 9 2 3 5.6 CC1(C)C2CCC1(C)C(NCc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
CHEMBL5188313 190546 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 421 9 2 3 5.6 CC1(C)C2CCC1(C)C(NCc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
142738582 183938 0 None 42 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4847662 183938 0 None 42 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
118638010 167004 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167004 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167004 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
3893 2255 92 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
4642 2255 92 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
5534 2255 92 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL108766 2255 92 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
DB03017 2255 92 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
23346507 87860 1 None 30 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL234834 87860 1 None 30 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/ml100106c
54584571 61840 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777877 61840 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
57522038 3824 54 None -1995 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
6490 3824 54 None -1995 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
CHEMBL2058533 3824 54 None -1995 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
145983825 165187 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 485 12 1 7 4.7 Cc1cc(OCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
CHEMBL4246335 165187 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 485 12 1 7 4.7 Cc1cc(OCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
127048842 139706 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 367 6 2 5 3.8 Cc1cccc(-c2cccc(NC(=O)c3nnc(CCC(=O)O)s3)c2)c1 10.1016/j.bmc.2016.04.065
CHEMBL3805328 139706 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 367 6 2 5 3.8 Cc1cccc(-c2cccc(NC(=O)c3nnc(CCC(=O)O)s3)c2)c1 10.1016/j.bmc.2016.04.065
90644302 111478 0 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288361 111478 0 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
1622278 94562 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 94562 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
90372616 141701 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 141701 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
145982433 166126 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1ccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4281988 166126 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1ccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)cc1 10.1016/j.ejmech.2018.09.071
90151763 157302 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccnc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4083678 157302 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccnc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
134141490 154047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 527 10 1 4 6.6 Cc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3926143 154047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 527 10 1 4 6.6 Cc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3991349 154047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 527 10 1 4 6.6 Cc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
53248846 61824 0 None 1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 61824 0 None 1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
57706009 80254 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 450 8 1 3 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151294 80254 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 450 8 1 3 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
57391960 69681 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml300133f
CHEMBL1939651 69681 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml300133f
127025488 137312 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 403 6 1 4 5.1 Cc1ccccc1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
CHEMBL3759922 137312 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 403 6 1 4 5.1 Cc1ccccc1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
142738553 161693 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4163511 161693 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3)cc2c1 10.1021/acsmedchemlett.7b00460
46231596 200288 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 401 4 1 4 5.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL607983 200288 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 401 4 1 4 5.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
90644303 111480 0 None -2 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288363 111480 0 None -2 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
137636358 155345 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4060499 155345 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
1622278 94562 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 94562 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
45107307 111479 4 None -3 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288362 111479 4 None -3 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
71460255 80384 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL2152069 80384 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acsmedchemlett.6b00443
71460255 80384 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL2152069 80384 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1016/j.bmcl.2019.04.050
127047532 139119 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 9 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC(C)C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797784 139119 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 9 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC(C)C)c1 10.1016/j.ejmech.2016.03.054
1050 1871 86 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
11595431 1871 86 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
CHEMBL207881 1871 86 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
145975484 163442 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 480 10 1 5 5.2 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4208237 163442 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 480 10 1 5 5.2 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
54757830 65020 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 335 3 1 2 4.3 O=C(O)CCc1ccc(C#Cc2ccnc3cc(Cl)ccc23)cc1 10.1021/jm2005699
CHEMBL1829169 65020 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 335 3 1 2 4.3 O=C(O)CCc1ccc(C#Cc2ccnc3cc(Cl)ccc23)cc1 10.1021/jm2005699
57521919 75924 0 None -23 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL2058532 75924 0 None -23 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL4207911 75924 0 None -23 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
24825491 87603 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 305 6 2 2 4.5 O=C(O)CCc1ccc(NCc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234467 87603 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 305 6 2 2 4.5 O=C(O)CCc1ccc(NCc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2006.12.084
24825492 149010 0 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL394666 149010 0 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1016/j.bmcl.2006.12.084
54757829 65019 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 375 5 1 2 4.7 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2Cc2ccccc2)cc1 10.1021/jm2005699
CHEMBL1829168 65019 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 375 5 1 2 4.7 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2Cc2ccccc2)cc1 10.1021/jm2005699
23346507 87860 1 None 30 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234834 87860 1 None 30 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1016/j.bmcl.2006.12.084
137638995 156423 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4072885 156423 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
137642604 157971 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4091228 157971 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
16058685 171991 0 None -1 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cellsAgonist activity at mouse GPR40 expressed in HEK293 cells
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.bmcl.2008.10.085
CHEMBL448569 171991 0 None -1 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cellsAgonist activity at mouse GPR40 expressed in HEK293 cells
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.bmcl.2008.10.085
131986030 164262 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218596 164262 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
11674915 58554 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL1688486 58554 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01357
137661294 158953 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101901 158953 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
68194743 181966 9 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
90357481 167055 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163916 167055 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301212 167055 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
162676686 182904 0 None -11 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 182904 0 None -11 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
90644296 111471 0 None 29 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288354 111471 0 None 29 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
11674915 58554 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688486 58554 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
57705880 110725 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL3264816 110725 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
57707025 164009 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4215239 164009 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
24857286 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
6484 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
CHEMBL1829174 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
DB12491 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
155512776 169097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4437470 169097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
155542122 172536 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4520404 172536 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
145971688 162467 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4175666 162467 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
24857286 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
6484 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
CHEMBL1829174 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
DB12491 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
90151527 156677 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4076149 156677 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
145947468 167113 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)CC5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4244619 167113 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)CC5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4301987 167113 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)CC5)c3)ccc21 10.1016/j.bmcl.2018.07.048
145948093 167165 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 9 1 3 7.2 CC(C)(CC(=O)O)c1ccc(OCc2cccc(-c3cccc4c3CCN(Cc3ccccc3)C4)c2)cc1 10.1016/j.bmcl.2018.07.048
CHEMBL4241897 167165 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 9 1 3 7.2 CC(C)(CC(=O)O)c1ccc(OCc2cccc(-c3cccc4c3CCN(Cc3ccccc3)C4)c2)cc1 10.1016/j.bmcl.2018.07.048
CHEMBL4302692 167165 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 9 1 3 7.2 CC(C)(CC(=O)O)c1ccc(OCc2cccc(-c3cccc4c3CCN(Cc3ccccc3)C4)c2)cc1 10.1016/j.bmcl.2018.07.048
15659412 202252 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL6931 202252 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
145990337 166227 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 390 6 1 5 3.3 O=C(O)CC1(c2ccc(OCC3COc4ccc(Cl)cc4O3)cc2)COC1 10.1016/j.bmc.2018.10.019
CHEMBL4283988 166227 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 390 6 1 5 3.3 O=C(O)CC1(c2ccc(OCC3COc4ccc(Cl)cc4O3)cc2)COC1 10.1016/j.bmc.2018.10.019
145986689 166656 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 376 4 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4291766 166656 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 376 4 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2018.08.075
137634330 155834 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4066238 155834 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
90644294 111469 0 None 13 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288352 111469 0 None 13 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
66562287 138648 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C=C(C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3787463 138648 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C=C(C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
51350272 58533 0 None 107 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58533 0 None 107 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
134133343 153938 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3F)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3898066 153938 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3F)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990349 153938 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3F)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
118144982 169784 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4447353 169784 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
73777175 143377 0 None -17 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 357 3 1 2 4.9 O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 10.1021/acsmedchemlett.6b00360
CHEMBL3901994 143377 0 None -17 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 357 3 1 2 4.9 O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 10.1021/acsmedchemlett.6b00360
71562640 86095 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 386 8 1 4 2.9 CS(=O)(=O)CCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315253 86095 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 386 8 1 4 2.9 CS(=O)(=O)CCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
15659412 202252 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL6931 202252 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
90372458 141692 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884347 141692 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
51350273 58550 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688482 58550 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
137644843 157614 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 423 6 1 5 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4087365 157614 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 423 6 1 5 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)s2)c1 10.1021/acs.jmedchem.6b01357
58173000 118623 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427707 118623 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1016/j.bmc.2015.07.028
58218673 156983 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079930 156983 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
58218726 158592 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097951 158592 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
71613093 89555 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381297 89555 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
145951402 162291 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 494 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(C4CCCCC4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172853 162291 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 494 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(C4CCCCC4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
4987566 94222 2 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 333 7 2 3 4.6 O=C(O)c1cccc(NCc2cccc(OCc3ccccc3)c2)c1 10.1021/jm7012425
CHEMBL252527 94222 2 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 333 7 2 3 4.6 O=C(O)c1cccc(NCc2cccc(OCc3ccccc3)c2)c1 10.1021/jm7012425
137638317 156181 0 None -11 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 387 6 1 5 4.4 COc1cc(CCC(=O)O)ccc1-c1ccc2c(C)nn(-c3ccccn3)c2c1 10.1021/acs.jmedchem.7b00210
CHEMBL4070273 156181 0 None -11 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 387 6 1 5 4.4 COc1cc(CCC(=O)O)ccc1-c1ccc2c(C)nn(-c3ccccn3)c2c1 10.1021/acs.jmedchem.7b00210
131986250 163133 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204776 163133 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58173000 118623 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1021/ml500391n
CHEMBL3427707 118623 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1021/ml500391n
162675949 182716 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4797024 182716 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
54583098 61480 0 None 70 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
CHEMBL1773258 61480 0 None 70 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
58319094 86122 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 328 3 1 1 3.9 O=C(O)CCc1ccc(C#Cc2ccccc2Br)cc1 10.1021/jm301470a
CHEMBL2315548 86122 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 328 3 1 1 3.9 O=C(O)CCc1ccc(C#Cc2ccccc2Br)cc1 10.1021/jm301470a
127031001 138603 0 None 91 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.4 CC(C)=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786972 138603 0 None 91 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.4 CC(C)=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
54586011 61479 0 None 14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
CHEMBL1773257 61479 0 None 14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
145981771 166115 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.7 O=C(O)CCc1ccc(OCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4281714 166115 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.7 O=C(O)CCc1ccc(OCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
561372 58519 59 None 20 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1688452 58519 59 None 20 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
90372625 167160 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167160 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167160 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
57325841 73757 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022579 73757 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
121294461 181849 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 11 1 7 6.1 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C4(CC(=O)O)COC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4786019 181849 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 11 1 7 6.1 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C4(CC(=O)O)COC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
90644288 111463 0 None -20 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288346 111463 0 None -20 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
145994196 166841 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 354 9 1 4 3.8 O=C(O)COc1ccc(OCCCOc2cccc(Cl)c2)cc1F 10.1016/j.ejmech.2018.09.071
CHEMBL4295200 166841 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 354 9 1 4 3.8 O=C(O)COc1ccc(OCCCOc2cccc(Cl)c2)cc1F 10.1016/j.ejmech.2018.09.071
131986182 164069 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216026 164069 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
54582628 61826 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777863 61826 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
44589697 191015 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 354 7 1 1 5.5 C=C/C=C/c1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1/C=C/C=C 10.1021/jm8010178
CHEMBL519548 191015 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 354 7 1 1 5.5 C=C/C=C/c1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1/C=C/C=C 10.1021/jm8010178
127033821 138287 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3781162 138287 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
57521812 75914 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 410 7 1 2 5.7 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Br)cc2)cc1 10.1021/jm300215x
CHEMBL2058523 75914 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 410 7 1 2 5.7 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Br)cc2)cc1 10.1021/jm300215x
127027728 137311 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 467 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759913 137311 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 467 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
137642604 157971 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4091228 157971 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
131986162 164284 0 None -3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218822 164284 0 None -3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58230598 182537 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 182537 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
148173135 170585 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 393 8 2 3 5.7 CC(C)c1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4458669 170585 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 393 8 2 3 5.7 CC(C)c1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
137638995 156423 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4072885 156423 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
127046667 139407 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccn1 10.1016/j.ejmech.2016.03.054
CHEMBL3799646 139407 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccn1 10.1016/j.ejmech.2016.03.054
155565379 174993 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4579146 174993 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
25150015 184722 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm8010178
CHEMBL485935 184722 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm8010178
3367 1134 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/jm2005699
46216676 1134 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/jm2005699
CHEMBL604126 1134 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/jm2005699
1050 1871 86 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
11595431 1871 86 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
CHEMBL207881 1871 86 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
168291052 191322 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.4 Cc1ccc(OCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5200197 191322 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.4 Cc1ccc(OCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
54580626 61837 0 None 3 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777874 61837 0 None 3 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
131986065 163301 0 None -4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206579 163301 0 None -4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
46231841 200443 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 435 4 1 4 5.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2C(F)(F)F)S1 10.1016/j.bmcl.2009.10.052
CHEMBL609037 200443 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 435 4 1 4 5.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2C(F)(F)F)S1 10.1016/j.bmcl.2009.10.052
71615670 89573 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381315 89573 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
54582628 61826 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777863 61826 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
168289402 190717 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 408 7 1 4 5.8 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccsc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5191306 190717 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 408 7 1 4 5.8 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccsc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
137647107 157011 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4080336 157011 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
10266133 155627 3 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4063898 155627 3 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
11507535 158751 1 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 3 2 0 5.4 CC(C)C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4099626 158751 1 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 3 2 0 5.4 CC(C)C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
58172991 122161 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 330 9 1 4 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604042 122161 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 330 9 1 4 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmc.2015.07.028
146316684 170999 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4464769 170999 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
58319135 86119 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 4 1 1 3.7 CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315545 86119 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 4 1 1 3.7 CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
25150013 185665 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2cccc(C(F)(F)F)c2)cc1 10.1021/jm8010178
CHEMBL487365 185665 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2cccc(C(F)(F)F)c2)cc1 10.1021/jm8010178
54584098 61476 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/ml100106c
CHEMBL1773254 61476 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/ml100106c
127047533 139376 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 11 1 5 5.9 CCCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799443 139376 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 11 1 5 5.9 CCCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
137658391 159101 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
CHEMBL4103681 159101 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
25150117 186105 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2cccc(CO)c2)cc1 10.1021/jm8010178
CHEMBL488385 186105 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2cccc(CO)c2)cc1 10.1021/jm8010178
118645756 180880 3 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 180880 3 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
131986295 162990 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202907 162990 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986294 163289 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206445 163289 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
90644562 111314 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
CHEMBL3287576 111314 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
118129979 155253 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155253 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
131986116 163272 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206318 163272 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
51049992 145086 4 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3915620 145086 4 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
51049992 145086 4 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
60195125 3825 5 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3825 5 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3825 5 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
44409926 75630 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 485 7 2 4 6.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCC2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205433 75630 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 485 7 2 4 6.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCC2)cc1 10.1016/j.bmcl.2006.01.007
127045863 139450 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799898 139450 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
90644293 111468 0 None 13 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
CHEMBL3288351 111468 0 None 13 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
60195038 81380 0 None 912 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 363 7 2 2 5.4 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL2164239 81380 0 None 912 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 363 7 2 2 5.4 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
142738539 161769 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Br)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4164625 161769 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Br)cc2c1 10.1021/acsmedchemlett.7b00460
118645671 180347 0 None 5 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4758060 180347 0 None 5 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
162659599 180616 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4761101 180616 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
118645392 179529 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4748392 179529 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
51350407 58556 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm101405t
CHEMBL1688488 58556 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm101405t
45107323 122184 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 410 8 1 4 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(OC(F)(F)F)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604065 122184 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 410 8 1 4 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(OC(F)(F)F)cccc32)cc1 10.1016/j.bmc.2015.07.028
57705679 162957 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(F)cc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4202429 162957 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(F)cc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
57706280 164275 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 10 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4218710 164275 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 10 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
46231778 197800 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 4.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL591686 197800 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 4.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
145992623 166305 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 352 6 1 4 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4285582 166305 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 352 6 1 4 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmc.2018.10.019
134130352 141613 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 141613 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
118145020 170502 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4457184 170502 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
127046663 139245 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 439 10 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC2CC2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798609 139245 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 439 10 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC2CC2)c1 10.1016/j.ejmech.2016.03.054
57705863 80253 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 436 8 1 3 6.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151293 80253 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 436 8 1 3 6.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
57391957 69669 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 312 8 1 3 4.0 C=CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939639 69669 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 312 8 1 3 4.0 C=CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
137640781 156475 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 516 10 1 6 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Oc3ccccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4073421 156475 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 516 10 1 6 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Oc3ccccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
57325917 73760 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022582 73760 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
54586011 61479 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
CHEMBL1773257 61479 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
25150012 192849 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 275 3 1 2 3.0 N#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL526510 192849 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 275 3 1 2 3.0 N#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
168274068 189692 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 478 10 1 4 6.8 Cc1ccc(OCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5175750 189692 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 478 10 1 4 6.8 Cc1ccc(OCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
90644295 111470 0 None -3 2 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288353 111470 0 None -3 2 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
51349860 58520 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL1688453 58520 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
54757619 65002 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 286 3 1 3 2.5 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)n2)cc1 10.1021/jm2005699
CHEMBL1829151 65002 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 286 3 1 3 2.5 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)n2)cc1 10.1021/jm2005699
118642379 141587 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 141587 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
118719720 115163 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 532 12 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(Cl)c2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353741 115163 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 532 12 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(Cl)c2)c1 10.1016/j.bmc.2014.11.016
90357481 167055 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163916 167055 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301212 167055 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
137646368 157484 0 None -3 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 358 5 1 5 3.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
CHEMBL4085695 157484 0 None -3 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 358 5 1 5 3.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
134133297 143247 0 None -117 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 372 7 1 3 4.9 Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
CHEMBL3900990 143247 0 None -117 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 372 7 1 3 4.9 Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
46231434 198921 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 297 4 1 3 3.2 O=C1NC(=O)C(Cc2ccc(Cc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599270 198921 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 297 4 1 3 3.2 O=C1NC(=O)C(Cc2ccc(Cc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
54582629 61827 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 61827 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
71562421 86113 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1cccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315539 86113 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1cccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)c1 10.1021/jm301470a
145985123 165356 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 513 14 1 7 5.5 Cc1cc(OCCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
CHEMBL4250135 165356 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 513 14 1 7 5.5 Cc1cc(OCCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
57521810 75912 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(F)cc2)cc1 10.1021/jm300215x
CHEMBL2058521 75912 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(F)cc2)cc1 10.1021/jm300215x
11265145 86107 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 248 2 1 1 3.2 O=C(O)/C=C/c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315533 86107 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 248 2 1 1 3.2 O=C(O)/C=C/c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
145957539 161691 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4163496 161691 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
54580624 61823 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777860 61823 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
145954367 162015 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4168467 162015 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
71613095 89557 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381299 89557 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
75204485 155455 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4061819 155455 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
23111754 73700 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022245 73700 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
134144214 149825 0 None -354 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 384 8 1 3 5.7 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3953203 149825 0 None -354 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 384 8 1 3 5.7 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
54582630 61829 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 61829 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
71562637 86129 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2cccc(OC(F)(F)F)c2)cc1 10.1021/jm301470a
CHEMBL2315555 86129 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2cccc(OC(F)(F)F)c2)cc1 10.1021/jm301470a
25149901 186104 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
CHEMBL488384 186104 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
145974719 164144 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 482 10 1 5 5.4 Cc1cc(OCC(C)C)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4217180 164144 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 482 10 1 5 5.4 Cc1cc(OCC(C)C)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
54585512 61834 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777871 61834 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
57521919 75924 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL2058532 75924 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL4207911 75924 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1021/jm300215x
54757620 65003 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 282 4 1 4 1.9 COc1nccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
CHEMBL1829152 65003 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 282 4 1 4 1.9 COc1nccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
25149901 186104 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
CHEMBL488384 186104 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
46231488 197662 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cc(C)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL590699 197662 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cc(C)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
90644299 111474 0 None -5 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288357 111474 0 None -5 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
127029850 138209 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780211 138209 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
127047531 139191 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 10 1 5 5.5 CCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798213 139191 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 10 1 5 5.5 CCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
57325840 73756 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 460 10 1 4 5.8 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022578 73756 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 460 10 1 4 5.8 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
58218655 155624 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4063889 155624 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
145957072 161724 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc(F)c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4163958 161724 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc(F)c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
24825509 87518 0 None 29 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
CHEMBL234057 87518 0 None 29 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
145967558 164280 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 398 8 1 5 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4218763 164280 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 398 8 1 5 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
853224 94139 11 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94139 11 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
58172984 122157 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 398 9 1 4 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmc.2015.07.028
CHEMBL3604039 122157 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 398 9 1 4 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmc.2015.07.028
54581632 61821 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 388 6 2 3 4.5 O=C(O)C(Cc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1)C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777858 61821 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 388 6 2 3 4.5 O=C(O)C(Cc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1)C(=O)O 10.1016/j.bmcl.2011.03.114
146314522 180138 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 495 12 2 5 5.7 COc1ccc(CCC(C)(C)O)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4755717 180138 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 495 12 2 5 5.7 COc1ccc(CCC(C)(C)O)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
44571477 183360 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL481542 183360 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
70522117 86130 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 236 2 1 1 2.7 O=C(O)Cc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315556 86130 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 236 2 1 1 2.7 O=C(O)Cc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
44571477 183360 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL481542 183360 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
25098573 2706 5 None -8 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm300215x
5587 2706 5 None -8 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm300215x
CHEMBL463785 2706 5 None -8 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm300215x
58172978 122156 2 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 402 8 1 3 5.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1Cl 10.1016/j.bmc.2015.07.028
CHEMBL3604038 122156 2 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 402 8 1 3 5.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1Cl 10.1016/j.bmc.2015.07.028
145982071 165923 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3cc(Br)ccc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4278249 165923 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3cc(Br)ccc3O2)cc1F 10.1016/j.bmc.2018.10.019
54583581 61831 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777868 61831 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
12002185 75480 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048625 75480 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
1050 1871 86 None 1 3 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
11595431 1871 86 None 1 3 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
CHEMBL207881 1871 86 None 1 3 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
85970906 137253 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 389 6 1 4 4.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccccc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759467 137253 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 389 6 1 4 4.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccccc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
44591693 183653 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 419 6 1 2 5.8 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483546 183653 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 419 6 1 2 5.8 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
44591612 183942 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 421 6 1 3 5.4 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(O[C@H]2CC[C@@H](C)CC2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL484771 183942 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 421 6 1 3 5.4 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(O[C@H]2CC[C@@H](C)CC2)cc1 10.1016/j.bmcl.2009.03.082
44591719 184195 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 408 6 1 4 5.1 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1nc2ccccc2s1 10.1016/j.bmcl.2009.03.082
CHEMBL485131 184195 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 408 6 1 4 5.1 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1nc2ccccc2s1 10.1016/j.bmcl.2009.03.082
127038399 136234 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 338 6 1 5 4.1 CC(C)Nc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741045 136234 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 338 6 1 5 4.1 CC(C)Nc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
4671033 144829 8 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 339 5 1 3 4.6 Cc1ccc(S(=O)(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3913640 144829 8 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 339 5 1 3 4.6 Cc1ccc(S(=O)(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1021/acs.jmedchem.6b00685
127042700 136149 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccccc2C#N)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740222 136149 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccccc2C#N)nc(-c2ccccn2)n1 10.1039/C5MD00037H
100502467 142321 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 357 5 0 3 4.4 CN(c1ccc(Oc2ccccc2)cc1)S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3893258 142321 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 357 5 0 3 4.4 CN(c1ccc(Oc2ccccc2)cc1)S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
44591691 183629 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 349 4 1 3 4.2 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
CHEMBL483342 183629 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 349 4 1 3 4.2 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
44591613 183943 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 387 5 1 3 4.9 CCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL484772 183943 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 387 5 1 3 4.9 CCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
127040115 136133 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 401 7 0 5 4.7 Fc1ccc(OCc2cc(OCC3CCC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3740072 136133 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 401 7 0 5 4.7 Fc1ccc(OCc2cc(OCC3CCC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127042382 136053 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 5 0 5 3.3 COc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739442 136053 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 5 0 5 3.3 COc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042380 136118 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)cc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739963 136118 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)cc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
674995 142472 13 None -3 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 343 5 1 3 4.4 O=S(=O)(Nc1ccc(Oc2ccccc2)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3894632 142472 13 None -3 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 343 5 1 3 4.4 O=S(=O)(Nc1ccc(Oc2ccccc2)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
44591692 183652 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 405 5 1 2 5.4 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483545 183652 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 405 5 1 2 5.4 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
44591651 184121 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 373 4 1 3 4.5 CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485025 184121 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 373 4 1 3 4.5 CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
126961699 136157 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3740291 136157 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
127042378 136377 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)ccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3742333 136377 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)ccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127041066 136383 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 5 0 5 3.3 CN(C)c1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3742371 136383 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 5 0 5 3.3 CN(C)c1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
134134846 143707 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 337 3 0 3 4.2 O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3904654 143707 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 337 3 0 3 4.2 O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
127040434 136200 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccccc1OCc1cc(C)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740758 136200 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccccc1OCc1cc(C)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040748 136208 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1cccc(OCc2cc(C)nc(-c3ccccn3)n2)c1 10.1039/C5MD00037H
CHEMBL3740835 136208 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1cccc(OCc2cc(C)nc(-c3ccccn3)n2)c1 10.1039/C5MD00037H
134147328 149517 0 None -3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 394 4 0 4 4.4 N#CCc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3950610 149517 0 None -3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 394 4 0 4 4.4 N#CCc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
44591628 184106 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2cc(C)cc(C)c2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485006 184106 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2cc(C)cc(C)c2)cc1 10.1016/j.bmcl.2009.03.082
44244518 184328 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 5 1 3 4.8 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
CHEMBL485328 184328 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 5 1 3 4.8 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
25272661 184202 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 339 5 1 3 3.5 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485146 184202 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 339 5 1 3 3.5 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1016/j.bmcl.2009.03.082
44591690 183696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 343 4 1 2 4.1 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483937 183696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 343 4 1 2 4.1 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.082
67134965 150474 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 4 0 3 4.1 O=S1(=O)c2ccccc2CN1c1cc(F)cc(OCc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3958418 150474 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 4 0 3 4.1 O=S1(=O)c2ccccc2CN1c1cc(F)cc(OCc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
127038400 136353 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 400 5 0 5 4.4 CC1(C)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3742135 136353 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 400 5 0 5 4.4 CC1(C)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
5332902 136079 4 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 288 4 1 4 3.9 Cc1cc(N/N=C/c2ccccc2)nc(-c2ccccc2)n1 10.1039/C5MD00037H
CHEMBL3739652 136079 4 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 288 4 1 4 3.9 Cc1cc(N/N=C/c2ccccc2)nc(-c2ccccc2)n1 10.1039/C5MD00037H
127040096 136089 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739712 136089 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040433 136269 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccc(Cl)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741358 136269 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccc(Cl)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042383 136336 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 325 6 0 5 3.7 CCOc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741974 136336 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 325 6 0 5 3.7 CCOc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042701 136226 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2cccc(C#N)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740984 136226 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2cccc(C#N)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
134154953 150744 0 None -7 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3960369 150744 0 None -7 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
805130 94595 13 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 348 6 1 4 4.3 O=C(NCc1cccc(Oc2ccccc2)c1)c1ccc([N+](=O)[O-])cc1 10.1021/jm7012425
CHEMBL255074 94595 13 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 348 6 1 4 4.3 O=C(NCc1cccc(Oc2ccccc2)c1)c1ccc([N+](=O)[O-])cc1 10.1021/jm7012425
134138099 147289 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3932897 147289 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
44591630 190888 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 470 6 1 4 5.7 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL519358 190888 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 470 6 1 4 5.7 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.03.082
44591629 184107 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C)c(C)c2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485007 184107 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C)c(C)c2)cc1 10.1016/j.bmcl.2009.03.082
127040388 136233 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccccc2Cl)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741030 136233 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccccc2Cl)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040116 136274 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 403 7 0 6 3.6 Fc1ccc(OCc2cc(OCC3COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741385 136274 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 403 7 0 6 3.6 Fc1ccc(OCc2cc(OCC3COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127040723 136326 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 388 5 1 6 2.7 OC1CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3741899 136326 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 388 5 1 6 2.7 OC1CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
127042702 136307 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccc(C#N)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741704 136307 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccc(C#N)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
134141650 146166 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3923955 146166 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
134145778 148815 0 None -13 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 355 3 0 3 4.3 O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3945213 148815 0 None -13 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 355 3 0 3 4.3 O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
127040118 136066 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 442 8 0 7 3.8 N#CCC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
CHEMBL3739522 136066 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 442 8 0 7 3.8 N#CCC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
127039708 136140 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2cccc(Cl)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740168 136140 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2cccc(Cl)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040059 136158 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccccc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740298 136158 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccccc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042381 136176 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740515 136176 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042379 136217 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740906 136217 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127038708 136242 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741109 136242 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040094 136256 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2cccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741230 136256 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2cccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
44591652 190999 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 413 6 1 3 5.3 O=C(O)[C@@H]1c2ccccc2C(=O)N(CC2CC2)[C@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL519525 190999 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 413 6 1 3 5.3 O=C(O)[C@@H]1c2ccccc2C(=O)N(CC2CC2)[C@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
134153067 151724 0 None -16 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3969073 151724 0 None -16 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 10.1021/acs.jmedchem.6b00685
127038401 136261 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 414 5 0 6 3.5 Fc1ccc(OCc2cc(N3CC4(CCO4)C3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741297 136261 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 414 5 0 6 3.5 Fc1ccc(OCc2cc(N3CC4(CCO4)C3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127040095 136292 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741570 136292 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127039385 136294 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 433 8 0 7 3.3 COC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
CHEMBL3741582 136294 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 433 8 0 7 3.3 COC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
127040097 136330 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)cc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741919 136330 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)cc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
2233248 168297 9 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 334 5 1 4 4.6 O=C(Nc1ccccc1)c1cccc(Oc2ccc([N+](=O)[O-])cc2)c1 10.1021/jm7012425
CHEMBL438164 168297 9 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 334 5 1 4 4.6 O=C(Nc1ccccc1)c1cccc(Oc2ccc([N+](=O)[O-])cc2)c1 10.1021/jm7012425
134152545 152943 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3979588 152943 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
127041988 136311 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741735 136311 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
58137077 136090 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 348 5 0 6 3.0 c1ccc(OCc2cc(N3CCOCC3)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
CHEMBL3739715 136090 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 348 5 0 6 3.0 c1ccc(OCc2cc(N3CCOCC3)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
127040093 136161 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccc(F)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740314 136161 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccc(F)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042713 136324 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 6 1 5 3.7 CCNc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741858 136324 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 6 1 5 3.7 CCNc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127038402 136268 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 478 7 0 7 3.4 CC1(CS(C)(=O)=O)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3741353 136268 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 478 7 0 7 3.4 CC1(CS(C)(=O)=O)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
127038403 136267 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 415 6 0 5 4.5 Fc1ccc(OCc2cc(OCC(F)(F)F)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741349 136267 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 415 6 0 5 4.5 Fc1ccc(OCc2cc(OCC(F)(F)F)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127040117 136182 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 417 7 0 6 4.0 CC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
CHEMBL3740598 136182 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 417 7 0 6 4.0 CC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
127040432 136177 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 277 4 0 4 3.4 Cc1cc(COc2ccccc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740555 136177 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 277 4 0 4 3.4 Cc1cc(COc2ccccc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127039748 136203 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740771 136203 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040749 136060 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccc(OCc2cc(C)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
CHEMBL3739500 136060 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccc(OCc2cc(C)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
2843133 147114 45 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 307 6 1 2 4.0 CCCCc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3931570 147114 45 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 307 6 1 2 4.0 CCCCc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b00685
44591689 183695 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 4 1 2 4.8 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483936 183695 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 4 1 2 4.8 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
44591627 184339 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 415 7 1 3 5.0 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485335 184339 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 415 7 1 3 5.0 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
5280933 177646 59 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
Drug Central 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O None
CHEMBL464982 177646 59 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
Drug Central 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O None
1049 360 70 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
4618 360 70 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
5280934 360 70 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
CHEMBL8739 360 70 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
DB00132 360 70 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
1056 3319 111 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
2405 3319 111 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
77999 3319 111 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
CHEMBL121 3319 111 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
DB00412 3319 111 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
1052 2290 81 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
3323 2290 81 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
5280450 2290 81 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
CHEMBL267476 2290 81 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
DB14104 2290 81 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
1054 2872 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
3400 2872 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
445639 2872 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
CHEMBL8659 2872 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
1051 1427 56 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
4289 1427 56 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
445580 1427 56 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
57417355 1427 56 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
CHEMBL367149 1427 56 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
DB03756 1427 56 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
3893 2255 92 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
4642 2255 92 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
5534 2255 92 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
CHEMBL108766 2255 92 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
DB03017 2255 92 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
10043 3537 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
24749700 3537 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
CHEMBL4297635 3537 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
DB15447 3537 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
1055 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
1055 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
1055 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
135369651 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
135369651 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
135369651 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
985 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
985 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
985 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
CHEMBL82293 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
CHEMBL82293 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
CHEMBL82293 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
DB03796 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
DB03796 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
DB03796 2945 100 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
1054 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
1054 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
1054 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
3400 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
3400 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
3400 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
445639 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
445639 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
445639 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
CHEMBL8659 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
CHEMBL8659 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
CHEMBL8659 2872 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
11005 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
11005 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
11005 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
2806 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
2806 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
2806 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
CHEMBL111077 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
CHEMBL111077 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
CHEMBL111077 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
DB08231 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
DB08231 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
DB08231 2654 100 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
1052 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
1052 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
1052 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
3323 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
3323 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
3323 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
5280450 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
5280450 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
5280450 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
CHEMBL267476 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
CHEMBL267476 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
CHEMBL267476 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
DB14104 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
DB14104 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
DB14104 2290 81 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
1049 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
1049 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
1049 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
4618 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
4618 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
4618 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
5280934 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
5280934 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
5280934 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
CHEMBL8739 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
CHEMBL8739 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
CHEMBL8739 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
DB00132 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
DB00132 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
DB00132 360 70 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
1051 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
1051 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
4289 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
4289 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
445580 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
445580 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
57417355 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
57417355 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
CHEMBL367149 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
CHEMBL367149 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
DB03756 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
DB03756 1427 56 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
3367 1134 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 18477808
46216676 1134 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 18477808
CHEMBL604126 1134 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 18477808
24857286 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
24857286 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
24857286 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
24857286 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
6484 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
6484 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
6484 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
6484 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
CHEMBL1829174 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
CHEMBL1829174 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
CHEMBL1829174 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
CHEMBL1829174 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
DB12491 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
DB12491 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
DB12491 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
DB12491 1594 66 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
1050 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 16702987
11595431 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 16702987
CHEMBL207881 1871 86 None -1 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 16702987
25150014 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 18947221
3952 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 18947221
CHEMBL449588 3822 48 None 44 2 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 18947221
10668 1922 11 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 31971610
139600331 1922 11 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 31971610
CHEMBL5169614 1922 11 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 31971610
60195125 3825 5 None 4 3 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 22724451
9149 3825 5 None 4 3 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 22724451
CHEMBL2164242 3825 5 None 4 3 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 22724451
6483 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 23687558
66553168 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 23687558
CHEMBL2386353 3823 49 None 13 4 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 23687558
46854655 391 43 None -8 3 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 22859723
6485 391 43 None -8 3 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 22859723
CHEMBL1829173 391 43 None -8 3 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 22859723
1056 3319 111 None - 1 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
2405 3319 111 None - 1 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
77999 3319 111 None - 1 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
CHEMBL121 3319 111 None - 1 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
DB00412 3319 111 None - 1 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
1053 2447 0 None - 1 Human 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 15 2 2 5.9 OC(=O)CC(CCCCCCCCCCC(CC(=O)O)(C)C)(C)C 12565875
121871 2447 0 None - 1 Human 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 15 2 2 5.9 OC(=O)CC(CCCCCCCCCCC(CC(=O)O)(C)C)(C)C 12565875
CHEMBL63829 2447 0 None - 1 Human 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 15 2 2 5.9 OC(=O)CC(CCCCCCCCCCC(CC(=O)O)(C)C)(C)C 12565875
1057 1863 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 16702987
1057 1863 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 17200419
11692123 1863 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 16702987
11692123 1863 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 17200419
CHEMBL4303679 1863 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 16702987
CHEMBL4303679 1863 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 17200419


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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
162673875 182404 0 None - 1 Mouse 9.4 pEC50 = 9.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182404 0 None - 1 Mouse 9.4 pEC50 = 9.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
52936292 181528 23 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
67087100 182016 0 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182016 0 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182404 0 None - 1 Rat 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182404 0 None - 1 Rat 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
67087041 181789 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 181789 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087100 182016 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182016 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087095 182793 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 182793 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194465 182724 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 182724 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
134139282 145959 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(F)(F)F)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3922381 145959 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(F)(F)F)c2)cc1 10.1021/acsmedchemlett.6b00331
162668378 181925 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 181925 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
162674654 182873 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 182873 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
67087095 182793 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 182793 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145086 4 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087246 182295 4 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087041 181789 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 181789 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
52936292 181528 23 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
71257551 150060 18 None - 1 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3955132 150060 18 None - 1 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
162674654 182873 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 182873 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
162668378 181925 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 181925 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
68194465 182724 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 182724 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162668378 181925 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 181925 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
68194743 181966 9 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162674998 182809 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 182809 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183003 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183003 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087246 182295 4 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
162674998 182809 0 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 182809 0 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
162664735 181504 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 181504 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
134136015 143675 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 475 12 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3904378 143675 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 475 12 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
46854655 391 43 None - 1 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None - 1 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None - 1 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
67087095 182793 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 182793 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194743 181966 9 None - 1 Rat 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None - 1 Rat 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182404 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182404 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1594 66 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
6484 1594 66 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
CHEMBL1829174 1594 66 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
DB12491 1594 66 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
134134433 142701 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 510 12 1 5 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccncc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3896509 142701 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 510 12 1 5 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccncc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
134150797 151453 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 459 11 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3966739 151453 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 459 11 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
134137203 142307 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 523 12 1 5 5.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3893141 142307 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 523 12 1 5 5.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
162664735 181504 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 181504 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
68194159 182479 0 None - 1 Rat 7.0 pEC50 = 7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 182479 0 None - 1 Rat 7.0 pEC50 = 7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
67087160 181762 0 None - 1 Human 7.0 pEC50 = 7 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 181762 0 None - 1 Human 7.0 pEC50 = 7 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11961321 111307 3 None - 0 Human 5.0 pEC50 = 5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111307 3 None - 0 Human 5.0 pEC50 = 5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
127033514 138251 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 381 6 1 5 4.6 Cc1nc(-c2ccccc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3780725 138251 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 381 6 1 5 4.6 Cc1nc(-c2ccccc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
46854655 391 43 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
6485 391 43 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
CHEMBL1829173 391 43 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
156010524 176542 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4cccc(C)c4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633625 176542 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4cccc(C)c4)cn3c2)cc1 10.1016/j.bmc.2020.115574
57705838 110756 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 508 10 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](F)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL3265139 110756 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 508 10 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](F)C(C)(C)C)c1 10.1021/ml4005123
58379987 89878 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 547 7 1 4 7.6 COc1cc(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml300427u
CHEMBL2385464 89878 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 547 7 1 4 7.6 COc1cc(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml300427u
127033821 138287 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3781162 138287 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
90655860 110761 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265144 110761 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
91809187 146591 7 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 146591 7 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
67087160 181762 0 None - 1 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 181762 0 None - 1 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182232 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182232 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
46854655 391 43 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
67087246 182295 4 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
46941175 61483 20 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL1773261 61483 20 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
58230598 182537 0 None - 1 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 182537 0 None - 1 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
155530111 170927 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4463798 170927 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
127036748 136992 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754173 136992 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
127029850 138209 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3780211 138209 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
57707214 110758 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 534 12 1 4 8.2 CCO[C@@H](c1cc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)ccc1-c1cc(OC)ccc1F)C(C)(C)C 10.1021/ml4005123
CHEMBL3265141 110758 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 534 12 1 4 8.2 CCO[C@@H](c1cc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)ccc1-c1cc(OC)ccc1F)C(C)(C)C 10.1021/ml4005123
1056 3319 111 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
2405 3319 111 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
77999 3319 111 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
CHEMBL121 3319 111 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
DB00412 3319 111 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
134138359 147088 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 419 10 2 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CNCc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3931296 147088 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 419 10 2 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CNCc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
15604310 111309 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287571 111309 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
134155821 150394 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 463 12 2 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCO)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3957744 150394 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 463 12 2 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCO)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
24857286 1594 66 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
57705806 110726 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 515 10 1 4 7.6 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3264817 110726 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 515 10 1 4 7.6 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c(F)cn1 10.1021/ml4005123
162666840 181872 0 None - 1 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 181872 0 None - 1 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
132578495 182304 2 None - 1 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182304 2 None - 1 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
59132613 136738 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 483 8 1 4 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1nccs1 10.1016/j.bmcl.2015.11.050
CHEMBL3752026 136738 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 483 8 1 4 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1nccs1 10.1016/j.bmcl.2015.11.050
CHEMBL5092999 213625 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
IPOne assayIPOne assay
ChEMBL None None None COCCCS(=O)(=O)c1cc(C)c(-c2ccc(F)c3c2CC[C@H]3Oc2ccc3c(c2)OC[C@H]3CC(=O)O)c(C)c1 10.6019/CHEMBL5058643
156021111 177478 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4647211 177478 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
59590781 110764 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265147 110764 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
46854655 391 43 None - 1 Human 7.9 pEC50 = 7.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
6485 391 43 None - 1 Human 7.9 pEC50 = 7.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
CHEMBL1829173 391 43 None - 1 Human 7.9 pEC50 = 7.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
58758896 137027 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 480 8 1 4 6.3 Cn1ccnc1C(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754486 137027 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 480 8 1 4 6.3 Cn1ccnc1C(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
90176463 113762 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
CHEMBL3330549 113762 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
155523655 170336 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 357 7 1 5 3.8 Cc1nc(-c2ccccc2)oc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4454699 170336 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 357 7 1 5 3.8 Cc1nc(-c2ccccc2)oc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
134465785 175537 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 175537 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
73356502 89882 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 486 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H]4C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385471 89882 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 486 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H]4C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
91809187 146591 7 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 146591 7 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
60195125 3825 5 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
9149 3825 5 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL2164242 3825 5 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
134134768 143795 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 516 11 1 5 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCN(C)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3905435 143795 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 516 11 1 5 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCN(C)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
162644059 181242 0 None - 1 Rat 4.9 pEC50 = 4.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None - 1 Rat 4.9 pEC50 = 4.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
57706451 110760 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H](OC)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL3265143 110760 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H](OC)C(C)(C)C)c1 10.1021/ml4005123
71816761 89879 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H]3[C@@H](C(=O)O)[C@@H]3C4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385466 89879 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H]3[C@@H](C(=O)O)[C@@H]3C4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
57706220 110757 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL3265140 110757 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/ml4005123
155563228 174734 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 441 7 1 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4573403 174734 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 441 7 1 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
118129974 156652 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 156652 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
90655861 110762 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265145 110762 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
58380381 89884 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385473 89884 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
156017497 177282 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cccc(C)c4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4644239 177282 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cccc(C)c4)nc3c2)cc1 10.1016/j.bmc.2020.115574
46854655 391 43 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
6485 391 43 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL1829173 391 43 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
127029851 138333 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL3781779 138333 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
155547595 173093 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1ccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4534812 173093 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1ccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)cc1 10.1016/j.ejmech.2018.12.069
156013146 176893 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4OCC)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639050 176893 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4OCC)cn3c2)cc1 10.1016/j.bmc.2020.115574
162667620 181975 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 181975 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
134137248 142565 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 473 12 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3895442 142565 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 473 12 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
134138706 147365 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 551 11 1 6 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCS(=O)(=O)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3933446 147365 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 551 11 1 6 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCS(=O)(=O)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
58230552 181637 0 None - 1 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None - 1 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
57706778 80385 25 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2152070 80385 25 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
57706778 80385 25 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
CHEMBL2152070 80385 25 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
86288852 110766 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265149 110766 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
118151370 158557 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 158557 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
68194237 181624 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 181624 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182232 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182232 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194159 182479 0 None - 1 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 182479 0 None - 1 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
67087160 181762 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 181762 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
6483 3823 49 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
66553168 3823 49 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL2386353 3823 49 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
68265494 89881 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385470 89881 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
155525700 170473 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4456869 170473 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
46941175 61483 20 None - 1 Mouse 7.7 pEC50 = 7.7 Binding
Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretionActivation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61483 20 None - 1 Mouse 7.7 pEC50 = 7.7 Binding
Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretionActivation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
75204006 113761 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330548 113761 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
68676271 136790 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccncc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752557 136790 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccncc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
127035472 136851 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 482 8 1 3 7.6 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccs1 10.1016/j.bmcl.2015.11.050
CHEMBL3753088 136851 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 482 8 1 3 7.6 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccs1 10.1016/j.bmcl.2015.11.050
162649435 179460 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 288 6 1 2 3.7 Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4747554 179460 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 288 6 1 2 3.7 Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
67087173 181878 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 181878 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145086 4 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
134140466 146102 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3923431 146102 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
68194476 182305 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182305 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
162676686 182904 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 182904 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183003 0 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183003 0 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134129919 141875 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 515 12 1 5 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3889768 141875 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 515 12 1 5 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
46854655 391 43 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acsmedchemlett.6b00331
6485 391 43 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acsmedchemlett.6b00331
CHEMBL1829173 391 43 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acsmedchemlett.6b00331
67087100 182016 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182016 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
90176463 113762 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
CHEMBL3330549 113762 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
134137874 152448 0 None - 0 Rat 4.7 pEC50 = 4.7 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152448 0 None - 0 Rat 4.7 pEC50 = 4.7 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152448 0 None - 0 Rat 4.7 pEC50 = 4.7 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
162656082 180120 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 299 6 1 3 3.3 N#Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4755578 180120 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 299 6 1 3 3.3 N#Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
127037633 137041 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754659 137041 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
58379893 89875 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385461 89875 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@H]2CCCC2(C)C)c1 10.1021/ml300427u
71816808 89883 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@]4(C)C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385472 89883 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@]4(C)C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
118129979 155253 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155253 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
6483 3823 49 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3823 49 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3823 49 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
15603739 137046 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754682 137046 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
57705939 110759 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 532 10 1 4 7.9 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2OCCCC2(C)C)c1 10.1021/ml4005123
CHEMBL3265142 110759 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 532 10 1 4 7.9 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2OCCCC2(C)C)c1 10.1021/ml4005123
46854655 391 43 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmc.2016.09.004
6485 391 43 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmc.2016.09.004
CHEMBL1829173 391 43 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmc.2016.09.004
68194127 182613 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 182613 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
127035636 136751 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 490 9 1 6 4.7 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3S(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752168 136751 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 490 9 1 6 4.7 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3S(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2015.11.050
127036959 136894 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753362 136894 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
156017123 177169 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4OCC)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4642543 177169 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4OCC)nc3c2)cc1 10.1016/j.bmc.2020.115574
51049992 145086 4 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3915620 145086 4 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmc.2016.09.004
59590895 110767 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265150 110767 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
67072752 86102 0 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL2315528 86102 0 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
127036959 136894 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753362 136894 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
155561358 175081 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1cccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4581313 175081 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1cccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)c1 10.1016/j.ejmech.2018.12.069
90655863 110765 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265148 110765 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
67087173 181878 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 181878 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
57393692 69684 8 None - 0 Human 7.6 pEC50 = 7.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL1939654 69684 8 None - 0 Human 7.6 pEC50 = 7.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
58380220 110768 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265151 110768 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
155569735 176102 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 371 7 1 4 4.9 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4535460 176102 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 371 7 1 4 4.9 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4598257 176102 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 371 7 1 4 4.9 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
145965707 163651 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4210871 163651 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
162676686 182904 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 182904 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
6483 3823 49 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3823 49 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3823 49 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
24857286 1594 66 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
6484 1594 66 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
CHEMBL1829174 1594 66 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
DB12491 1594 66 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
1050 1871 86 None 1 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
11595431 1871 86 None 1 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
CHEMBL207881 1871 86 None 1 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
90655862 110763 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265146 110763 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
156635003 180354 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 394 3 2 3 3.9 Nc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
CHEMBL4758125 180354 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 394 3 2 3 3.9 Nc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
11961321 111307 3 None - 0 Crab-eating macaque 7.5 pEC50 = 7.5 Binding
Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111307 3 None - 0 Crab-eating macaque 7.5 pEC50 = 7.5 Binding
Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
134139990 145795 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)=O)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3921143 145795 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)=O)c2)cc1 10.1021/acsmedchemlett.6b00331
75204006 113761 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330548 113761 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
127035669 136793 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752601 136793 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
71257551 150060 18 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3955132 150060 18 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
162664735 181504 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 181504 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5075693 212619 2 None - 1 Human 8.5 pEC50 = 8.5 Binding
IPOne assayIPOne assay
ChEMBL None None None Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Oc1ccc2c(c1)OC[C@H]2CC(=O)O 10.6019/CHEMBL5058643
46854655 391 43 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
51357276 181425 0 None - 1 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None - 1 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087041 181789 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 181789 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162674654 182873 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 182873 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
134465794 170511 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 170511 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
68194237 181624 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 181624 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182232 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182232 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194465 182724 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 182724 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
118129999 157225 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157225 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
90655859 110727 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cncc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
CHEMBL3264818 110727 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cncc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
127036829 136783 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752487 136783 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
118129981 158920 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 158920 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
162645828 179083 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 352 6 1 2 4.2 O=C(O)CCc1ccc(COc2cc(F)ccc2Br)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4743323 179083 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 352 6 1 2 4.2 O=C(O)CCc1ccc(COc2cc(F)ccc2Br)cc1 10.1016/j.bmcl.2020.127650
162652317 179741 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 304 7 1 3 3.4 COc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4751137 179741 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 304 7 1 3 3.4 COc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
156013152 176904 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639182 176904 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
1050 1871 86 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.07.043
11595431 1871 86 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.07.043
CHEMBL207881 1871 86 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.07.043
58230552 181637 0 None - 1 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None - 1 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
132606864 157204 0 None - 1 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157204 0 None - 1 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
6483 3823 49 None - 1 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3823 49 None - 1 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3823 49 None - 1 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
9823501 99744 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 4 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL288341 99744 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 4 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4445519 99744 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 4 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
11961321 111307 3 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287569 111307 3 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
15603842 111308 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287570 111308 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
11961321 111307 3 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111307 3 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
132606863 157281 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157281 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
68674201 136765 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 476 8 1 2 7.6 O=C(O)CC(c1ccccc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752303 136765 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 476 8 1 2 7.6 O=C(O)CC(c1ccccc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
127035471 136966 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1ccccn1 10.1016/j.bmcl.2015.11.050
CHEMBL3753980 136966 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1ccccn1 10.1016/j.bmcl.2015.11.050
57522038 3824 54 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmcl.2020.127650
6490 3824 54 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmcl.2020.127650
CHEMBL2058533 3824 54 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmcl.2020.127650
58230552 181637 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
67361692 89867 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 540 7 1 3 8.4 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385303 89867 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 540 7 1 3 8.4 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
24857286 1594 66 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
90644561 111306 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 418 7 1 2 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3C)c2)cc1 10.1021/ml400501x
CHEMBL3287568 111306 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 418 7 1 2 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3C)c2)cc1 10.1021/ml400501x
24897670 111312 19 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
CHEMBL3287574 111312 19 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
162667620 181975 0 None - 1 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 181975 0 None - 1 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
127036828 136912 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753533 136912 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
90158812 113760 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
CHEMBL3330547 113760 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
57706032 110755 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 460 10 1 3 7.6 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265138 110755 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 460 10 1 3 7.6 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
145965467 163614 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4210415 163614 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
90655858 110754 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)n3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265137 110754 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)n3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
155512244 169062 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 373 7 1 5 4.3 Cc1nc(-c2ccccc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4436948 169062 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 373 7 1 5 4.3 Cc1nc(-c2ccccc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
70901463 89880 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385467 89880 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
134136203 142439 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 433 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(C)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3894356 142439 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 433 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(C)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
162644059 181242 0 None - 1 Mouse 5.4 pEC50 = 5.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None - 1 Mouse 5.4 pEC50 = 5.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
156020437 177574 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4648853 177574 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
67072752 86102 0 None - 1 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse FFA1Agonist activity at mouse FFA1
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315528 86102 0 None - 1 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse FFA1Agonist activity at mouse FFA1
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
89671280 146155 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmc.2017.03.001
CHEMBL3923877 146155 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmc.2017.03.001
68194476 182305 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182305 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
134140675 146246 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 509 12 1 4 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccccc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3924534 146246 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 509 12 1 4 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccccc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
162676686 182904 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 182904 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087173 181878 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 181878 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134147518 149584 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 487 11 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3951157 149584 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 487 11 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
59132740 136845 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccnc1 10.1016/j.bmcl.2015.11.050
CHEMBL3753057 136845 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccnc1 10.1016/j.bmcl.2015.11.050
15602772 111311 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
CHEMBL3287573 111311 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
127035638 136944 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753790 136944 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
156010854 176545 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C5CCCCC5)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633642 176545 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C5CCCCC5)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
162666840 181872 0 None - 1 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 181872 0 None - 1 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
127036828 136912 0 None - 0 Human 4.4 pEC50 = 4.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753533 136912 0 None - 0 Human 4.4 pEC50 = 4.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
127035667 136762 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752274 136762 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
127037608 136874 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753265 136874 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
127036747 137044 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754670 137044 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
118129979 155253 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155253 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
24857286 1594 66 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
6484 1594 66 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
CHEMBL1829174 1594 66 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
DB12491 1594 66 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
156016183 177094 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4641652 177094 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
156013404 176885 2 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4638956 176885 2 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
127035668 136815 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752807 136815 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
837245 10499 41 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 315 3 1 2 3.8 Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
CHEMBL1170012 10499 41 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 315 3 1 2 3.8 Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
156019672 177416 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(CC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4646212 177416 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(CC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
52936292 181528 23 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
51357276 181425 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162667620 181975 0 None - 1 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 181975 0 None - 1 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
44223813 89887 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.8 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H](CC(=O)O)CC4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385476 89887 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.8 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H](CC(=O)O)CC4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
156013456 176901 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639121 176901 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
156019224 177397 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4645989 177397 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
67359903 89885 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385474 89885 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
68194159 182479 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 182479 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
156012263 176720 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4636540 176720 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
24857286 1594 66 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
6484 1594 66 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
CHEMBL1829174 1594 66 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
DB12491 1594 66 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
3367 1134 1 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
46216676 1134 1 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
CHEMBL604126 1134 1 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
58230598 182537 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 182537 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
132578495 182304 2 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182304 2 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
561372 58519 59 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL1688452 58519 59 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
156014759 176678 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(F)(F)F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4635975 176678 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(F)(F)F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
156011495 176780 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C5CCCCC5)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4637557 176780 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C5CCCCC5)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
51357276 181425 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
90158812 113760 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
CHEMBL3330547 113760 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
127035667 136762 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752274 136762 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
118129998 156781 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 156781 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
162673626 182611 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 350 3 2 3 3.7 Nc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
CHEMBL4795755 182611 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 350 3 2 3 3.7 Nc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
90644562 111314 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
CHEMBL3287576 111314 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
68194237 181624 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 181624 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
127035669 136793 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752601 136793 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
156013517 176936 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639658 176936 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
127037633 137041 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754659 137041 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
155569722 175684 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 353 7 1 4 4.7 Cc1nc(-c2ccccc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4528449 175684 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 353 7 1 4 4.7 Cc1nc(-c2ccccc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4594952 175684 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 353 7 1 4 4.7 Cc1nc(-c2ccccc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
73891117 113764 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330550 113764 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
132578495 182304 2 None - 1 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182304 2 None - 1 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
46854655 391 43 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300427u
6485 391 43 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300427u
CHEMBL1829173 391 43 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300427u
162644059 181242 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
15603739 137046 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754682 137046 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
67072752 86102 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL2315528 86102 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
127036748 136992 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754173 136992 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
156019823 177365 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(C)C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4645557 177365 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(C)C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
156016011 177033 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4640818 177033 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
68194476 182305 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182305 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
137633536 155754 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
Agonist activity at mouse FFA1 receptorAgonist activity at mouse FFA1 receptor
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 Mouse 5.2 pEC50 = 5.2 Binding
Agonist activity at mouse FFA1 receptorAgonist activity at mouse FFA1 receptor
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
156010092 176533 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633473 176533 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
156019930 177388 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cc(F)ccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4645938 177388 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cc(F)ccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
11961321 111307 3 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Agonist activity at rat GPR40 in presence of 0.01% human serum albuminAgonist activity at rat GPR40 in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111307 3 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Agonist activity at rat GPR40 in presence of 0.01% human serum albuminAgonist activity at rat GPR40 in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
73891117 113764 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330550 113764 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
23083113 176878 6 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 306 6 1 2 4.4 O=C(O)CCc1ccc(OCc2cccc3ccccc23)cc1 10.1016/j.bmc.2019.115263
CHEMBL4638816 176878 6 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 306 6 1 2 4.4 O=C(O)CCc1ccc(OCc2cccc3ccccc23)cc1 10.1016/j.bmc.2019.115263
15603947 111310 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 502 8 1 7 5.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncnn2C)cc1 10.1021/ml400501x
CHEMBL3287572 111310 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 502 8 1 7 5.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncnn2C)cc1 10.1021/ml400501x
127035668 136815 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752807 136815 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
118129999 157225 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157225 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
25150014 3822 48 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
3952 3822 48 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
CHEMBL449588 3822 48 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
156017576 177265 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(CC)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4644067 177265 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(CC)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
156021586 177506 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(F)(F)F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4647663 177506 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(F)(F)F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
162674533 182883 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 372 3 2 3 4.4 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4799103 182883 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 372 3 2 3 4.4 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
57706227 110724 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 10 1 4 7.7 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3264815 110724 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 10 1 4 7.7 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
155565451 175022 7 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL4579901 175022 7 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.ejmech.2018.12.069
118129981 158920 0 None - 1 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 158920 0 None - 1 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
162666840 181872 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 181872 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
118129998 156781 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 156781 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
15604434 111313 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncco2)cc1 10.1021/ml400501x
CHEMBL3287575 111313 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncco2)cc1 10.1021/ml400501x
127036829 136783 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752487 136783 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
67072752 86102 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL2315528 86102 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
127035637 136731 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 437 8 1 5 5.1 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3C#N)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3751968 136731 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 437 8 1 5 5.1 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3C#N)c2)cc1 10.1016/j.bmcl.2015.11.050
134139119 145453 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 511 12 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)CC)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3918387 145453 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 511 12 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)CC)c2)cc1 10.1021/acsmedchemlett.6b00331
71257551 150060 18 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3955132 150060 18 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
68194127 182613 0 None - 1 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 182613 0 None - 1 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
134142245 144967 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 503 11 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCOCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3914686 144967 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 503 11 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCOCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
134142149 144935 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 519 11 1 5 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCSCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3914418 144935 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 519 11 1 5 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCSCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
68194743 181966 9 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
156016727 177144 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4642297 177144 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
156016929 177151 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Modulation of GPR40 (unknown origin)Modulation of GPR40 (unknown origin)
ChEMBL 540 7 1 7 5.3 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)C(C)C2)c(Cl)cn1 10.1016/j.bmc.2019.115263
CHEMBL4642324 177151 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Modulation of GPR40 (unknown origin)Modulation of GPR40 (unknown origin)
ChEMBL 540 7 1 7 5.3 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)C(C)C2)c(Cl)cn1 10.1016/j.bmc.2019.115263
15603946 111167 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
CHEMBL3286409 111167 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
58230598 182537 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 182537 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
23136411 58524 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2019.115263
CHEMBL1688457 58524 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2019.115263
127035639 137030 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1cccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754524 137030 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1cccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)c1 10.1016/j.bmcl.2015.11.050
57705880 110725 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml4005123
CHEMBL3264816 110725 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml4005123
71575419 89541 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381282 89541 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
8852666 192081 21 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of GPR40 (unknown origin)Positive allosteric modulation of GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
CHEMBL5219102 192081 21 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of GPR40 (unknown origin)Positive allosteric modulation of GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
156011880 176756 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4637214 176756 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
127034370 138312 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3781477 138312 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
57705648 89886 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 474 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385475 89886 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 474 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
156016232 177198 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4642960 177198 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
3893 2255 92 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
4642 2255 92 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
5534 2255 92 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL108766 2255 92 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
DB03017 2255 92 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
156009878 176550 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 281 6 1 3 3.2 N#Cc1ccccc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmc.2019.115263
CHEMBL4633698 176550 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 281 6 1 3 3.2 N#Cc1ccccc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmc.2019.115263
162676881 183003 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183003 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1594 66 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
134143418 144800 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 477 13 1 5 5.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCOC)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3913383 144800 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 477 13 1 5 5.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCOC)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
134137874 152448 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152448 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152448 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
51049992 145086 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
46854655 391 43 None - 1 Human 7.1 pEC50 = 7.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
6485 391 43 None - 1 Human 7.1 pEC50 = 7.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
CHEMBL1829173 391 43 None - 1 Human 7.1 pEC50 = 7.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
45254027 89874 6 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385460 89874 6 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
58380284 89872 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(C4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385459 89872 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(C4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
156021515 177564 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4648621 177564 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
68194127 182613 0 None - 1 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 182613 0 None - 1 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57706902 110722 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 490 10 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2CC(C)(C)C)c1 10.1021/ml4005123
CHEMBL3264813 110722 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 490 10 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2CC(C)(C)C)c1 10.1021/ml4005123
46854655 391 43 None - 1 Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
6485 391 43 None - 1 Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
CHEMBL1829173 391 43 None - 1 Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
127037608 136874 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753265 136874 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
162674998 182809 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 182809 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1594 66 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
6484 1594 66 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL1829174 1594 66 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
DB12491 1594 66 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
58380255 89876 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 528 7 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385462 89876 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 528 7 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
57707110 110723 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 535 10 1 4 7.9 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3264814 110723 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 535 10 1 4 7.9 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
24857286 1594 66 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
6484 1594 66 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
CHEMBL1829174 1594 66 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
DB12491 1594 66 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
127033818 138218 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL3780334 138218 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
118129974 156652 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 156652 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
127036960 136864 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753188 136864 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
156009978 176524 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633252 176524 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
58379717 89877 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 546 7 1 3 8.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385463 89877 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 546 7 1 3 8.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
118151370 158557 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 158557 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
127036960 136864 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753188 136864 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
54580627 61838 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777875 61838 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
53248846 61824 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 61824 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
54582629 61827 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 61827 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
54584572 61841 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777878 61841 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
53248848 61839 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 61839 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
127040096 136089 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739712 136089 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
54586485 61828 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777865 61828 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
54586484 61825 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 61825 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
54583582 61835 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777872 61835 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
54584571 61840 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777877 61840 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
54583581 61831 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777868 61831 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
54582630 61829 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 61829 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
127041988 136311 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741735 136311 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
54580625 61836 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777873 61836 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
54581633 61832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777869 61832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
54580626 61837 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777874 61837 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
54582628 61826 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777863 61826 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
54580624 61823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777860 61823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
54586486 61833 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777870 61833 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
54582631 61830 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777867 61830 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
54585512 61834 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777871 61834 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
53248847 61818 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 61818 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
126961699 136157 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3740291 136157 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
16661950 137141 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 415 10 1 6 4.2 CCOC(=O)CCCCCOc1ccc2cc(CC3SC(=O)NC3=O)ccc2c1 10.1016/j.ejmech.2015.12.049
CHEMBL3758511 137141 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 415 10 1 6 4.2 CCOC(=O)CCCCCOc1ccc2cc(CC3SC(=O)NC3=O)ccc2c1 10.1016/j.ejmech.2015.12.049
16058685 171991 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.ejmech.2015.12.049
CHEMBL448569 171991 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.ejmech.2015.12.049
46854655 391 43 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
24857286 1594 66 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
6484 1594 66 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
CHEMBL1829174 1594 66 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
DB12491 1594 66 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
52936292 181528 23 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
67087246 182295 4 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145086 4 None - 1 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None - 1 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194743 181966 9 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162644059 181242 0 None - 1 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None - 1 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
127051856 140196 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL3817889 140196 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
24857286 1594 66 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
57706778 80385 25 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
CHEMBL2152070 80385 25 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
58230552 181637 0 None - 1 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None - 1 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
127051856 140196 0 None - 1 Human 8.1 pKd = 8.1 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL3817889 140196 0 None - 1 Human 8.1 pKd = 8.1 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
51357276 181425 0 None - 1 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None - 1 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162668378 181925 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 181925 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182404 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182404 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
67087095 182793 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 182793 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162674654 182873 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 182873 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
67085761 156483 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4073525 156483 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57413290 75473 0 None 2 2 Rat 8.0 pKi = 8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048617 75473 0 None 2 2 Rat 8.0 pKi = 8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
23111682 73754 0 None -5 2 Rat 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022576 73754 0 None -5 2 Rat 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
68194159 182479 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 182479 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
23083015 75467 0 None -19 2 Rat 5.0 pKi = 5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
CHEMBL2048611 75467 0 None -19 2 Rat 5.0 pKi = 5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
118129998 156781 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 156781 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
57414677 75273 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047164 75273 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
51357276 181425 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 181425 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11271473 74123 0 None -2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022584 74123 0 None -2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2027975 74123 0 None -2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
57414402 75262 0 None -4 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047152 75262 0 None -4 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857375 75278 0 None -5 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047169 75278 0 None -5 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111781 73702 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022247 73702 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23111781 73702 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022247 73702 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
57414543 75271 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
CHEMBL2047162 75271 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
24857376 75279 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047170 75279 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57413373 75474 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048618 75474 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
57413375 76866 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2048620 76866 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2079468 76866 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
57414679 75275 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
CHEMBL2047166 75275 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
57413287 75468 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
CHEMBL2048612 75468 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
68194449 182232 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182232 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57325674 73704 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022249 73704 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
58218673 156983 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079930 156983 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
162667620 181975 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 181975 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
23111693 73710 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
CHEMBL2022255 73710 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
23111766 73713 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022258 73713 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
68194127 182613 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 182613 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
58218740 155904 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4067052 155904 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
58218551 158501 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4096887 158501 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
561372 58519 59 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL1688452 58519 59 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
67087173 181878 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 181878 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
6484 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
CHEMBL1829174 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
DB12491 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
24857286 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
6484 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
CHEMBL1829174 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
DB12491 1594 66 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
91809187 146591 7 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 146591 7 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
57414676 75272 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047163 75272 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
11190525 75472 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048616 75472 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11226058 75477 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048622 75477 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
57413289 75471 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048615 75471 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11203294 75478 2 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048623 75478 2 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
162676686 182904 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 182904 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
11203294 75478 2 None -2 2 Human 7.8 pKi = 7.8 Binding
FFAR1 binding assayFFAR1 binding assay
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 75478 2 None -2 2 Human 7.8 pKi = 7.8 Binding
FFAR1 binding assayFFAR1 binding assay
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
23111693 73710 0 None -12 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
CHEMBL2022255 73710 0 None -12 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
23111689 73712 0 None -27 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022257 73712 0 None -27 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
71457285 82245 18 None -4 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2179472 82245 18 None -4 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
23111781 73702 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022247 73702 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23111694 73711 0 None -24 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
CHEMBL2022256 73711 0 None -24 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
57414405 75265 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047155 75265 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857285 75267 0 None -7 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047157 75267 0 None -7 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414539 75268 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047158 75268 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57414540 75270 0 None -5 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047160 75270 0 None -5 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111781 73702 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022247 73702 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
23111682 73754 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022576 73754 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23642299 75277 0 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047168 75277 0 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
12002202 75481 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048626 75481 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
23157282 76867 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048628 76867 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2079469 76867 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
58218694 157925 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4090766 157925 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137653896 157999 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
CHEMBL4091552 157999 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
24857375 75278 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047169 75278 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
11398822 75479 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048624 75479 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
12002201 75482 1 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048627 75482 1 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
57414676 75272 0 None -12 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047163 75272 0 None -12 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
46854655 391 43 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 391 43 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 391 43 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
162664735 181504 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 181504 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
67087100 182016 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182016 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11236925 75475 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048619 75475 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
12002185 75480 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048625 75480 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
68194476 182305 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182305 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
23111734 73755 0 None -7 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022577 73755 0 None -7 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
23642299 75277 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047168 75277 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
58230598 182537 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 182537 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
67072752 86102 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL2315528 86102 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
57414401 75261 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047151 75261 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
11489259 75476 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048621 75476 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
23111668 73698 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022243 73698 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
57414404 75264 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047154 75264 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
23111668 73698 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022243 73698 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
57325916 73759 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022581 73759 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
1050 1871 86 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
11595431 1871 86 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
CHEMBL207881 1871 86 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
57414403 75263 0 None -8 2 Rat 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047153 75263 0 None -8 2 Rat 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
57414267 75259 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047149 75259 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57413290 75473 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048617 75473 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL5075693 212619 2 None - 1 Human 7.6 pKi = 7.6 Binding
FFAR1 biochemical assayFFAR1 biochemical assay
ChEMBL None None None Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Oc1ccc2c(c1)OC[C@H]2CC(=O)O 10.6019/CHEMBL5058643
137649008 156604 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2CCC[C@@]2(C)CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4075190 156604 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2CCC[C@@]2(C)CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
24857285 75267 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047157 75267 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414267 75259 0 None -10 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047149 75259 0 None -10 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
23111754 73700 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022245 73700 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
23111754 73700 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022245 73700 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
57414402 75262 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047152 75262 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57413288 75470 0 None -4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048614 75470 0 None -4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
71257551 150060 18 None - 1 Human 7.6 pKi = 7.6 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3955132 150060 18 None - 1 Human 7.6 pKi = 7.6 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
11674915 58554 1 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL1688486 58554 1 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11327107 73703 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
CHEMBL2022248 73703 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
57325841 73757 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022579 73757 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
57414403 75263 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047153 75263 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
57414680 75276 0 None -8 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047167 75276 0 None -8 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
11327107 73703 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
CHEMBL2022248 73703 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
24857286 1594 66 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
6484 1594 66 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL1829174 1594 66 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
DB12491 1594 66 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
57325842 73758 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022580 73758 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
57414268 75260 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047150 75260 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
67087160 181762 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 181762 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
23111666 73708 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
CHEMBL2022253 73708 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
67087041 181789 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 181789 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194465 182724 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 182724 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
23083189 75466 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
CHEMBL2048610 75466 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
57414538 75266 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047156 75266 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
23111734 73755 0 None -7 2 Rat 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2022577 73755 0 None -7 2 Rat 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57414540 75270 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047160 75270 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414680 75276 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047167 75276 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
137638269 156334 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4071899 156334 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218640 158376 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4095599 158376 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
132578495 182304 2 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182304 2 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
118129999 157225 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157225 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
51350138 58541 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
CHEMBL1688473 58541 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
23111734 73755 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022577 73755 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
23111734 73755 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2022577 73755 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
51350138 58541 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL1688473 58541 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
51350138 58541 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
CHEMBL1688473 58541 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
57414679 75275 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
CHEMBL2047166 75275 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
58218651 157774 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4089171 157774 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
118129979 155253 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155253 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
23111766 73713 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022258 73713 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
57414405 75265 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047155 75265 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
51350138 58541 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL1688473 58541 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
58218607 155399 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4061093 155399 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57414543 75271 0 None -30 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
CHEMBL2047162 75271 0 None -30 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
118129981 158920 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 158920 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
57414539 75268 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047158 75268 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
71457285 82245 18 None 4 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2179472 82245 18 None 4 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
23111704 73699 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022244 73699 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
23111704 73699 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022244 73699 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
24857286 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
6484 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
CHEMBL1829174 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
DB12491 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
24857286 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
6484 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
CHEMBL1829174 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
DB12491 1594 66 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
51031010 156090 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4069191 156090 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
57325917 73760 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022582 73760 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
162674998 182809 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 182809 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183003 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183003 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11226058 75477 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048622 75477 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
60195125 3825 5 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
9149 3825 5 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL2164242 3825 5 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
57413373 75474 0 None 2 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048618 75474 0 None 2 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
12002185 75480 0 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048625 75480 0 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
12002201 75482 1 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048627 75482 1 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
67087246 182295 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182295 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145086 4 None - 1 Human 8.3 pKi = 8.3 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3915620 145086 4 None - 1 Human 8.3 pKi = 8.3 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
51049992 145086 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145086 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
52936292 181528 23 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 181528 23 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57414678 75274 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
CHEMBL2047165 75274 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
57414678 75274 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
CHEMBL2047165 75274 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
23111791 73707 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022252 73707 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
46854655 391 43 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
6485 391 43 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL1829173 391 43 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
162666840 181872 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 181872 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
11271473 74123 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022584 74123 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2027975 74123 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
58218638 156894 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4078852 156894 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
132606864 157204 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157204 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
11674915 58554 1 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL1688486 58554 1 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
23082877 75469 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
CHEMBL2048613 75469 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
23111791 73707 0 None -11 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022252 73707 0 None -11 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
137636358 155345 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4060499 155345 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
12002202 75481 0 None 3 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048626 75481 0 None 3 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
57413289 75471 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048615 75471 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
46941175 61483 20 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL1773261 61483 20 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
57414538 75266 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047156 75266 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
23111668 73698 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022243 73698 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
23083015 75467 0 None 19 2 Human 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
CHEMBL2048611 75467 0 None 19 2 Human 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
23111668 73698 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022243 73698 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
51350138 58541 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
CHEMBL1688473 58541 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
51350138 58541 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
CHEMBL1688473 58541 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
57414677 75273 0 None -5 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047164 75273 0 None -5 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111689 73712 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022257 73712 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
23111671 73709 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
CHEMBL2022254 73709 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
23083189 75466 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
CHEMBL2048610 75466 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
23111704 73699 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022244 73699 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
24857376 75279 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047170 75279 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111704 73699 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022244 73699 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
68194237 181624 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 181624 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57413288 75470 0 None 4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048614 75470 0 None 4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
23157282 76867 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048628 76867 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2079469 76867 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
11203294 75478 2 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048623 75478 2 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
11190525 75472 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048616 75472 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11236925 75475 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048619 75475 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
57413375 76866 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2048620 76866 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2079468 76866 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
23111694 73711 0 None 24 2 Human 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
CHEMBL2022256 73711 0 None 24 2 Human 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
58218709 157872 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
CHEMBL4090240 157872 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
118151370 158557 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 158557 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
118129974 156652 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 156652 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
25150014 3822 48 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
3952 3822 48 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
CHEMBL449588 3822 48 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
58218542 156225 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070703 156225 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
57414542 76863 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047161 76863 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2079433 76863 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57325917 73760 0 None 5 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022582 73760 0 None 5 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
58230552 181637 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 181637 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
3367 1134 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
46216676 1134 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
CHEMBL604126 1134 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
24857286 1594 66 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1594 66 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1594 66 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1594 66 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
58218608 156143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4069764 156143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57414268 75260 0 None -26 2 Rat 5.1 pKi = 5.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047150 75260 0 None -26 2 Rat 5.1 pKi = 5.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
162644059 181242 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181242 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
137661294 158953 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101901 158953 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
11398822 75479 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048624 75479 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
68194743 181966 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 181966 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57414542 76863 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047161 76863 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2079433 76863 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414404 75264 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047154 75264 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
57414401 75261 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047151 75261 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
6483 3823 49 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
66553168 3823 49 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL2386353 3823 49 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
23082877 75469 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
CHEMBL2048613 75469 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
58218630 159108 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103729 159108 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
11489259 75476 0 None 2 2 Rat 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048621 75476 0 None 2 2 Rat 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
58218655 155624 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4063889 155624 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
57413287 75468 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
CHEMBL2048612 75468 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
137076846 1094 0 None - 1 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 16 3 9 4.7 OC(=O)CCc1ccc(cc1F)OCc1cccc(c1)c1ccc(cc1C)OCCOCCNc1ccc(c2=NCN=c12)N(O)[O] 27074625
9148 1094 0 None - 1 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 16 3 9 4.7 OC(=O)CCc1ccc(cc1F)OCc1cccc(c1)c1ccc(cc1C)OCCOCCNc1ccc(c2=NCN=c12)N(O)[O] 27074625