Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
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 DOI
164616580 185433 None 0 Human Functional pEC50 = 10.4 10.4 - 1
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 185433 None 0 Human Functional pEC50 = 10.4 10.4 - 1
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 180358 None 0 Human Functional pEC50 = 10 10.0 - 1
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 180358 None 0 Human Functional pEC50 = 10 10.0 - 1
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 174071 None 0 Human Functional pEC50 = 10.0 10.0 -15 2
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 174071 None 0 Human Functional pEC50 = 10.0 10.0 -15 2
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 171578 None 0 Human Functional pEC50 = 9.7 9.7 -1 2
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 171578 None 0 Human Functional pEC50 = 9.7 9.7 -1 2
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 185115 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 185115 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 171181 None 0 Human Functional pEC50 = 9.6 9.6 -4 2
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 171181 None 0 Human Functional pEC50 = 9.6 9.6 -4 2
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 149347 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 149347 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 174071 None 0 Rat Functional pEC50 = 9.5 9.5 15 2
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 174071 None 0 Rat Functional pEC50 = 9.5 9.5 15 2
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 171181 None 0 Rat Functional pEC50 = 9.5 9.5 4 2
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 171181 None 0 Rat Functional pEC50 = 9.5 9.5 4 2
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 1624 None 46 Human Functional pEC50 = 9.5 9.5 -3 3
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 1624 None 46 Human Functional pEC50 = 9.5 9.5 -3 3
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 1624 None 46 Human Functional pEC50 = 9.5 9.5 -3 3
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 1624 None 46 Human Functional pEC50 = 9.5 9.5 -3 3
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 184712 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 184712 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 146776 None 0 Rat Functional pEC50 = 9.4 9.4 10 2
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 146776 None 0 Rat Functional pEC50 = 9.4 9.4 10 2
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 171578 None 0 Rat Functional pEC50 = 9.4 9.4 1 2
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 171578 None 0 Rat Functional pEC50 = 9.4 9.4 1 2
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 185417 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 185417 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 184626 None 0 Human Functional pEC50 = 9.4 9.4 42 2
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 184626 None 0 Human Functional pEC50 = 9.4 9.4 42 2
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 167709 None 5 Rat Functional pEC50 = 9.3 9.3 10 2
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 167709 None 5 Rat Functional pEC50 = 9.3 9.3 10 2
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 167709 None 5 Rat Functional pEC50 = 9.3 9.3 10 2
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 111317 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 111317 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 182216 None 24 Human Functional pEC50 = 9.2 9.2 -7 3
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 182216 None 24 Human Functional pEC50 = 9.2 9.2 -7 3
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 186255 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 186255 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 185303 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 185303 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 167709 None 5 Human Functional pEC50 = 9.1 9.1 -10 2
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 167709 None 5 Human Functional pEC50 = 9.1 9.1 -10 2
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 167709 None 5 Human Functional pEC50 = 9.1 9.1 -10 2
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 167752 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 167752 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 167752 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 176215 None 0 Human Functional pEC50 = 9.0 9.0 -15 2
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 176215 None 0 Human Functional pEC50 = 9.0 9.0 -15 2
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 183412 None 0 Human Functional pEC50 = 9.0 9.0 -3 3
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 183412 None 0 Human Functional pEC50 = 9.0 9.0 -3 3
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 159196 None 0 Human Functional pEC50 = 9 9.0 7 2
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 159196 None 0 Human Functional pEC50 = 9 9.0 7 2
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 173772 None 0 Human Functional pEC50 = 9.0 9.0 6 2
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 173772 None 0 Human Functional pEC50 = 9.0 9.0 6 2
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 167689 None 0 Human Functional pEC50 = 9.0 9.0 -12 2
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 167689 None 0 Human Functional pEC50 = 9.0 9.0 -12 2
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 167689 None 0 Human Functional pEC50 = 9.0 9.0 -12 2
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 142339 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 142339 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 145707 None 7 Human Functional pEC50 = 8.9 8.9 -20 3
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 145707 None 7 Human Functional pEC50 = 8.9 8.9 -20 3
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 167753 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 167753 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 167753 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 167689 None 0 Rat Functional pEC50 = 8.9 8.9 12 2
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 167689 None 0 Rat Functional pEC50 = 8.9 8.9 12 2
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 167689 None 0 Rat Functional pEC50 = 8.9 8.9 12 2
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 111864 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 111864 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 395 None 35 Human Functional pEC50 = 8.9 8.9 -8 3
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 395 None 35 Human Functional pEC50 = 8.9 8.9 -8 3
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 395 None 35 Human Functional pEC50 = 8.9 8.9 -8 3
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 182993 None 0 Human Functional pEC50 = 8.8 8.8 -6 3
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 182993 None 0 Human Functional pEC50 = 8.8 8.8 -6 3
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 167664 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 167664 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 167664 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 167847 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 167847 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 167847 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 111312 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 111312 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 142257 None 0 Human Functional pEC50 = 8.8 8.8 -15 2
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 142257 None 0 Human Functional pEC50 = 8.8 8.8 -15 2
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 142257 None 0 Human Functional pEC50 = 8.8 8.8 -15 2
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 142257 None 0 Human Functional pEC50 = 8.8 8.8 -15 2
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 142257 None 0 Human Functional pEC50 = 8.8 8.8 -15 2
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 142257 None 0 Human Functional pEC50 = 8.8 8.8 -15 2
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 182613 None 0 Human Functional pEC50 = 8.7 8.7 -4 3
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 182613 None 0 Human Functional pEC50 = 8.7 8.7 -4 3
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 167823 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 167823 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 167823 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 166732 None 0 Human Functional pEC50 = 8 8.0 - 1
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 166732 None 0 Human Functional pEC50 = 8 8.0 - 1
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 189660 None 0 Human Functional pEC50 = 8 8.0 - 1
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 189660 None 0 Human Functional pEC50 = 8 8.0 - 1
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 150555 None 0 Human Functional pEC50 = 8 8.0 - 1
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 150555 None 0 Human Functional pEC50 = 8 8.0 - 1
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 163720 None 0 Human Functional pEC50 = 8 8.0 3 2
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 163720 None 0 Human Functional pEC50 = 8 8.0 3 2
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 1156 None 0 Human Functional pEC50 = 8 8.0 - 1
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 1156 None 0 Human Functional pEC50 = 8 8.0 - 1
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 1156 None 0 Human Functional pEC50 = 8 8.0 - 1
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 205023 None 0 Human Functional pEC50 = 8 8.0 - 1
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 205023 None 0 Human Functional pEC50 = 8 8.0 - 1
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 112030 None 0 Human Functional pEC50 = 8 8.0 31 2
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 112030 None 0 Human Functional pEC50 = 8 8.0 31 2
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 74085 None 0 Human Functional pEC50 = 8 8.0 - 1
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 74085 None 0 Human Functional pEC50 = 8 8.0 - 1
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 182312 None 0 Human Functional pEC50 = 8 8.0 -4 3
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 182312 None 0 Human Functional pEC50 = 8 8.0 -4 3
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 164079 None 0 Rat Functional pEC50 = 8 8.0 1 2
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 164079 None 0 Rat Functional pEC50 = 8 8.0 1 2
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 147252 None 0 Rat Functional pEC50 = 8 8.0 - 1
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 147252 None 0 Rat Functional pEC50 = 8 8.0 - 1
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 153070 None 0 Human Functional pEC50 = 8.0 8.0 1995 2
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 153070 None 0 Human Functional pEC50 = 8.0 8.0 1995 2
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 153070 None 0 Human Functional pEC50 = 8.0 8.0 1995 2
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 140492 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 140492 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 163979 None 0 Human Functional pEC50 = 7 7.0 - 1
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 163979 None 0 Human Functional pEC50 = 7 7.0 - 1
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 164600 None 0 Human Functional pEC50 = 7 7.0 - 1
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 164600 None 0 Human Functional pEC50 = 7 7.0 - 1
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 395 None 35 Human Functional pEC50 = 7 7.0 -8 3
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 395 None 35 Human Functional pEC50 = 7 7.0 -8 3
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 395 None 35 Human Functional pEC50 = 7 7.0 -8 3
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 1902 None 58 Human Functional pEC50 = 7 7.0 -1 3
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 1902 None 58 Human Functional pEC50 = 7 7.0 -1 3
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 1902 None 58 Human Functional pEC50 = 7 7.0 -1 3
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 122743 None 0 Human Functional pEC50 = 7 7.0 - 1
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 122743 None 0 Human Functional pEC50 = 7 7.0 - 1
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 179692 None 0 Human Functional pEC50 = 7 7.0 - 1
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 179692 None 0 Human Functional pEC50 = 7 7.0 - 1
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 180063 None 0 Human Functional pEC50 = 7 7.0 - 1
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 180063 None 0 Human Functional pEC50 = 7 7.0 - 1
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 156005 None 0 Human Functional pEC50 = 7 7.0 - 1
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 156005 None 0 Human Functional pEC50 = 7 7.0 - 1
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 167138 None 0 Human Functional pEC50 = 7 7.0 - 1
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 167138 None 0 Human Functional pEC50 = 7 7.0 - 1
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 62184 None 0 Mouse Functional pEC50 = 7 7.0 -2 2
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 62184 None 0 Mouse Functional pEC50 = 7 7.0 -2 2
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 75078 None 0 Human Functional pEC50 = 7 7.0 - 1
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 75078 None 0 Human Functional pEC50 = 7 7.0 - 1
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 75989 None 0 Human Functional pEC50 = 7 7.0 - 1
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 75989 None 0 Human Functional pEC50 = 7 7.0 - 1
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 87860 None 0 Human Functional pEC50 = 6 6.0 - 1
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 87860 None 0 Human Functional pEC50 = 6 6.0 - 1
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 86581 None 0 Human Functional pEC50 = 6 6.0 - 1
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 86581 None 0 Human Functional pEC50 = 6 6.0 - 1
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 86592 None 0 Human Functional pEC50 = 6 6.0 - 1
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 86592 None 0 Human Functional pEC50 = 6 6.0 - 1
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 180727 None 0 Human Functional pEC50 = 6 6.0 - 1
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 180727 None 0 Human Functional pEC50 = 6 6.0 - 1
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
172457497 196421 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 401 7 1 4 4.2 O=C(O)C[S+]([O-])c1ccc(OCc2cccc(-c3ccncc3Cl)c2)cc1 10.1016/j.ejmech.2023.115267
CHEMBL5423697 196421 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 401 7 1 4 4.2 O=C(O)C[S+]([O-])c1ccc(OCc2cccc(-c3ccncc3Cl)c2)cc1 10.1016/j.ejmech.2023.115267
3335 98737 None 64 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 254 5 1 2 3.4 O=C(O)CCC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL277522 98737 None 64 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 254 5 1 2 3.4 O=C(O)CCC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2022.114883
23136477 58847 None 2 Human Functional pEC50 = 5 5.0 -15 2
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 58847 None 2 Human Functional pEC50 = 5 5.0 -15 2
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 58847 None 2 Human Functional pEC50 = 5 5.0 -15 2
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 158135 None 0 Human Functional pEC50 = 5 5.0 -26 2
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 158135 None 0 Human Functional pEC50 = 5 5.0 -26 2
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 203543 None 0 Human Functional pEC50 = 7 7.0 - 1
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 203543 None 0 Human Functional pEC50 = 7 7.0 - 1
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 142224 None 0 Human Functional pEC50 = 7 7.0 - 1
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 142224 None 0 Human Functional pEC50 = 7 7.0 - 1
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 162201 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 162201 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 139913 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 139913 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 173941 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 173941 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 164868 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 164868 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 158135 None 0 Human Functional pEC50 = 5.0 5.0 -26 2
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 158135 None 0 Human Functional pEC50 = 5.0 5.0 -26 2
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 124039 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124039 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 165084 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 165084 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 166534 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 166534 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 192032 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 192032 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 167634 None 0 Human Functional pEC50 = 6.0 6.0 -16 2
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 167634 None 0 Human Functional pEC50 = 6.0 6.0 -16 2
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 167634 None 0 Human Functional pEC50 = 6.0 6.0 -16 2
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
3335 98737 None 64 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 254 5 1 2 3.4 O=C(O)CCC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL277522 98737 None 64 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 254 5 1 2 3.4 O=C(O)CCC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2022.114883
53248847 62167 None 0 Mouse Functional pEC50 = 7.0 7.0 1 2
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 62167 None 0 Mouse Functional pEC50 = 7.0 7.0 1 2
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 152334 None 0 Human Functional pEC50 = 6.0 6.0 -117 3
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 152334 None 0 Human Functional pEC50 = 6.0 6.0 -117 3
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 167752 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 167752 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 167752 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 90015 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 90015 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124037 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124037 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 76291 None 0 Human Functional pEC50 = 5.0 5.0 -13 2
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 76291 None 0 Human Functional pEC50 = 5.0 5.0 -13 2
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 76291 None 0 Human Functional pEC50 = 5.0 5.0 -13 2
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 163176 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 163176 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 140403 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 140403 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 140328 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 140328 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 164874 None 0 Human Functional pEC50 = 7.0 7.0 -6 2
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 164874 None 0 Human Functional pEC50 = 7.0 7.0 -6 2
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 185288 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 185288 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 122521 None 2 Human Functional pEC50 = 6.0 6.0 - 1
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 122521 None 2 Human Functional pEC50 = 6.0 6.0 - 1
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 65366 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 65366 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 61830 None 0 Human Functional pEC50 = 6.0 6.0 22 2
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 61830 None 0 Human Functional pEC50 = 6.0 6.0 22 2
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 62178 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 62178 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 164300 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
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 164300 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
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 123422 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 123422 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 202855 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 202855 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 203571 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 203571 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 162889 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162889 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124045 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124045 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 76302 None 0 Human Functional pEC50 = 7.0 7.0 8 2
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 76302 None 0 Human Functional pEC50 = 7.0 7.0 8 2
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 192788 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 192788 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 171737 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 171737 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 65349 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 65349 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 180233 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 180233 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 163730 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 163730 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 111863 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 111863 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 147212 None 15 Human Functional pEC50 = 8.0 8.0 -3 2
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 147212 None 15 Human Functional pEC50 = 8.0 8.0 -3 2
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 181593 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 181593 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 182612 None 0 Human Functional pEC50 = 8.0 8.0 4 2
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 182612 None 0 Human Functional pEC50 = 8.0 8.0 4 2
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 182477 None 0 Human Functional pEC50 = 8.0 8.0 -14 3
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 182477 None 0 Human Functional pEC50 = 8.0 8.0 -14 3
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 183691 None 0 Human Functional pEC50 = 8.0 8.0 -10 3
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 183691 None 0 Human Functional pEC50 = 8.0 8.0 -10 3
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 182312 None 0 Human Functional pEC50 = 8.0 8.0 -4 3
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 182312 None 0 Human Functional pEC50 = 8.0 8.0 -4 3
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 119197 None 6 Rat Functional pEC50 = 8.0 8.0 -2 2
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 119197 None 6 Rat Functional pEC50 = 8.0 8.0 -2 2
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 162779 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 162779 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 175049 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 175049 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 139780 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 139780 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 90012 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 90012 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 80828 None 25 Rat Functional pEC50 = 7.9 7.9 8 2
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 80828 None 25 Rat Functional pEC50 = 7.9 7.9 8 2
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 175506 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 175506 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 153070 None 0 Human Functional pEC50 = 7.9 7.9 1995 2
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 153070 None 0 Human Functional pEC50 = 7.9 7.9 1995 2
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 153070 None 0 Human Functional pEC50 = 7.9 7.9 1995 2
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 190377 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 190377 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 163695 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 163695 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 70045 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 70045 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 158607 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 158607 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 157915 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 157915 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 158510 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 158510 None 0 Human Functional pEC50 = 7.0 7.0 4 2
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 157094 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 157094 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 159879 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 159879 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 166855 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 166855 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124038 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 124038 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 58848 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 58848 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 80829 None 2 Human Functional pEC50 = 6.0 6.0 - 1
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 80829 None 2 Human Functional pEC50 = 6.0 6.0 - 1
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 70032 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 70032 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 156030 None 0 Mouse Functional pEC50 = 6.0 6.0 -7 2
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 156030 None 0 Mouse Functional pEC50 = 6.0 6.0 -7 2
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 159552 None 0 Mouse Functional pEC50 = 6.0 6.0 1 2
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 159552 None 0 Mouse Functional pEC50 = 6.0 6.0 1 2
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 157296 None 0 Mouse Functional pEC50 = 6.0 6.0 -1 2
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 157296 None 0 Mouse Functional pEC50 = 6.0 6.0 -1 2
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 112024 None 0 Rat Functional pEC50 = 6.0 6.0 -13 2
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 112024 None 0 Rat Functional pEC50 = 6.0 6.0 -13 2
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 166956 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 166956 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 155914 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 155914 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 157879 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 157879 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 166003 None 0 Human Functional pEC50 = 5.0 5.0 -17 2
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 166003 None 0 Human Functional pEC50 = 5.0 5.0 -17 2
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 363 None 48 Human Functional pEC50 = 5.0 5.0 1 3
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 363 None 48 Human Functional pEC50 = 5.0 5.0 1 3
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 363 None 48 Human Functional pEC50 = 5.0 5.0 1 3
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 363 None 48 Human Functional pEC50 = 5.0 5.0 1 3
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 363 None 48 Human Functional pEC50 = 5.0 5.0 1 3
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 90007 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 90007 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 122530 None 3 Human Functional pEC50 = 6.0 6.0 - 1
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 122530 None 3 Human Functional pEC50 = 6.0 6.0 - 1
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 161119 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 161119 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 161119 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 65360 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 65360 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 75952 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 75952 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 146898 None 0 Human Functional pEC50 = 6.0 6.0 -35 3
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 146898 None 0 Human Functional pEC50 = 6.0 6.0 -35 3
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 203022 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 203022 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 62167 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 62167 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 162865 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162865 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 122531 None 1 Human Functional pEC50 = 6.0 6.0 - 1
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 122531 None 1 Human Functional pEC50 = 6.0 6.0 - 1
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 164438 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 164438 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 161739 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 161739 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 162722 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 162722 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 62185 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 62185 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 139866 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 139866 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162280 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162280 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 141073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 141073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 161216 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161216 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161216 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 76295 None 0 Human Functional pEC50 = 5.9 5.9 1 2
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 76295 None 0 Human Functional pEC50 = 5.9 5.9 1 2
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 88322 None 0 Human Functional pEC50 = 5.9 5.9 30 2
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 88322 None 0 Human Functional pEC50 = 5.9 5.9 30 2
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 2287 None 65 Human Functional pEC50 = 4.9 4.9 -1 4
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 2287 None 65 Human Functional pEC50 = 4.9 4.9 -1 4
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 2287 None 65 Human Functional pEC50 = 4.9 4.9 -1 4
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 2287 None 65 Human Functional pEC50 = 4.9 4.9 -1 4
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 2287 None 65 Human Functional pEC50 = 4.9 4.9 -1 4
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 107571 None 40 Human Functional pEC50 = 4.9 4.9 -8 2
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 107571 None 40 Human Functional pEC50 = 4.9 4.9 -8 2
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 123424 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123424 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 137833 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 137833 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 159551 None 0 Human Functional pEC50 = 4.9 4.9 -12 2
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 159551 None 0 Human Functional pEC50 = 4.9 4.9 -12 2
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 154528 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 154528 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 154528 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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
170551835 196117 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 344 5 1 2 5.1 CC#CC(CC(=O)O)c1ccc(-c2ccc3cc(OC)ccc3c2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5417244 196117 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 344 5 1 2 5.1 CC#CC(CC(=O)O)c1ccc(-c2ccc3cc(OC)ccc3c2)cc1 10.1016/j.ejmech.2022.114883
118129974 157286 None 0 Human Functional pEC50 = 6.9 6.9 -4 2
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 157286 None 0 Human Functional pEC50 = 6.9 6.9 -4 2
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 167451 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 167451 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164445 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164445 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 1455 None 44 Human Functional pEC50 = 4.9 4.9 -14 2
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 1455 None 44 Human Functional pEC50 = 4.9 4.9 -14 2
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 1455 None 44 Human Functional pEC50 = 4.9 4.9 -14 2
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 1455 None 44 Human Functional pEC50 = 4.9 4.9 -14 2
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 1455 None 44 Human Functional pEC50 = 4.9 4.9 -14 2
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 1455 None 44 Human Functional pEC50 = 4.9 4.9 -14 2
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 138901 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 138901 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 157663 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 157663 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 156386 None 0 Human Functional pEC50 = 4.9 4.9 -173 6
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 156386 None 0 Human Functional pEC50 = 4.9 4.9 -173 6
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 202953 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 202953 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 147212 None 15 Human Functional pEC50 = 6.9 6.9 -3 2
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 147212 None 15 Human Functional pEC50 = 6.9 6.9 -3 2
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 140376 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 140376 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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
90479828 183190 None 14 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
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 10.1016/j.ejmech.2022.114883
CHEMBL4794409 183190 None 14 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
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 10.1016/j.ejmech.2022.114883
131986116 163919 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
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 163919 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
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 122736 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122736 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122747 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122747 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122761 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122761 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122762 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122762 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 140144 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 140144 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 183190 None 14 Human Functional pEC50 = 7.9 7.9 - 1
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 183190 None 14 Human Functional pEC50 = 7.9 7.9 - 1
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 75850 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75850 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 182113 None 0 Human Functional pEC50 = 7.9 7.9 -10 3
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 182113 None 0 Human Functional pEC50 = 7.9 7.9 -10 3
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 183301 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 183301 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 182216 None 24 Human Functional pEC50 = 7.9 7.9 -7 3
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 182216 None 24 Human Functional pEC50 = 7.9 7.9 -7 3
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 164892 None 0 Rat Functional pEC50 = 7.9 7.9 1 2
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 164892 None 0 Rat Functional pEC50 = 7.9 7.9 1 2
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 77171 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 77171 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 179578 None 0 Human Functional pEC50 = 7.9 7.9 5 2
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 179578 None 0 Human Functional pEC50 = 7.9 7.9 5 2
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 74807 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 74807 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 61832 None 27 Human Functional pEC50 = 7.9 7.9 -1 3
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 61832 None 27 Human Functional pEC50 = 7.9 7.9 -1 3
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 140946 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 140946 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 58856 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58856 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58876 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58876 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163879 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163879 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 170202 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 170202 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 170729 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 170729 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 202651 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 202651 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 70036 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 70036 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 122760 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 122760 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 112028 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 112028 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 180230 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 180230 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 181247 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 181247 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 157117 None 0 Human Functional pEC50 = 6.9 6.9 12 2
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 157117 None 0 Human Functional pEC50 = 6.9 6.9 12 2
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 159014 None 0 Human Functional pEC50 = 6.9 6.9 15 2
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 159014 None 0 Human Functional pEC50 = 6.9 6.9 15 2
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 166622 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 166622 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 65368 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 65368 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58875 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58875 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 90021 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 90021 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 122532 None 3 Human Functional pEC50 = 5.9 5.9 - 1
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 122532 None 3 Human Functional pEC50 = 5.9 5.9 - 1
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 80695 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 80695 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 80706 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 80706 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 1902 None 58 Human Functional pEC50 = 5.9 5.9 -1 3
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 1902 None 58 Human Functional pEC50 = 5.9 5.9 -1 3
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 1902 None 58 Human Functional pEC50 = 5.9 5.9 -1 3
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 70037 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 70037 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 70046 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 70046 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 159204 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 159204 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 159525 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
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 159525 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
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 167693 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 167693 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 167693 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 162779 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 162779 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 163080 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 163080 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 203063 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 203063 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 115599 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 115599 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123425 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123425 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 161312 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161312 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161312 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 142320 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 142320 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 90024 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 90024 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 95056 None 9 Human Functional pEC50 = 4.9 4.9 - 1
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 95056 None 9 Human Functional pEC50 = 4.9 4.9 - 1
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 142214 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 142214 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 142232 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142232 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 86576 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 86576 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164006 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164006 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 138949 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 138949 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 87357 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 87357 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 202772 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 202772 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 62188 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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 62188 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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 62185 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 62185 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 62177 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 2
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 62177 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 2
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 90027 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 90027 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163826 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163826 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 61831 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 61831 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 140430 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 140430 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142270 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 142270 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 148363 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 148363 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 179435 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 179435 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 156386 None 0 Human Functional pEC50 = 4.9 4.9 -173 6
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 156386 None 0 Human Functional pEC50 = 4.9 4.9 -173 6
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 157922 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 157922 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 159551 None 0 Human Functional pEC50 = 4.9 4.9 -12 2
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 159551 None 0 Human Functional pEC50 = 4.9 4.9 -12 2
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 61821 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 61821 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 122569 None 2 Human Functional pEC50 = 5.9 5.9 - 1
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 122569 None 2 Human Functional pEC50 = 5.9 5.9 - 1
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 161079 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161079 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161079 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 62172 None 0 Mouse Functional pEC50 = 6.9 6.9 -2 2
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 62172 None 0 Mouse Functional pEC50 = 6.9 6.9 -2 2
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 167689 None 0 Human Functional pEC50 = 6.9 6.9 -12 2
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 167689 None 0 Human Functional pEC50 = 6.9 6.9 -12 2
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 167689 None 0 Human Functional pEC50 = 6.9 6.9 -12 2
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 142209 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142209 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 169678 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 169678 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 154541 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 154541 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 154541 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161187 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161187 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161187 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164387 None 0 Rat Functional pEC50 = 6.9 6.9 5 2
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 164387 None 0 Rat Functional pEC50 = 6.9 6.9 5 2
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 164883 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164883 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 140370 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 140370 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 184626 None 0 Human Functional pEC50 = 4.9 4.9 42 2
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 184626 None 0 Human Functional pEC50 = 4.9 4.9 42 2
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 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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.2022.114883
6485 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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.2022.114883
CHEMBL1829173 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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.2022.114883
46854655 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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 395 None 35 Human Functional pEC50 = 7.9 7.9 -8 3
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 80828 None 25 Human Functional pEC50 = 7.9 7.9 -8 2
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 80828 None 25 Human Functional pEC50 = 7.9 7.9 -8 2
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 75646 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75646 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 164033 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 164033 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 164211 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
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 164211 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
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 122700 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122700 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122752 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122752 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122757 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122757 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122763 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 122763 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 1902 None 58 Human Functional pEC50 = 7.9 7.9 -1 3
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 1902 None 58 Human Functional pEC50 = 7.9 7.9 -1 3
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 1902 None 58 Human Functional pEC50 = 7.9 7.9 -1 3
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 147760 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 147760 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75853 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75853 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 395 None 35 Mouse Functional pEC50 = 7.9 7.9 1 3
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 395 None 35 Mouse Functional pEC50 = 7.9 7.9 1 3
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 395 None 35 Mouse Functional pEC50 = 7.9 7.9 1 3
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 167818 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 167818 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 167818 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 77171 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 77171 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 90006 None 0 Human Functional pEC50 = 7.9 7.9 5 2
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 90006 None 0 Human Functional pEC50 = 7.9 7.9 5 2
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 62190 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 62190 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 112022 None 0 Human Functional pEC50 = 6.9 6.9 10 2
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 112022 None 0 Human Functional pEC50 = 6.9 6.9 10 2
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 166515 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 166515 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 182450 None 0 Human Functional pEC50 = 6.9 6.9 -6 3
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 182450 None 0 Human Functional pEC50 = 6.9 6.9 -6 3
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 112023 None 0 Rat Functional pEC50 = 6.9 6.9 -13 2
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 112023 None 0 Rat Functional pEC50 = 6.9 6.9 -13 2
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 112031 None 0 Rat Functional pEC50 = 6.9 6.9 -9 2
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 112031 None 0 Rat Functional pEC50 = 6.9 6.9 -9 2
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 80828 None 25 Human Functional pEC50 = 6.9 6.9 -8 2
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 80828 None 25 Human Functional pEC50 = 6.9 6.9 -8 2
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 80828 None 25 Human Functional pEC50 = 6.9 6.9 -8 2
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 80828 None 25 Human Functional pEC50 = 6.9 6.9 -8 2
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 154527 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 154527 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 154527 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 158790 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 158790 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 159374 None 0 Mouse Functional pEC50 = 5.9 5.9 -4 2
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 159374 None 0 Mouse Functional pEC50 = 5.9 5.9 -4 2
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 159510 None 0 Mouse Functional pEC50 = 5.9 5.9 2 2
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 159510 None 0 Mouse Functional pEC50 = 5.9 5.9 2 2
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 156391 None 0 Mouse Functional pEC50 = 5.9 5.9 - 1
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 156391 None 0 Mouse Functional pEC50 = 5.9 5.9 - 1
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 158134 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 158134 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 162863 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 162863 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 80704 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 80704 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 122578 None 5 Human Functional pEC50 = 4.9 4.9 - 1
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 122578 None 5 Human Functional pEC50 = 4.9 4.9 - 1
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 157922 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 157922 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 65345 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 65345 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 90039 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 90039 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123459 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123459 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162591 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162591 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163220 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163220 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162132 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162132 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164714 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 164714 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 145707 None 7 Human Functional pEC50 = 6.9 6.9 -20 3
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 145707 None 7 Human Functional pEC50 = 6.9 6.9 -20 3
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 65369 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 65369 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58849 None 0 Human Functional pEC50 = 6.9 6.9 11 2
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 58849 None 0 Human Functional pEC50 = 6.9 6.9 11 2
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 157006 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 157006 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 204656 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 204656 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123420 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123420 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123421 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123421 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 148664 None 0 Human Functional pEC50 = 5.9 5.9 -23 3
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 148664 None 0 Human Functional pEC50 = 5.9 5.9 -23 3
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 164681 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164681 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 166808 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 166808 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 62168 None 7 Human Functional pEC50 = 5.9 5.9 - 1
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 62168 None 7 Human Functional pEC50 = 5.9 5.9 - 1
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 62190 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 62190 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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
172457330 196246 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 394 7 1 3 4.7 Cc1cccc(C)c1-c1cccc(COc2ccc([S@+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
CHEMBL5419668 196246 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 394 7 1 3 4.7 Cc1cccc(C)c1-c1cccc(COc2ccc([S@+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
134149615 148664 None 0 Human Functional pEC50 = 5.9 5.9 -23 3
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 148664 None 0 Human Functional pEC50 = 5.9 5.9 -23 3
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 138865 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 138865 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142257 None 0 Human Functional pEC50 = 5.9 5.9 -15 2
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 142257 None 0 Human Functional pEC50 = 5.9 5.9 -15 2
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 142257 None 0 Human Functional pEC50 = 5.9 5.9 -15 2
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 163005 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 163005 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 86573 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 86573 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 86578 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 86578 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164639 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164639 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 142257 None 0 Human Functional pEC50 = 5.9 5.9 -15 2
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 142257 None 0 Human Functional pEC50 = 5.9 5.9 -15 2
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 142257 None 0 Human Functional pEC50 = 5.9 5.9 -15 2
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 202961 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 202961 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 142232 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 142232 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 150327 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
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 150327 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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
24857286 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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.2022.114883
6484 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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.2022.114883
CHEMBL1829174 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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.2022.114883
DB12491 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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.2022.114883
146948845 185986 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 185986 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75647 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75647 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 112031 None 0 Human Functional pEC50 = 7.9 7.9 9 2
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 112031 None 0 Human Functional pEC50 = 7.9 7.9 9 2
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 75852 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 75852 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 182663 None 0 Human Functional pEC50 = 7.9 7.9 -3 3
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 182663 None 0 Human Functional pEC50 = 7.9 7.9 -3 3
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 181930 None 0 Human Functional pEC50 = 7.9 7.9 45 3
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 181930 None 0 Human Functional pEC50 = 7.9 7.9 45 3
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 182704 None 0 Human Functional pEC50 = 7.9 7.9 -11 3
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 182704 None 0 Human Functional pEC50 = 7.9 7.9 -11 3
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 162586 None 0 Rat Functional pEC50 = 7.9 7.9 1 3
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 162586 None 0 Rat Functional pEC50 = 7.9 7.9 1 3
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 164033 None 0 Rat Functional pEC50 = 7.9 7.9 -1 2
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 164033 None 0 Rat Functional pEC50 = 7.9 7.9 -1 2
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 164512 None 0 Rat Functional pEC50 = 7.9 7.9 3 2
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 164512 None 0 Rat Functional pEC50 = 7.9 7.9 3 2
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 164547 None 0 Rat Functional pEC50 = 7.9 7.9 1 2
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 164547 None 0 Rat Functional pEC50 = 7.9 7.9 1 2
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 142245 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 142245 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 1624 None 46 Human Functional pEC50 = 7.9 7.9 -3 3
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 140492 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 140492 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 58866 None 0 Human Functional pEC50 = 7.9 7.9 660 2
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 58866 None 0 Human Functional pEC50 = 7.9 7.9 660 2
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 61832 None 27 Human Functional pEC50 = 7.8 7.8 -1 3
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 61832 None 27 Human Functional pEC50 = 7.8 7.8 -1 3
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 81753 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 81753 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75029 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75029 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 164947 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164947 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 182847 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 182847 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 156030 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 156030 None 0 Human Functional pEC50 = 6.9 6.9 7 2
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 74132 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 74132 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 183225 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
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 183225 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
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 123426 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123426 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 157422 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 2
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 157422 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 2
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 112022 None 0 Rat Functional pEC50 = 5.9 5.9 -10 2
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 112022 None 0 Rat Functional pEC50 = 5.9 5.9 -10 2
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 159742 None 0 Mouse Functional pEC50 = 4.9 4.9 -1 2
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 159742 None 0 Mouse Functional pEC50 = 4.9 4.9 -1 2
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 62177 None 0 Human Functional pEC50 = 5.9 5.9 2 2
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 62177 None 0 Human Functional pEC50 = 5.9 5.9 2 2
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 202960 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 202960 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 90401 None 0 Human Functional pEC50 = 6.9 6.9 58 2
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 90401 None 0 Human Functional pEC50 = 6.9 6.9 58 2
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 164341 None 0 Human Functional pEC50 = 5.9 5.9 -4 2
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 164341 None 0 Human Functional pEC50 = 5.9 5.9 -4 2
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 159847 None 0 Human Functional pEC50 = 5.9 5.9 -2 2
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 159847 None 0 Human Functional pEC50 = 5.9 5.9 -2 2
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 140127 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 140127 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 203335 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 203335 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162331 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162331 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 86572 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 86572 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 90399 None 0 Human Functional pEC50 = 6.8 6.8 39 2
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 90399 None 0 Human Functional pEC50 = 6.8 6.8 39 2
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 76452 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 76452 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 139107 None 0 Human Functional pEC50 = 5.8 5.8 2 2
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 139107 None 0 Human Functional pEC50 = 5.8 5.8 2 2
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 90407 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 90407 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 90023 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 90023 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 191140 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 191140 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 94713 None 5 Human Functional pEC50 = 4.8 4.8 - 1
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 94713 None 5 Human Functional pEC50 = 4.8 4.8 - 1
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 151165 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 151165 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167689 None 0 Human Functional pEC50 = 6.8 6.8 -12 2
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 167689 None 0 Human Functional pEC50 = 6.8 6.8 -12 2
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 167689 None 0 Human Functional pEC50 = 6.8 6.8 -12 2
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 142339 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 142339 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 122756 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 122756 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 123396 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 123396 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 3886 None 39 Mouse Functional pEC50 = 6.8 6.8 -13 4
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 3886 None 39 Mouse Functional pEC50 = 6.8 6.8 -13 4
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 3886 None 39 Mouse Functional pEC50 = 6.8 6.8 -13 4
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 167174 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 167174 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 158826 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 158826 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 164270 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164270 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 123423 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 123423 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 161277 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 161277 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 161277 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 156442 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 156442 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 62179 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 2
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 62179 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 2
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 62181 None 0 Mouse Functional pEC50 = 6.8 6.8 2 2
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 62181 None 0 Mouse Functional pEC50 = 6.8 6.8 2 2
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 164547 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 164547 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 164892 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 164892 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 75851 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75851 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75859 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75859 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 395 None 35 Human Functional pEC50 = 7.8 7.8 -8 3
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 395 None 35 Human Functional pEC50 = 7.8 7.8 -8 3
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 395 None 35 Human Functional pEC50 = 7.8 7.8 -8 3
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 175489 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 175489 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 163606 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 163606 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 183086 None 0 Rat Functional pEC50 = 7.8 7.8 -3 2
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 183086 None 0 Rat Functional pEC50 = 7.8 7.8 -3 2
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 176313 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 176313 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 139959 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 139959 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 171327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 171327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 183097 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 183097 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156536 None 0 Human Functional pEC50 = 6.8 6.8 45 2
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 156536 None 0 Human Functional pEC50 = 6.8 6.8 45 2
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 157843 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 157843 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 159140 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 159140 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156515 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156515 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 158847 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 158847 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 166832 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 166832 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 192022 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 192022 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 122734 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 122734 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 157117 None 0 Mouse Functional pEC50 = 5.8 5.8 -12 2
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 157117 None 0 Mouse Functional pEC50 = 5.8 5.8 -12 2
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 157235 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 2
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 157235 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 2
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 175752 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 175752 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 86582 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 86582 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 94688 None 10 Human Functional pEC50 = 4.8 4.8 - 1
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 94688 None 10 Human Functional pEC50 = 4.8 4.8 - 1
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
170551847 195019 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 270 4 1 2 4.0 CC#CC(CC(=O)O)c1ccc(-c2ccccc2)s1 10.1016/j.ejmech.2022.114883
CHEMBL5395099 195019 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 270 4 1 2 4.0 CC#CC(CC(=O)O)c1ccc(-c2ccccc2)s1 10.1016/j.ejmech.2022.114883
71257551 150681 None 25 Human Functional pEC50 = 6.8 6.8 -14 3
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 150681 None 25 Human Functional pEC50 = 6.8 6.8 -14 3
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 140354 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 140354 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 163681 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 163681 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 115726 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 115726 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 190382 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 190382 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 164051 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 164051 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 142320 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 142320 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 58846 None 0 Human Functional pEC50 = 6.8 6.8 77 2
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 58846 None 0 Human Functional pEC50 = 6.8 6.8 77 2
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 186492 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 186492 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156078 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 156078 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 162618 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162618 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 175786 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 175786 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 62179 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 62179 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 165115 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 165115 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 163684 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 163684 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 62180 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 62180 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 153367 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 153367 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 156078 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 156078 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 159698 None 0 Human Functional pEC50 = 5.8 5.8 -40 2
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 159698 None 0 Human Functional pEC50 = 5.8 5.8 -40 2
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 159847 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 159847 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
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 1624 None 46 Human Functional pEC50 = 7.8 7.8 -3 3
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 1624 None 46 Human Functional pEC50 = 7.8 7.8 -3 3
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 1624 None 46 Human Functional pEC50 = 7.8 7.8 -3 3
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 1624 None 46 Human Functional pEC50 = 7.8 7.8 -3 3
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 75638 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75638 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75656 None 1 Human Functional pEC50 = 7.8 7.8 - 1
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 75656 None 1 Human Functional pEC50 = 7.8 7.8 - 1
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 75657 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75657 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 163978 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 163978 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 171297 None 0 Human Functional pEC50 = 7.8 7.8 2 2
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 171297 None 0 Human Functional pEC50 = 7.8 7.8 2 2
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 111721 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 111721 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 157415 None 0 Human Functional pEC50 = 7.8 7.8 5 2
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 157415 None 0 Human Functional pEC50 = 7.8 7.8 5 2
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 90010 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 90010 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 164874 None 0 Rat Functional pEC50 = 7.8 7.8 6 2
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 164874 None 0 Rat Functional pEC50 = 7.8 7.8 6 2
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 112020 None 0 Rat Functional pEC50 = 7.8 7.8 -4 2
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 112020 None 0 Rat Functional pEC50 = 7.8 7.8 -4 2
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 142252 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 142252 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 174103 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 174103 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 185339 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 185339 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 58858 None 0 Human Functional pEC50 = 7.8 7.8 107 2
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 58858 None 0 Human Functional pEC50 = 7.8 7.8 107 2
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 90404 None 0 Human Functional pEC50 = 7.8 7.8 562 2
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 90404 None 0 Human Functional pEC50 = 7.8 7.8 562 2
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 122518 None 2 Human Functional pEC50 = 6.8 6.8 - 1
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 122518 None 2 Human Functional pEC50 = 6.8 6.8 - 1
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 80828 None 25 Human Functional pEC50 = 6.8 6.8 -8 2
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 171968 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 171968 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 180524 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 180524 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 1624 None 46 Human Functional pEC50 = 6.8 6.8 -3 3
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 1624 None 46 Human Functional pEC50 = 6.8 6.8 -3 3
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 1624 None 46 Human Functional pEC50 = 6.8 6.8 -3 3
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 1624 None 46 Human Functional pEC50 = 6.8 6.8 -3 3
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 122522 None 2 Human Functional pEC50 = 5.8 5.8 - 1
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 122522 None 2 Human Functional pEC50 = 5.8 5.8 - 1
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 122731 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 122731 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 155566 None 5 Human Functional pEC50 = 4.8 4.8 - 1
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 155566 None 5 Human Functional pEC50 = 4.8 4.8 - 1
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 86585 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 86585 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 142224 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 142224 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 170225 None 0 Rat Functional pEC50 = 6.8 6.8 -3 2
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 170225 None 0 Rat Functional pEC50 = 6.8 6.8 -3 2
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 159698 None 0 Human Functional pEC50 = 5.8 5.8 -40 2
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 159698 None 0 Human Functional pEC50 = 5.8 5.8 -40 2
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 204141 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 204141 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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
170551841 196296 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 298 4 1 1 4.6 CC#CC(CC(=O)O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5420725 196296 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 298 4 1 1 4.6 CC#CC(CC(=O)O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2022.114883
127052270 140320 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 140320 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 162838 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162838 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 61823 None 2 Human Functional pEC50 = 6.8 6.8 17 2
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 61823 None 2 Human Functional pEC50 = 6.8 6.8 17 2
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 88024 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 88024 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 137777 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 137777 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 137864 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 137864 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 94711 None 9 Human Functional pEC50 = 4.8 4.8 - 1
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 94711 None 9 Human Functional pEC50 = 4.8 4.8 - 1
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 155216 None 10 Human Functional pEC50 = 4.8 4.8 - 1
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 155216 None 10 Human Functional pEC50 = 4.8 4.8 - 1
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 395 None 35 Human Functional pEC50 = 6.8 6.8 -8 3
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 395 None 35 Human Functional pEC50 = 6.8 6.8 -8 3
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 395 None 35 Human Functional pEC50 = 6.8 6.8 -8 3
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 164237 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164237 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 140343 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 140343 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 142214 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 142214 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 75649 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75649 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75651 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75651 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75652 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75652 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75658 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75658 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 181463 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 181463 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 183658 None 1 Human Functional pEC50 = 7.8 7.8 - 1
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 183658 None 1 Human Functional pEC50 = 7.8 7.8 - 1
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 182192 None 0 Human Functional pEC50 = 7.8 7.8 -7 3
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 182192 None 0 Human Functional pEC50 = 7.8 7.8 -7 3
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 182477 None 0 Human Functional pEC50 = 7.8 7.8 -14 3
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 182477 None 0 Human Functional pEC50 = 7.8 7.8 -14 3
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 183167 None 0 Human Functional pEC50 = 7.8 7.8 -4 3
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 183167 None 0 Human Functional pEC50 = 7.8 7.8 -4 3
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 183497 None 0 Human Functional pEC50 = 7.8 7.8 -5 3
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 183497 None 0 Human Functional pEC50 = 7.8 7.8 -5 3
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 181568 None 7 Rat Functional pEC50 = 7.8 7.8 -2 3
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 181568 None 7 Rat Functional pEC50 = 7.8 7.8 -2 3
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 81752 None 0 Human Functional pEC50 = 7.8 7.8 630 2
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 81752 None 0 Human Functional pEC50 = 7.8 7.8 630 2
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 81825 None 0 Human Functional pEC50 = 7.8 7.8 5248 2
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 81825 None 0 Human Functional pEC50 = 7.8 7.8 5248 2
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 58863 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 58863 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 58864 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 58864 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164694 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164694 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 192342 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 192342 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 158873 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 158873 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 167298 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167298 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156722 None 0 Mouse Functional pEC50 = 6.8 6.8 -3 2
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 156722 None 0 Mouse Functional pEC50 = 6.8 6.8 -3 2
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 58884 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 58884 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 74075 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 74075 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 122728 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 122728 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 157290 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 157290 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 159552 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
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 159552 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
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 62176 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 62176 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 162955 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162955 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 149630 None 0 Human Functional pEC50 = 6.8 6.8 9 2
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 149630 None 0 Human Functional pEC50 = 6.8 6.8 9 2
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 76783 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 76783 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164540 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164540 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 65367 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 65367 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 1156 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 1156 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 1156 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 140385 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 140385 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 161507 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 161507 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 170246 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 170246 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 1902 None 58 Human Functional pEC50 = 4.8 4.8 -1 3
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 1902 None 58 Human Functional pEC50 = 4.8 4.8 -1 3
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 1902 None 58 Human Functional pEC50 = 4.8 4.8 -1 3
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 162462 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162462 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 140285 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 140285 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 75641 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75641 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75650 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75650 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75654 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 75654 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 164810 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 164810 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 203261 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 203261 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 112029 None 0 Human Functional pEC50 = 7.8 7.8 5 2
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 112029 None 0 Human Functional pEC50 = 7.8 7.8 5 2
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 182663 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 182663 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 164004 None 0 Rat Functional pEC50 = 7.8 7.8 2 2
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 164004 None 0 Rat Functional pEC50 = 7.8 7.8 2 2
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 58879 None 1 Rat Functional pEC50 = 7.8 7.8 -1 2
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 58879 None 1 Rat Functional pEC50 = 7.8 7.8 -1 2
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 181593 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
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 181593 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
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 142214 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 142214 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 90396 None 0 Human Functional pEC50 = 7.7 7.7 75 2
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 90396 None 0 Human Functional pEC50 = 7.7 7.7 75 2
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 90405 None 0 Human Functional pEC50 = 7.7 7.7 64 2
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 90405 None 0 Human Functional pEC50 = 7.7 7.7 64 2
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 165271 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 165271 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 61832 None 27 Human Functional pEC50 = 7.7 7.7 -1 3
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 61832 None 27 Human Functional pEC50 = 7.7 7.7 -1 3
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 61832 None 27 Human Functional pEC50 = 7.7 7.7 -1 3
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 61832 None 27 Human Functional pEC50 = 7.7 7.7 -1 3
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 61832 None 27 Human Functional pEC50 = 7.7 7.7 -1 3
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 61832 None 27 Human Functional pEC50 = 7.7 7.7 -1 3
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 70043 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 70043 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 182610 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 182610 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156861 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 156861 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 74083 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 74083 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 182325 None 0 Human Functional pEC50 = 6.8 6.8 -4 3
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 182325 None 0 Human Functional pEC50 = 6.8 6.8 -4 3
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 94628 None 7 Human Functional pEC50 = 5.8 5.8 - 1
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 94628 None 7 Human Functional pEC50 = 5.8 5.8 - 1
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 58862 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 58862 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 191738 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 191738 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 162448 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 162448 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 162839 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 162839 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 2321 None 51 Human Functional pEC50 = 5.8 5.8 -7 4
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 2321 None 51 Human Functional pEC50 = 5.8 5.8 -7 4
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 2321 None 51 Human Functional pEC50 = 5.8 5.8 -7 4
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 2321 None 51 Human Functional pEC50 = 5.8 5.8 -7 4
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 2321 None 51 Human Functional pEC50 = 5.8 5.8 -7 4
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 167165 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 167165 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 156921 None 0 Human Functional pEC50 = 4.7 4.7 -97 2
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 156921 None 0 Human Functional pEC50 = 4.7 4.7 -97 2
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 3888 None 8 Rat Functional pEC50 = 6.7 6.7 -4 3
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 3888 None 8 Rat Functional pEC50 = 6.7 6.7 -4 3
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 3888 None 8 Rat Functional pEC50 = 6.7 6.7 -4 3
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 87980 None 0 Human Functional pEC50 = 6.7 6.7 29 2
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 87980 None 0 Human Functional pEC50 = 6.7 6.7 29 2
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 139238 None 0 Human Functional pEC50 = 5.7 5.7 2 2
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 139238 None 0 Human Functional pEC50 = 5.7 5.7 2 2
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
170551850 196269 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 333 5 1 2 4.5 CC#CC(CC(=O)O)c1ccc(-c2cccc(N3CCCC3)c2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5420250 196269 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 333 5 1 2 4.5 CC#CC(CC(=O)O)c1ccc(-c2cccc(N3CCCC3)c2)cc1 10.1016/j.ejmech.2022.114883
134134229 143342 None 0 Human Functional pEC50 = 5.7 5.7 -61 3
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 143342 None 0 Human Functional pEC50 = 5.7 5.7 -61 3
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 143342 None 0 Human Functional pEC50 = 5.7 5.7 -61 3
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 143342 None 0 Human Functional pEC50 = 5.7 5.7 -61 3
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 163837 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 163837 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 86551 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 86551 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 65365 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 65365 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 61827 None 0 Human Functional pEC50 = 6.7 6.7 34 2
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 61827 None 0 Human Functional pEC50 = 6.7 6.7 34 2
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 58847 None 2 Human Functional pEC50 = 4.7 4.7 -15 2
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 58847 None 2 Human Functional pEC50 = 4.7 4.7 -15 2
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 58847 None 2 Human Functional pEC50 = 4.7 4.7 -15 2
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 166617 None 18 Human Functional pEC50 = 4.7 4.7 - 1
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 166617 None 18 Human Functional pEC50 = 4.7 4.7 - 1
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 140814 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 140814 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 162160 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 162160 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 203406 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 203406 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 122581 None 2 Human Functional pEC50 = 4.7 4.7 - 1
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 122581 None 2 Human Functional pEC50 = 4.7 4.7 - 1
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 137716 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 137716 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 58880 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 58880 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 1953 None 20 Human Functional pEC50 = 7.7 7.7 - 1
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 1953 None 20 Human Functional pEC50 = 7.7 7.7 - 1
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 1953 None 20 Human Functional pEC50 = 7.7 7.7 - 1
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 179682 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 179682 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 111314 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 111314 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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
10668 1953 None 20 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human FFAR1 expressed in CHO cells by FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells by FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.ejmech.2022.114883
139600331 1953 None 20 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human FFAR1 expressed in CHO cells by FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells by FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.ejmech.2022.114883
CHEMBL5169614 1953 None 20 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human FFAR1 expressed in CHO cells by FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells by FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.ejmech.2022.114883
57414680 75655 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 75655 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 77245 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 77245 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 77245 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 163615 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 163615 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 119198 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 119198 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 122741 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 122741 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 182983 None 5 Human Functional pEC50 = 7.7 7.7 -12 3
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 182983 None 5 Human Functional pEC50 = 7.7 7.7 -12 3
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 163615 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
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 163615 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
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 163954 None 0 Rat Functional pEC50 = 7.7 7.7 1 2
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 163954 None 0 Rat Functional pEC50 = 7.7 7.7 1 2
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 163978 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
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 163978 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
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 162559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 162559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 90031 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 90031 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 169834 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 169834 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 86563 None 0 Human Functional pEC50 = 7.7 7.7 5 3
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 86563 None 0 Human Functional pEC50 = 7.7 7.7 5 3
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 86563 None 0 Human Functional pEC50 = 7.7 7.7 5 3
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 86563 None 0 Human Functional pEC50 = 7.7 7.7 5 3
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 122764 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 122764 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157572 None 0 Human Functional pEC50 = 6.7 6.7 17 2
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 157572 None 0 Human Functional pEC50 = 6.7 6.7 17 2
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 159812 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 159812 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 182560 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
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 182560 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
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 112032 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
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 112032 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
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 90011 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 90011 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 86564 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 86564 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164298 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164298 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 80694 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80694 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80701 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80701 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 156968 None 0 Mouse Functional pEC50 = 5.7 5.7 -8 2
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 156968 None 0 Mouse Functional pEC50 = 5.7 5.7 -8 2
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 159014 None 0 Mouse Functional pEC50 = 5.7 5.7 -15 2
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 159014 None 0 Mouse Functional pEC50 = 5.7 5.7 -15 2
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 95089 None 8 Human Functional pEC50 = 4.7 4.7 - 1
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 95089 None 8 Human Functional pEC50 = 4.7 4.7 - 1
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 2747 None 10 Human Functional pEC50 = 4.7 4.7 -8 2
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 2747 None 10 Human Functional pEC50 = 4.7 4.7 -8 2
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 2747 None 10 Human Functional pEC50 = 4.7 4.7 -8 2
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 156691 None 0 Mouse Functional pEC50 = 4.7 4.7 -9 2
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 156691 None 0 Mouse Functional pEC50 = 4.7 4.7 -9 2
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 157810 None 0 Mouse Functional pEC50 = 4.7 4.7 - 1
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 157810 None 0 Mouse Functional pEC50 = 4.7 4.7 - 1
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 58847 None 2 Human Functional pEC50 = 5.7 5.7 -15 2
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 58847 None 2 Human Functional pEC50 = 5.7 5.7 -15 2
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 58847 None 2 Human Functional pEC50 = 5.7 5.7 -15 2
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 139746 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 139746 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 157463 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 157463 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 87980 None 0 Human Functional pEC50 = 6.7 6.7 29 2
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 87980 None 0 Human Functional pEC50 = 6.7 6.7 29 2
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 163908 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163908 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164567 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164567 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 90408 None 0 Human Functional pEC50 = 5.7 5.7 33 2
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 90408 None 0 Human Functional pEC50 = 5.7 5.7 33 2
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 3888 None 8 Human Functional pEC50 = 5.7 5.7 4 3
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 3888 None 8 Human Functional pEC50 = 5.7 5.7 4 3
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 3888 None 8 Human Functional pEC50 = 5.7 5.7 4 3
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 137915 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 137915 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 157149 None 0 Human Functional pEC50 = 4.7 4.7 -117 2
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 157149 None 0 Human Functional pEC50 = 4.7 4.7 -117 2
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 173003 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 173003 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164247 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 164247 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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
170551856 196731 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 265 4 1 2 3.3 CC#CC(CC(=O)O)c1ccc(-c2ccccc2)nc1 10.1016/j.ejmech.2022.114883
CHEMBL5431117 196731 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 265 4 1 2 3.3 CC#CC(CC(=O)O)c1ccc(-c2ccccc2)nc1 10.1016/j.ejmech.2022.114883
134465785 176215 None 0 Human Functional pEC50 = 6.7 6.7 -15 2
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 176215 None 0 Human Functional pEC50 = 6.7 6.7 -15 2
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 61827 None 0 Human Functional pEC50 = 6.7 6.7 34 2
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 61827 None 0 Human Functional pEC50 = 6.7 6.7 34 2
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 86570 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 86570 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 139173 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 139173 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 186792 None 0 Human Functional pEC50 = 6.7 6.7 61 2
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 88066 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 88066 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 149940 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 149940 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 156821 None 0 Human Functional pEC50 = 4.7 4.7 -32 2
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 156821 None 0 Human Functional pEC50 = 4.7 4.7 -32 2
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 156921 None 0 Human Functional pEC50 = 4.7 4.7 -97 2
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 156921 None 0 Human Functional pEC50 = 4.7 4.7 -97 2
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 157149 None 0 Human Functional pEC50 = 4.7 4.7 -117 2
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 157149 None 0 Human Functional pEC50 = 4.7 4.7 -117 2
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 186443 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 186443 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 171578 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 171578 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 164858 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 164858 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 157859 None 0 Human Functional pEC50 = 8.7 8.7 2 2
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 157859 None 0 Human Functional pEC50 = 8.7 8.7 2 2
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 179974 None 0 Human Functional pEC50 = 8.7 8.7 15 2
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 179974 None 0 Human Functional pEC50 = 8.7 8.7 15 2
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 181568 None 7 Human Functional pEC50 = 8.7 8.7 -1 3
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 181568 None 7 Human Functional pEC50 = 8.7 8.7 -1 3
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 164211 None 0 Rat Functional pEC50 = 8.7 8.7 6 2
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 164211 None 0 Rat Functional pEC50 = 8.7 8.7 6 2
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 171420 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 171420 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 183481 None 0 Human Functional pEC50 = 8.7 8.7 -6 3
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 183481 None 0 Human Functional pEC50 = 8.7 8.7 -6 3
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 172906 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 172906 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 183497 None 0 Human Functional pEC50 = 8.6 8.6 -5 3
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 183497 None 0 Human Functional pEC50 = 8.6 8.6 -5 3
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 142257 None 0 Rat Functional pEC50 = 8.6 8.6 15 2
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 142257 None 0 Rat Functional pEC50 = 8.6 8.6 15 2
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 142257 None 0 Rat Functional pEC50 = 8.6 8.6 15 2
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 186089 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 186089 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 141103 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 141103 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 180163 None 0 Human Functional pEC50 = 8.6 8.6 11 2
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 180163 None 0 Human Functional pEC50 = 8.6 8.6 11 2
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 167689 None 0 Human Functional pEC50 = 8.6 8.6 -12 2
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 167689 None 0 Human Functional pEC50 = 8.6 8.6 -12 2
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 167689 None 0 Human Functional pEC50 = 8.6 8.6 -12 2
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 142209 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 142209 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 167634 None 0 Human Functional pEC50 = 8.6 8.6 -16 2
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 167634 None 0 Human Functional pEC50 = 8.6 8.6 -16 2
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 167634 None 0 Human Functional pEC50 = 8.6 8.6 -16 2
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 183301 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 183301 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 183412 None 0 Human Functional pEC50 = 8.5 8.5 -3 3
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 183412 None 0 Human Functional pEC50 = 8.5 8.5 -3 3
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 58877 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 58877 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 86563 None 0 Human Functional pEC50 = 7.7 7.7 5 3
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 86563 None 0 Human Functional pEC50 = 7.7 7.7 5 3
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 139096 None 0 Human Functional pEC50 = 7.7 7.7 1000 2
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 139096 None 0 Human Functional pEC50 = 7.7 7.7 1000 2
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 164079 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
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 164079 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
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 164581 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 164581 None 0 Human Functional pEC50 = 7.7 7.7 1 2
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 112034 None 2 Human Functional pEC50 = 7.7 7.7 3 2
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 112034 None 2 Human Functional pEC50 = 7.7 7.7 3 2
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 112034 None 2 Human Functional pEC50 = 7.7 7.7 3 2
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 112034 None 2 Human Functional pEC50 = 7.7 7.7 3 2
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 122767 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 122767 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 112034 None 2 Human Functional pEC50 = 7.7 7.7 3 2
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 112034 None 2 Human Functional pEC50 = 7.7 7.7 3 2
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 173772 None 0 Human Functional pEC50 = 7.7 7.7 6 2
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 173772 None 0 Human Functional pEC50 = 7.7 7.7 6 2
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 162586 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 162586 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 75849 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 75849 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 182613 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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 182613 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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 163948 None 0 Rat Functional pEC50 = 7.7 7.7 4 2
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 163948 None 0 Rat Functional pEC50 = 7.7 7.7 4 2
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 164581 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
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 164581 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
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 139096 None 0 Human Functional pEC50 = 7.7 7.7 1000 2
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 139096 None 0 Human Functional pEC50 = 7.7 7.7 1000 2
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 185867 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 185867 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 170480 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 170480 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167222 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167222 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 181768 None 0 Rat Functional pEC50 = 6.7 6.7 -5 2
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 181768 None 0 Rat Functional pEC50 = 6.7 6.7 -5 2
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 152670 None 0 Human Functional pEC50 = 5.7 5.7 -8 2
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 152670 None 0 Human Functional pEC50 = 5.7 5.7 -8 2
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 156437 None 0 Mouse Functional pEC50 = 5.7 5.7 2 2
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 156437 None 0 Mouse Functional pEC50 = 5.7 5.7 2 2
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
141515497 195707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 298 3 1 2 2.6 Cc1ccccc1C#Cc1ccc([S+]([O-])CC(=O)O)cc1 10.1016/j.ejmech.2023.115267
CHEMBL5409372 195707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 298 3 1 2 2.6 Cc1ccccc1C#Cc1ccc([S+]([O-])CC(=O)O)cc1 10.1016/j.ejmech.2023.115267
172448668 196024 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 381 7 1 4 3.8 Cc1cnccc1-c1cccc(COc2ccc([S+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
CHEMBL5415281 196024 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 381 7 1 4 3.8 Cc1cnccc1-c1cccc(COc2ccc([S+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
134139528 154628 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 154628 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 154628 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 159674 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 159674 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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
170551876 197176 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 298 4 1 1 4.6 CC#CC(CC(=O)O)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5440434 197176 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 298 4 1 1 4.6 CC#CC(CC(=O)O)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.ejmech.2022.114883
46231486 202800 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 202800 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 162963 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 162963 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 58846 None 0 Human Functional pEC50 = 6.7 6.7 77 2
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 58846 None 0 Human Functional pEC50 = 6.7 6.7 77 2
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 141316 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 141316 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 76814 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 76814 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 76296 None 0 Human Functional pEC50 = 5.7 5.7 -10 2
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 76296 None 0 Human Functional pEC50 = 5.7 5.7 -10 2
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 86553 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 86553 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 76814 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 76814 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 90026 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 90026 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 161125 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 161125 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 161125 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 202650 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 202650 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 139174 None 0 Human Functional pEC50 = 6.7 6.7 165 2
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 139174 None 0 Human Functional pEC50 = 6.7 6.7 165 2
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 166765 None 59 Human Functional pEC50 = 4.7 4.7 -12 2
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 166765 None 59 Human Functional pEC50 = 4.7 4.7 -12 2
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 203062 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 203062 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 122766 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 122766 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 74081 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 74081 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 183481 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
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 183481 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
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 163780 None 0 Rat Functional pEC50 = 7.7 7.7 3 2
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 163780 None 0 Rat Functional pEC50 = 7.7 7.7 3 2
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 164520 None 0 Rat Functional pEC50 = 7.7 7.7 1 2
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 164520 None 0 Rat Functional pEC50 = 7.7 7.7 1 2
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 180334 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 180334 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 81751 None 25 Human Functional pEC50 = 7.7 7.7 - 1
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 81751 None 25 Human Functional pEC50 = 7.7 7.7 - 1
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 122524 None 1 Human Functional pEC50 = 6.7 6.7 - 1
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 122524 None 1 Human Functional pEC50 = 6.7 6.7 - 1
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 164830 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164830 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157972 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157972 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 158884 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 158884 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 122733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 122733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157709 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157709 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 166664 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 166664 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167077 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167077 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167395 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167395 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157915 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 157915 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 112017 None 0 Rat Functional pEC50 = 6.7 6.7 -2 2
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 112017 None 0 Rat Functional pEC50 = 6.7 6.7 -2 2
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 80705 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80705 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80826 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80826 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 190642 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 190642 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 122750 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 122750 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 156007 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 156007 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 151340 None 0 Human Functional pEC50 = 5.7 5.7 -38 2
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 151340 None 0 Human Functional pEC50 = 5.7 5.7 -38 2
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 167252 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 167252 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 157313 None 0 Mouse Functional pEC50 = 5.7 5.7 -7 2
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 157313 None 0 Mouse Functional pEC50 = 5.7 5.7 -7 2
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 112027 None 0 Rat Functional pEC50 = 5.7 5.7 -32 2
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 112027 None 0 Rat Functional pEC50 = 5.7 5.7 -32 2
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 189873 None 0 Human Functional pEC50 = 4.7 4.7 -12 2
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 189873 None 0 Human Functional pEC50 = 4.7 4.7 -12 2
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 137800 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 137800 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 162792 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 162792 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167119 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 167119 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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
170551844 196238 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 282 4 1 1 4.1 CC#CC(CC(=O)O)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5419482 196238 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 282 4 1 1 4.1 CC#CC(CC(=O)O)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.ejmech.2022.114883
86803188 122570 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 122570 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 164714 None 0 Rat Functional pEC50 = 6.7 6.7 -1 2
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 164714 None 0 Rat Functional pEC50 = 6.7 6.7 -1 2
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 164369 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164369 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164661 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 164661 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 161586 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 161586 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 90397 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 90397 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 61818 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 61818 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 139755 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 139755 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 173760 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 173760 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 164049 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 164049 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 156821 None 0 Human Functional pEC50 = 4.7 4.7 -32 2
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 156821 None 0 Human Functional pEC50 = 4.7 4.7 -32 2
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 204137 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 204137 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 88025 None 0 Human Functional pEC50 = 6.7 6.7 208 2
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 88025 None 0 Human Functional pEC50 = 6.7 6.7 208 2
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 86587 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 86587 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 90009 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 90009 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163376 None 3 Human Functional pEC50 = 5.7 5.7 - 1
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 163376 None 3 Human Functional pEC50 = 5.7 5.7 - 1
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 111316 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 111316 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 75644 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 75644 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 74076 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 74076 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 172906 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
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 172906 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
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 58879 None 1 Human Functional pEC50 = 7.7 7.7 1 2
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 58879 None 1 Human Functional pEC50 = 7.7 7.7 1 2
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 182993 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
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 182993 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
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 142245 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 142245 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 90403 None 0 Human Functional pEC50 = 7.7 7.7 173 2
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 90403 None 0 Human Functional pEC50 = 7.7 7.7 173 2
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 173870 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 173870 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 139856 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 139856 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 190127 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 190127 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 169659 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 169659 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 171152 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 171152 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 156669 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 156669 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 156968 None 0 Human Functional pEC50 = 6.7 6.7 8 2
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 156968 None 0 Human Functional pEC50 = 6.7 6.7 8 2
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 157819 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 157819 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 174071 None 0 Human Functional pEC50 = 6.7 6.7 -15 2
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 174071 None 0 Human Functional pEC50 = 6.7 6.7 -15 2
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 80700 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 80700 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 85800 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 85800 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 1902 None 58 Human Functional pEC50 = 5.7 5.7 -1 3
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 1902 None 58 Human Functional pEC50 = 5.7 5.7 -1 3
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 1902 None 58 Human Functional pEC50 = 5.7 5.7 -1 3
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 151191 None 0 Human Functional pEC50 = 5.7 5.7 -63 2
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 151191 None 0 Human Functional pEC50 = 5.7 5.7 -63 2
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 165991 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 165991 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 202771 None 2 Human Functional pEC50 = 5.7 5.7 - 1
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 202771 None 2 Human Functional pEC50 = 5.7 5.7 - 1
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 86589 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 86589 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 1902 None 58 Human Functional pEC50 = 6.7 6.7 -1 3
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 1902 None 58 Human Functional pEC50 = 6.7 6.7 -1 3
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 1902 None 58 Human Functional pEC50 = 6.7 6.7 -1 3
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 62188 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 62188 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 166991 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 166991 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 171986 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 171986 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 155217 None 7 Human Functional pEC50 = 4.7 4.7 - 1
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 155217 None 7 Human Functional pEC50 = 4.7 4.7 - 1
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 201875 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 201875 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 86569 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 86569 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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
170551874 197172 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 332 4 1 1 5.0 CC#C[C@@H](CC(=O)O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5440386 197172 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 332 4 1 1 5.0 CC#C[C@@H](CC(=O)O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2022.114883
131986057 163750 None 0 Human Functional pEC50 = 7.6 7.6 1 2
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 163750 None 0 Human Functional pEC50 = 7.6 7.6 1 2
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 74073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 122744 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 122744 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 75855 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75855 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75861 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75861 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 182450 None 0 Human Functional pEC50 = 7.6 7.6 -6 3
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 182450 None 0 Human Functional pEC50 = 7.6 7.6 -6 3
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 183092 None 0 Human Functional pEC50 = 7.6 7.6 -13 3
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 183092 None 0 Human Functional pEC50 = 7.6 7.6 -13 3
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 162586 None 0 Mouse Functional pEC50 = 7.6 7.6 -1 3
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 162586 None 0 Mouse Functional pEC50 = 7.6 7.6 -1 3
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 395 None 35 Rat Functional pEC50 = 7.6 7.6 -1 3
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 395 None 35 Rat Functional pEC50 = 7.6 7.6 -1 3
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 395 None 35 Rat Functional pEC50 = 7.6 7.6 -1 3
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 162411 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 162411 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 142320 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 142320 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 81824 None 0 Human Functional pEC50 = 7.6 7.6 181 2
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 81824 None 0 Human Functional pEC50 = 7.6 7.6 181 2
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 180215 None 0 Rat Functional pEC50 = 7.6 7.6 -2 2
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 180215 None 0 Rat Functional pEC50 = 7.6 7.6 -2 2
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 112033 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 112033 None 0 Human Functional pEC50 = 6.6 6.6 3 2
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 80690 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 80690 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 80693 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 80693 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 156256 None 0 Human Functional pEC50 = 5.6 5.6 -2 2
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 156256 None 0 Human Functional pEC50 = 5.6 5.6 -2 2
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 162631 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 162631 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 137823 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 137823 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 156201 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 156201 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 184579 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 184579 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 145707 None 7 Human Functional pEC50 = 6.6 6.6 -20 3
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 145707 None 7 Human Functional pEC50 = 6.6 6.6 -20 3
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 163643 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 163643 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 163971 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 163971 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 203797 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 203797 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 161074 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 161074 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 161074 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 203569 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 203569 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 166933 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 166933 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 204584 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 204584 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 167310 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167310 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164931 None 0 Rat Functional pEC50 = 6.6 6.6 3 2
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 164931 None 0 Rat Functional pEC50 = 6.6 6.6 3 2
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 149630 None 0 Human Functional pEC50 = 6.6 6.6 9 2
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 149630 None 0 Human Functional pEC50 = 6.6 6.6 9 2
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 122571 None 4 Human Functional pEC50 = 5.6 5.6 - 1
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 122571 None 4 Human Functional pEC50 = 5.6 5.6 - 1
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 163849 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 163849 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164844 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164844 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 75640 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75640 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74084 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74084 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 183691 None 0 Human Functional pEC50 = 7.6 7.6 -10 3
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 183691 None 0 Human Functional pEC50 = 7.6 7.6 -10 3
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 164810 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
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 164810 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
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 167818 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 167818 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 167818 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 175295 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 175295 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 139825 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 139825 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 140078 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 140078 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 140078 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 58857 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 58857 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 175539 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 175539 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 203360 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 203360 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 70047 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 70047 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 157692 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 157692 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 161585 None 10 Human Functional pEC50 = 6.6 6.6 - 1
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 161585 None 10 Human Functional pEC50 = 6.6 6.6 - 1
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 157838 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 157838 None 0 Human Functional pEC50 = 5.6 5.6 2 2
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 156167 None 0 Mouse Functional pEC50 = 5.6 5.6 -9 2
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 156167 None 0 Mouse Functional pEC50 = 5.6 5.6 -9 2
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 157838 None 0 Mouse Functional pEC50 = 5.6 5.6 -2 2
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 157838 None 0 Mouse Functional pEC50 = 5.6 5.6 -2 2
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 158741 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 158741 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167634 None 0 Human Functional pEC50 = 6.6 6.6 -16 2
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 167634 None 0 Human Functional pEC50 = 6.6 6.6 -16 2
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 167634 None 0 Human Functional pEC50 = 6.6 6.6 -16 2
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 164093 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164093 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 165525 None 0 Human Functional pEC50 = 4.6 4.6 -354 2
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 165525 None 0 Human Functional pEC50 = 4.6 4.6 -354 2
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 62187 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 62187 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 171420 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 171420 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 61822 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 61822 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 95090 None 17 Human Functional pEC50 = 4.6 4.6 - 1
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 95090 None 17 Human Functional pEC50 = 4.6 4.6 - 1
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 167818 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167818 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167818 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 62176 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 62176 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 142257 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
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 142257 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
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 142257 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
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 142257 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
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 142257 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
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 142257 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
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 62171 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 62171 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 62188 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 62188 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 163722 None 0 Human Functional pEC50 = 7.6 7.6 2 2
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 163722 None 0 Human Functional pEC50 = 7.6 7.6 2 2
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 70049 None 11 Human Functional pEC50 = 7.6 7.6 - 1
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 70049 None 11 Human Functional pEC50 = 7.6 7.6 - 1
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 75857 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75857 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75858 None 4 Human Functional pEC50 = 7.6 7.6 - 1
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 75858 None 4 Human Functional pEC50 = 7.6 7.6 - 1
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 162933 None 0 Rat Functional pEC50 = 7.6 7.6 1 3
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 162933 None 0 Rat Functional pEC50 = 7.6 7.6 1 3
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 75858 None 4 Human Functional pEC50 = 7.6 7.6 - 1
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 75858 None 4 Human Functional pEC50 = 7.6 7.6 - 1
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 142320 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 142320 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 140124 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 140124 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 81751 None 25 Human Functional pEC50 = 7.6 7.6 - 1
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 81751 None 25 Human Functional pEC50 = 7.6 7.6 - 1
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 139818 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 139818 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 183067 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 183067 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 156367 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 156367 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 112026 None 0 Rat Functional pEC50 = 6.6 6.6 -29 2
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 112026 None 0 Rat Functional pEC50 = 6.6 6.6 -29 2
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 112025 None 0 Human Functional pEC50 = 5.6 5.6 3 2
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 112025 None 0 Human Functional pEC50 = 5.6 5.6 3 2
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 152804 None 0 Human Functional pEC50 = 5.6 5.6 -18 3
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 152804 None 0 Human Functional pEC50 = 5.6 5.6 -18 3
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 152288 None 0 Human Functional pEC50 = 5.6 5.6 -72 3
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 152288 None 0 Human Functional pEC50 = 5.6 5.6 -72 3
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 87515 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 87515 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 88025 None 0 Human Functional pEC50 = 6.6 6.6 208 2
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 88025 None 0 Human Functional pEC50 = 6.6 6.6 208 2
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 164256 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 164256 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 65358 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 65358 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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
145967091 164212 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux 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.2023.115267
CHEMBL4209845 164212 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux 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.2023.115267
71655226 90398 None 0 Human Functional pEC50 = 5.6 5.6 36 2
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 90398 None 0 Human Functional pEC50 = 5.6 5.6 36 2
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 142252 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 142252 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164828 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164828 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 156538 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 156538 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 161308 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 161308 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 161308 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 162559 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 162559 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164556 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 164556 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 122572 None 2 Human Functional pEC50 = 5.6 5.6 - 1
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 122572 None 2 Human Functional pEC50 = 5.6 5.6 - 1
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 203262 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 203262 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 183186 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 183186 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 81751 None 25 Human Functional pEC50 = 7.6 7.6 - 1
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 81751 None 25 Human Functional pEC50 = 7.6 7.6 - 1
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 77249 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 77249 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 77249 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 164716 None 0 Rat Functional pEC50 = 7.6 7.6 3 2
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 164716 None 0 Rat Functional pEC50 = 7.6 7.6 3 2
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 58849 None 0 Human Functional pEC50 = 6.6 6.6 11 2
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 58849 None 0 Human Functional pEC50 = 6.6 6.6 11 2
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 58871 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 58871 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 14918 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 14918 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 14918 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 191401 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 191401 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 70038 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 70038 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 161174 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 161174 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 161174 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 156167 None 0 Human Functional pEC50 = 6.6 6.6 9 2
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 156167 None 0 Human Functional pEC50 = 6.6 6.6 9 2
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 156848 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 156848 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 166764 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 166764 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 119200 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 119200 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 158245 None 0 Mouse Functional pEC50 = 5.6 5.6 1 2
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 158245 None 0 Mouse Functional pEC50 = 5.6 5.6 1 2
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 158299 None 0 Mouse Functional pEC50 = 5.6 5.6 -10 2
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 158299 None 0 Mouse Functional pEC50 = 5.6 5.6 -10 2
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 158478 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 2
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 158478 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 2
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 156236 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 156236 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 203478 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 203478 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 86566 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 86566 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 58858 None 0 Human Functional pEC50 = 6.6 6.6 107 2
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 58858 None 0 Human Functional pEC50 = 6.6 6.6 107 2
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 122573 None 1 Human Functional pEC50 = 5.6 5.6 - 1
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 122573 None 1 Human Functional pEC50 = 5.6 5.6 - 1
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 62188 None 0 Mouse Functional pEC50 = 6.6 6.6 -2 2
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 62188 None 0 Mouse Functional pEC50 = 6.6 6.6 -2 2
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 122574 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 122574 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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
82092005 195330 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 266 5 1 1 4.3 O=C(O)CC(c1ccc(-c2ccccc2)cc1)C1CC1 10.1016/j.ejmech.2022.114883
CHEMBL5401286 195330 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 266 5 1 1 4.3 O=C(O)CC(c1ccc(-c2ccccc2)cc1)C1CC1 10.1016/j.ejmech.2022.114883
145977404 163942 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 163942 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 58858 None 0 Human Functional pEC50 = 7.6 7.6 107 2
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 58858 None 0 Human Functional pEC50 = 7.6 7.6 107 2
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
10668 1953 None 20 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.ejmech.2022.114883
139600331 1953 None 20 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.ejmech.2022.114883
CHEMBL5169614 1953 None 20 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.ejmech.2022.114883
24857286 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 122732 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 122732 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 74073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74076 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74076 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 165282 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 165282 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 1624 None 46 Human Functional pEC50 = 7.6 7.6 -3 3
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 190218 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 190218 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 75642 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 75642 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 182423 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 182423 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 159231 None 0 Mouse Functional pEC50 = 6.6 6.6 -3 2
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 159231 None 0 Mouse Functional pEC50 = 6.6 6.6 -3 2
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 58872 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 58872 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 58874 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 58874 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 70044 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 70044 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 156345 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 156345 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 163728 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 163728 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 166822 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 166822 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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
170551864 195255 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 320 4 1 1 5.2 CC#CC(CC(=O)O)c1ccc(-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5399508 195255 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 320 4 1 1 5.2 CC#CC(CC(=O)O)c1ccc(-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.ejmech.2022.114883
145976136 163890 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 163890 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 65356 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 65356 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167121 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167121 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164920 None 0 Human Functional pEC50 = 7.6 7.6 1 2
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 164920 None 0 Human Functional pEC50 = 7.6 7.6 1 2
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 74072 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74072 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74128 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74128 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74129 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74129 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 162556 None 0 Rat Functional pEC50 = 7.6 7.6 1 3
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 162556 None 0 Rat Functional pEC50 = 7.6 7.6 1 3
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 173772 None 0 Rat Functional pEC50 = 7.6 7.6 -6 2
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 173772 None 0 Rat Functional pEC50 = 7.6 7.6 -6 2
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 180163 None 0 Rat Functional pEC50 = 7.6 7.6 -11 2
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 180163 None 0 Rat Functional pEC50 = 7.6 7.6 -11 2
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 1902 None 58 Human Functional pEC50 = 7.6 7.6 -1 3
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 1902 None 58 Human Functional pEC50 = 7.6 7.6 -1 3
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 1902 None 58 Human Functional pEC50 = 7.6 7.6 -1 3
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 164942 None 28 Human Functional pEC50 = 7.5 7.5 - 1
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 164942 None 28 Human Functional pEC50 = 7.5 7.5 - 1
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 1902 None 58 Human Functional pEC50 = 7.5 7.5 -1 3
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 1902 None 58 Human Functional pEC50 = 7.5 7.5 -1 3
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 1902 None 58 Human Functional pEC50 = 7.5 7.5 -1 3
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 167836 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 167836 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 167836 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 154557 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 154557 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 154557 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 158308 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 158308 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 167425 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 167425 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 182992 None 2 Human Functional pEC50 = 5.6 5.6 -13 3
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 182992 None 2 Human Functional pEC50 = 5.6 5.6 -13 3
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 90017 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 90017 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 62186 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 62186 None 0 Human Functional pEC50 = 5.6 5.6 -3 2
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 158476 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 158476 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 167355 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167355 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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
170551842 196575 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 306 5 1 1 5.1 CC#CC(CC(=O)O)c1ccc(-c2ccc(C(C)C)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5427077 196575 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 306 5 1 1 5.1 CC#CC(CC(=O)O)c1ccc(-c2ccc(C(C)C)cc2)cc1 10.1016/j.ejmech.2022.114883
145987167 167308 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167308 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 163870 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 163870 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 76817 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 76817 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 163120 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 163120 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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
172469880 197089 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 430 8 1 5 3.9 COc1ccc(F)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c1 10.1016/j.ejmech.2023.115267
CHEMBL5438434 197089 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 430 8 1 5 3.9 COc1ccc(F)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c1 10.1016/j.ejmech.2023.115267
57414678 75653 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 75653 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 163954 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
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 163954 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
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 119194 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119194 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119194 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119194 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 180236 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 180236 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 75862 None 1 Human Functional pEC50 = 7.5 7.5 - 1
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 75862 None 1 Human Functional pEC50 = 7.5 7.5 - 1
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 74086 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 74086 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 142229 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 142229 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular 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.2023.115267
6484 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular 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.2023.115267
CHEMBL1829174 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular 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.2023.115267
DB12491 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular 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.2023.115267
24857286 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 174164 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 174164 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 75639 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 75639 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 75645 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 75645 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 158099 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 158099 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 111723 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
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 111723 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
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
170551877 196273 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 308 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(-c2ccc(OC)c(C)c2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5420293 196273 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 308 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(-c2ccc(OC)c(C)c2)cc1 10.1016/j.ejmech.2022.114883
145986046 166007 None 0 Human Functional pEC50 = 4.5 4.5 -19 2
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 166007 None 0 Human Functional pEC50 = 4.5 4.5 -19 2
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 65362 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 65362 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 146351 None 0 Human Functional pEC50 = 5.5 5.5 -104 3
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 146351 None 0 Human Functional pEC50 = 5.5 5.5 -104 3
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
170551840 195692 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 278 4 1 1 4.2 CC#CC(CC(=O)O)c1ccc(-c2ccc(C)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5409222 195692 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 278 4 1 1 4.2 CC#CC(CC(=O)O)c1ccc(-c2ccc(C)cc2)cc1 10.1016/j.ejmech.2022.114883
134130787 142353 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 142353 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 150681 None 25 Human Functional pEC50 = 8.5 8.5 -14 3
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 150681 None 25 Human Functional pEC50 = 8.5 8.5 -14 3
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 169678 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 169678 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 175670 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 175670 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 171181 None 0 Human Functional pEC50 = 8.5 8.5 -4 2
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 171181 None 0 Human Functional pEC50 = 8.5 8.5 -4 2
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 142257 None 0 Human Functional pEC50 = 8.5 8.5 -15 2
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 142257 None 0 Human Functional pEC50 = 8.5 8.5 -15 2
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 142257 None 0 Human Functional pEC50 = 8.5 8.5 -15 2
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 142257 None 0 Human Functional pEC50 = 8.5 8.5 -15 2
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 142257 None 0 Human Functional pEC50 = 8.5 8.5 -15 2
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 142257 None 0 Human Functional pEC50 = 8.5 8.5 -15 2
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 111315 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 111315 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 112016 None 0 Human Functional pEC50 = 8.5 8.5 10 2
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 112016 None 0 Human Functional pEC50 = 8.5 8.5 10 2
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 80828 None 25 Human Functional pEC50 = 8.5 8.5 -8 2
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 80828 None 25 Human Functional pEC50 = 8.5 8.5 -8 2
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 182566 None 0 Human Functional pEC50 = 8.5 8.5 -8 3
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 182566 None 0 Human Functional pEC50 = 8.5 8.5 -8 3
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 111867 None 25 Human Functional pEC50 = 8.4 8.4 - 1
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 111867 None 25 Human Functional pEC50 = 8.4 8.4 - 1
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 119197 None 6 Human Functional pEC50 = 8.4 8.4 2 2
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 119197 None 6 Human Functional pEC50 = 8.4 8.4 2 2
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 119197 None 6 Human Functional pEC50 = 8.4 8.4 2 2
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 119197 None 6 Human Functional pEC50 = 8.4 8.4 2 2
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 112020 None 0 Human Functional pEC50 = 8.4 8.4 4 2
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 112020 None 0 Human Functional pEC50 = 8.4 8.4 4 2
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 111866 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 111866 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 119188 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 119188 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 119188 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 119188 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 170455 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 170455 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 58867 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58867 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58868 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58868 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58878 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58878 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 74129 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 74129 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 164152 None 0 Human Functional pEC50 = 7.5 7.5 -5 2
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 164152 None 0 Human Functional pEC50 = 7.5 7.5 -5 2
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 122740 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 122740 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58866 None 0 Human Functional pEC50 = 7.5 7.5 660 2
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 58866 None 0 Human Functional pEC50 = 7.5 7.5 660 2
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 163750 None 0 Rat Functional pEC50 = 7.5 7.5 -1 2
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 163750 None 0 Rat Functional pEC50 = 7.5 7.5 -1 2
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 142207 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 142207 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90029 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90029 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90013 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90013 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58845 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 58845 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 58870 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 58870 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 122525 None 3 Human Functional pEC50 = 6.5 6.5 - 1
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 122525 None 3 Human Functional pEC50 = 6.5 6.5 - 1
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 176305 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 176305 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 122575 None 2 Human Functional pEC50 = 5.5 5.5 - 1
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 122575 None 2 Human Functional pEC50 = 5.5 5.5 - 1
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 162856 None 0 Human Functional pEC50 = 5.5 5.5 -64 3
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 162856 None 0 Human Functional pEC50 = 5.5 5.5 -64 3
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 159328 None 0 Mouse Functional pEC50 = 5.5 5.5 -9 2
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 159328 None 0 Mouse Functional pEC50 = 5.5 5.5 -9 2
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 167777 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167777 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167777 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 164341 None 0 Rat Functional pEC50 = 6.5 6.5 4 2
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 164341 None 0 Rat Functional pEC50 = 6.5 6.5 4 2
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 122579 None 1 Human Functional pEC50 = 4.5 4.5 - 1
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 122579 None 1 Human Functional pEC50 = 4.5 4.5 - 1
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 143375 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 143375 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 76861 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 76861 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 166686 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 166686 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 163057 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 163057 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 62167 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 62167 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 156026 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 156026 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167269 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167269 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 204901 None 2 Human Functional pEC50 = 6.5 6.5 - 1
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 204901 None 2 Human Functional pEC50 = 6.5 6.5 - 1
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 166487 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 166487 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 162505 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 162505 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 86575 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 86575 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164782 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 164782 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 119190 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119190 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119190 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119190 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 62182 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 62182 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 77248 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 77248 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 77248 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 162933 None 0 Mouse Functional pEC50 = 7.5 7.5 -1 3
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 162933 None 0 Mouse Functional pEC50 = 7.5 7.5 -1 3
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 180749 None 0 Rat Functional pEC50 = 7.5 7.5 -4 2
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 180749 None 0 Rat Functional pEC50 = 7.5 7.5 -4 2
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 58846 None 0 Human Functional pEC50 = 6.5 6.5 77 2
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 58846 None 0 Human Functional pEC50 = 6.5 6.5 77 2
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 164410 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164410 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 159328 None 0 Human Functional pEC50 = 6.5 6.5 9 2
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 159328 None 0 Human Functional pEC50 = 6.5 6.5 9 2
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 159374 None 0 Human Functional pEC50 = 6.5 6.5 4 2
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 159374 None 0 Human Functional pEC50 = 6.5 6.5 4 2
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 112021 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
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 112021 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
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 122735 None 1 Human Functional pEC50 = 5.5 5.5 - 1
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 122735 None 1 Human Functional pEC50 = 5.5 5.5 - 1
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
172455954 196401 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 395 7 1 4 4.1 Cc1cncc(C)c1-c1cccc(COc2ccc([S+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
CHEMBL5422997 196401 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 395 7 1 4 4.1 Cc1cncc(C)c1-c1cccc(COc2ccc([S+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
90372458 142311 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 142311 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 65370 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 65370 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 75952 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 75952 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 363 None 48 Human Functional pEC50 = 5.5 5.5 1 3
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 204855 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 204855 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 143349 None 0 Human Functional pEC50 = 5.5 5.5 -22 3
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 143349 None 0 Human Functional pEC50 = 5.5 5.5 -22 3
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 58865 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58865 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 3885 None 44 Human Functional pEC50 = 7.5 7.5 6 9
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 3885 None 44 Human Functional pEC50 = 7.5 7.5 6 9
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 3885 None 44 Human Functional pEC50 = 7.5 7.5 6 9
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 112018 None 0 Human Functional pEC50 = 7.5 7.5 20 2
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 112018 None 0 Human Functional pEC50 = 7.5 7.5 20 2
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 75856 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 75856 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 183561 None 0 Human Functional pEC50 = 7.5 7.5 -9 3
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 183561 None 0 Human Functional pEC50 = 7.5 7.5 -9 3
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 164249 None 0 Rat Functional pEC50 = 7.5 7.5 2 2
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 164249 None 0 Rat Functional pEC50 = 7.5 7.5 2 2
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 164676 None 0 Rat Functional pEC50 = 7.5 7.5 1 2
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 164676 None 0 Rat Functional pEC50 = 7.5 7.5 1 2
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 179974 None 0 Rat Functional pEC50 = 7.5 7.5 -15 2
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 179974 None 0 Rat Functional pEC50 = 7.5 7.5 -15 2
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 3885 None 44 Human Functional pEC50 = 7.5 7.5 6 9
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 3885 None 44 Human Functional pEC50 = 7.5 7.5 6 9
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 3885 None 44 Human Functional pEC50 = 7.5 7.5 6 9
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 140078 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 140078 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 140078 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 58861 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 58861 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 158878 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 158878 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 112030 None 0 Rat Functional pEC50 = 6.5 6.5 -31 2
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 112030 None 0 Rat Functional pEC50 = 6.5 6.5 -31 2
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 95057 None 7 Human Functional pEC50 = 5.5 5.5 - 1
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 95057 None 7 Human Functional pEC50 = 5.5 5.5 - 1
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 165395 None 45 Human Functional pEC50 = 5.5 5.5 - 1
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 165395 None 45 Human Functional pEC50 = 5.5 5.5 - 1
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 70033 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 70033 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 122751 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 122751 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 159217 None 0 Mouse Functional pEC50 = 5.5 5.5 -8 2
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 159217 None 0 Mouse Functional pEC50 = 5.5 5.5 -8 2
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
170551849 195200 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 304 5 1 1 4.8 CC#CC(CC(=O)O)c1ccc(-c2ccc(C3CC3)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5398640 195200 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 304 5 1 1 4.8 CC#CC(CC(=O)O)c1ccc(-c2ccc(C3CC3)cc2)cc1 10.1016/j.ejmech.2022.114883
137640417 157193 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 157193 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 76749 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 76749 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 190985 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 190985 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 171334 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 171334 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164392 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 164392 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167753 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 167753 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 167753 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 167840 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167840 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167840 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 74072 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 74072 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 74087 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 74087 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 164920 None 0 Rat Functional pEC50 = 7.5 7.5 -1 2
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 164920 None 0 Rat Functional pEC50 = 7.5 7.5 -1 2
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 90402 None 0 Human Functional pEC50 = 7.5 7.5 47 2
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 90402 None 0 Human Functional pEC50 = 7.5 7.5 47 2
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 140023 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 140023 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 1624 None 46 Human Functional pEC50 = 7.5 7.5 -3 3
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 119199 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 119199 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 158411 None 0 Mouse Functional pEC50 = 6.5 6.5 -4 2
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 158411 None 0 Mouse Functional pEC50 = 6.5 6.5 -4 2
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 164261 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164261 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 61820 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 61820 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 175489 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 175489 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 203527 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 203527 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164099 None 3 Human Functional pEC50 = 5.5 5.5 -36 5
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 164099 None 3 Human Functional pEC50 = 5.5 5.5 -36 5
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 161194 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 161194 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 161194 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 151536 None 0 Human Functional pEC50 = 5.5 5.5 -100 3
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 151536 None 0 Human Functional pEC50 = 5.5 5.5 -100 3
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 86584 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 86584 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 58850 None 0 Human Functional pEC50 = 7.5 7.5 14 2
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 58850 None 0 Human Functional pEC50 = 7.5 7.5 14 2
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 181546 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 181546 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 171297 None 0 Rat Functional pEC50 = 7.5 7.5 -2 2
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 171297 None 0 Rat Functional pEC50 = 7.5 7.5 -2 2
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 90008 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90008 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 61832 None 27 Human Functional pEC50 = 7.5 7.5 -1 3
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 61832 None 27 Human Functional pEC50 = 7.5 7.5 -1 3
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 58866 None 0 Human Functional pEC50 = 7.5 7.5 660 2
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 58866 None 0 Human Functional pEC50 = 7.5 7.5 660 2
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 138814 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 138814 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 191169 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 191169 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 159749 None 0 Human Functional pEC50 = 6.5 6.5 13 2
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 159749 None 0 Human Functional pEC50 = 6.5 6.5 13 2
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 166658 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 166658 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 157572 None 0 Mouse Functional pEC50 = 5.5 5.5 -17 2
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 157572 None 0 Mouse Functional pEC50 = 5.5 5.5 -17 2
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 80829 None 2 Human Functional pEC50 = 4.5 4.5 - 1
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 80829 None 2 Human Functional pEC50 = 4.5 4.5 - 1
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 167102 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167102 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 86571 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 86571 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 165834 None 0 Human Functional pEC50 = 5.5 5.5 6 2
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 165834 None 0 Human Functional pEC50 = 5.5 5.5 6 2
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 142206 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 142206 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 62167 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 62167 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 58869 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58869 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 112035 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 112035 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 122749 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 122749 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 112035 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 112035 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 167709 None 5 Human Functional pEC50 = 7.5 7.5 -10 2
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 167709 None 5 Human Functional pEC50 = 7.5 7.5 -10 2
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 167709 None 5 Human Functional pEC50 = 7.5 7.5 -10 2
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 142320 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 142320 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 86567 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 86567 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90400 None 0 Human Functional pEC50 = 7.5 7.5 223 2
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 90400 None 0 Human Functional pEC50 = 7.5 7.5 223 2
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 90035 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 90035 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 58882 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 58882 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 58883 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 58883 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 165841 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 165841 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 159510 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 159510 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 164099 None 3 Mouse Functional pEC50 = 5.5 5.5 -38 5
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 164099 None 3 Mouse Functional pEC50 = 5.5 5.5 -38 5
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
172455723 196124 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 530 12 1 6 4.6 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc([S@+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
CHEMBL5417303 196124 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 530 12 1 6 4.6 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc([S@+]([O-])CC(=O)O)cc2)c1 10.1016/j.ejmech.2023.115267
25150011 186795 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 186795 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 140297 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 140297 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 76299 None 0 Human Functional pEC50 = 5.5 5.5 -15 2
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 76299 None 0 Human Functional pEC50 = 5.5 5.5 -15 2
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 175049 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 175049 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 137757 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 137757 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 154252 None 0 Human Functional pEC50 = 5.5 5.5 -123 3
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 154252 None 0 Human Functional pEC50 = 5.5 5.5 -123 3
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 167342 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 167342 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 122768 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 122768 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167753 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167753 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167753 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 142214 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 142214 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 173773 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 173773 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 164178 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 164178 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 76011 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 76011 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 90014 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 90014 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 172111 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 172111 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 190562 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 190562 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 119189 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 119189 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 69873 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 69873 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 119189 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 119189 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 159217 None 0 Human Functional pEC50 = 6.4 6.4 8 2
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 159217 None 0 Human Functional pEC50 = 6.4 6.4 8 2
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 156226 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 156226 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 156997 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 156997 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 182992 None 2 Human Functional pEC50 = 6.4 6.4 -13 3
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 182992 None 2 Human Functional pEC50 = 6.4 6.4 -13 3
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 58847 None 2 Human Functional pEC50 = 5.4 5.4 -15 2
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 58847 None 2 Human Functional pEC50 = 5.4 5.4 -15 2
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 58847 None 2 Human Functional pEC50 = 5.4 5.4 -15 2
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 94628 None 7 Human Functional pEC50 = 5.4 5.4 - 1
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 94628 None 7 Human Functional pEC50 = 5.4 5.4 - 1
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 152463 None 0 Human Functional pEC50 = 5.4 5.4 -218 2
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 152463 None 0 Human Functional pEC50 = 5.4 5.4 -218 2
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 1455 None 44 Human Functional pEC50 = 4.4 4.4 -14 2
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 1455 None 44 Human Functional pEC50 = 4.4 4.4 -14 2
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 1455 None 44 Human Functional pEC50 = 4.4 4.4 -14 2
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 1455 None 44 Human Functional pEC50 = 4.4 4.4 -14 2
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 1455 None 44 Human Functional pEC50 = 4.4 4.4 -14 2
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 1455 None 44 Human Functional pEC50 = 4.4 4.4 -14 2
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 156034 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 156034 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 166607 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 166607 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 163974 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 163974 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 90410 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 90410 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 61819 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 61819 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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
170551853 196649 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 254 4 1 2 3.5 CC#CC(CC(=O)O)c1ccc(-c2ccco2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5428940 196649 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 254 4 1 2 3.5 CC#CC(CC(=O)O)c1ccc(-c2ccco2)cc1 10.1016/j.ejmech.2022.114883
145974382 164635 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164635 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 140380 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 140380 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164004 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 164004 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 181768 None 0 Human Functional pEC50 = 7.4 7.4 5 2
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 181768 None 0 Human Functional pEC50 = 7.4 7.4 5 2
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 139106 None 0 Human Functional pEC50 = 7.4 7.4 707 2
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 139106 None 0 Human Functional pEC50 = 7.4 7.4 707 2
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 140078 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 140078 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 140078 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 162637 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 162637 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 111319 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 111319 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 80701 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 80701 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 111723 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 111723 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 111723 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 111723 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 159577 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 159577 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 62183 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 2
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 62183 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 2
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 90413 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 90413 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 185538 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 185538 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 185538 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 185538 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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
170551863 196557 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 312 5 1 2 4.1 CC#CC(CC(=O)O)c1ccc(-c2ccc(OC)c(F)c2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5426547 196557 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 312 5 1 2 4.1 CC#CC(CC(=O)O)c1ccc(-c2ccc(OC)c(F)c2)cc1 10.1016/j.ejmech.2022.114883
170551837 196160 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(-c2ccc(OCc3ccccc3)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5417866 196160 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(-c2ccc(OCc3ccccc3)cc2)cc1 10.1016/j.ejmech.2022.114883
145990731 167116 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167116 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 156154 None 0 Human Functional pEC50 = 5.4 5.4 -63 2
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 156154 None 0 Human Functional pEC50 = 5.4 5.4 -63 2
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 58854 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 58854 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 181568 None 7 Mouse Functional pEC50 = 7.4 7.4 1 3
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 181568 None 7 Mouse Functional pEC50 = 7.4 7.4 1 3
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 112016 None 0 Rat Functional pEC50 = 7.4 7.4 -10 2
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 112016 None 0 Rat Functional pEC50 = 7.4 7.4 -10 2
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 86555 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 86555 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 90406 None 0 Human Functional pEC50 = 7.4 7.4 83 2
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 90406 None 0 Human Functional pEC50 = 7.4 7.4 83 2
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 167836 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167836 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167836 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 74076 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 74076 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 170684 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 170684 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 90036 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 90036 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 139974 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 139974 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 143838 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 143838 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166737 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166737 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 122729 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 122729 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 159206 None 0 Mouse Functional pEC50 = 5.4 5.4 1 2
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 159206 None 0 Mouse Functional pEC50 = 5.4 5.4 1 2
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 80827 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 80827 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 167664 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 167664 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 167664 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 167847 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 167847 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 167847 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 159228 None 0 Human Functional pEC50 = 5.4 5.4 -7 2
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 159228 None 0 Human Functional pEC50 = 5.4 5.4 -7 2
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 166550 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 166550 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 161276 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 161276 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 161276 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167446 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167446 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 175388 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 175388 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 139271 None 0 Human Functional pEC50 = 6.4 6.4 26 2
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 139271 None 0 Human Functional pEC50 = 6.4 6.4 26 2
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 115600 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 115600 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 65357 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 65357 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 75643 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 75643 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 164520 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 164520 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 162556 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 162556 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 74082 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 74082 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 182325 None 0 Human Functional pEC50 = 7.4 7.4 -4 3
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 182325 None 0 Human Functional pEC50 = 7.4 7.4 -4 3
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 163720 None 0 Rat Functional pEC50 = 7.4 7.4 -3 2
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 163720 None 0 Rat Functional pEC50 = 7.4 7.4 -3 2
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 1624 None 46 Rat Functional pEC50 = 7.4 7.4 -28 3
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 1624 None 46 Rat Functional pEC50 = 7.4 7.4 -28 3
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 1624 None 46 Rat Functional pEC50 = 7.4 7.4 -28 3
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 1624 None 46 Rat Functional pEC50 = 7.4 7.4 -28 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 90030 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 90030 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 165309 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 165309 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88062 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88062 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 86559 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 86559 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 75618 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 75618 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 190422 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 190422 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 191517 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 191517 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 158625 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 158625 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 162636 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 162636 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 80828 None 25 Human Functional pEC50 = 6.4 6.4 -8 2
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 80828 None 25 Human Functional pEC50 = 6.4 6.4 -8 2
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 80828 None 25 Human Functional pEC50 = 6.4 6.4 -8 2
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 80828 None 25 Human Functional pEC50 = 6.4 6.4 -8 2
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 157124 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 157124 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 62181 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
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 62181 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
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
172443765 195039 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 405 7 1 5 4.0 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc([S+]([O-])CC(=O)O)cc1 10.1016/j.ejmech.2023.115267
CHEMBL5395377 195039 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
ChEMBL 405 7 1 5 4.0 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc([S+]([O-])CC(=O)O)cc1 10.1016/j.ejmech.2023.115267
155530636 171638 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 171638 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 88023 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 88023 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166561 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 166561 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 76908 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 76908 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 88067 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 88067 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 88068 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 88068 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 156154 None 0 Human Functional pEC50 = 5.4 5.4 -63 2
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 156154 None 0 Human Functional pEC50 = 5.4 5.4 -63 2
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 159228 None 0 Human Functional pEC50 = 5.4 5.4 -7 2
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 159228 None 0 Human Functional pEC50 = 5.4 5.4 -7 2
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 191783 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 191783 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 163730 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 163730 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 163910 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 163910 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 163637 None 0 Rat Functional pEC50 = 8.4 8.4 2 2
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 163637 None 0 Rat Functional pEC50 = 8.4 8.4 2 2
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 164909 None 0 Rat Functional pEC50 = 8.4 8.4 1 2
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 164909 None 0 Rat Functional pEC50 = 8.4 8.4 1 2
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 176215 None 0 Rat Functional pEC50 = 8.4 8.4 15 2
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 176215 None 0 Rat Functional pEC50 = 8.4 8.4 15 2
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 183092 None 0 Human Functional pEC50 = 8.4 8.4 -13 3
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 183092 None 0 Human Functional pEC50 = 8.4 8.4 -13 3
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 182920 None 0 Human Functional pEC50 = 8.4 8.4 -4 3
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 182920 None 0 Human Functional pEC50 = 8.4 8.4 -4 3
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 167823 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 167823 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 167823 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 141288 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 141288 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 75854 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 75854 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 183086 None 0 Human Functional pEC50 = 8.4 8.4 3 2
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 183086 None 0 Human Functional pEC50 = 8.4 8.4 3 2
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 175388 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 175388 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 182704 None 0 Human Functional pEC50 = 8.3 8.3 -11 3
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 182704 None 0 Human Functional pEC50 = 8.3 8.3 -11 3
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 185151 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 185151 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 171388 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 171388 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 141103 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 141103 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 183561 None 0 Human Functional pEC50 = 8.3 8.3 -9 3
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 183561 None 0 Human Functional pEC50 = 8.3 8.3 -9 3
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 172906 None 0 Rat Functional pEC50 = 8.3 8.3 1 2
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 172906 None 0 Rat Functional pEC50 = 8.3 8.3 1 2
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 58851 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 58851 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 169628 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 169628 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 75846 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 75846 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 86554 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 86554 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 65373 None 10 Human Functional pEC50 = 7.4 7.4 - 1
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 65373 None 10 Human Functional pEC50 = 7.4 7.4 - 1
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 191782 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 191782 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 173783 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 173783 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 122576 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 122576 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 80692 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 80692 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167640 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167640 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167640 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 142206 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 142206 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 156267 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 156267 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 203544 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 203544 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 166539 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 166539 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 162411 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 162411 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 142207 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 142207 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 76303 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 76303 None 0 Human Functional pEC50 = 6.4 6.4 1 2
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 65347 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 65347 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 62178 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 62178 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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
170551871 195230 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 332 4 1 1 5.0 CC#CC(CC(=O)O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5399210 195230 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 332 4 1 1 5.0 CC#CC(CC(=O)O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2022.114883
46854655 395 None 35 Human Functional pEC50 = 7.4 7.4 -8 3
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 395 None 35 Human Functional pEC50 = 7.4 7.4 -8 3
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 395 None 35 Human Functional pEC50 = 7.4 7.4 -8 3
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 171956 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 171956 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 162557 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 162557 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 1624 None 46 Human Functional pEC50 = 7.4 7.4 -3 3
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 170101 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 170101 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 154602 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 154602 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 154602 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 158365 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 158365 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 181488 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 181488 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 137802 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 137802 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164480 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164480 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 142229 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 142229 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 86577 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 86577 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 139085 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 139085 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 88025 None 0 Human Functional pEC50 = 6.4 6.4 208 2
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 88025 None 0 Human Functional pEC50 = 6.4 6.4 208 2
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 162284 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 162284 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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
151213992 196136 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 264 4 1 1 3.9 CC#CC(CC(=O)O)c1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2022.114883
CHEMBL5417455 196136 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay
ChEMBL 264 4 1 1 3.9 CC#CC(CC(=O)O)c1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2022.114883
134135852 144469 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 144469 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 62174 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 62174 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 163018 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 163018 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 162556 None 0 Mouse Functional pEC50 = 7.4 7.4 -1 3
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 162556 None 0 Mouse Functional pEC50 = 7.4 7.4 -1 3
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 65375 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 65375 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 80702 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 80702 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 112021 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 112021 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 191770 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 191770 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 145730 None 0 Human Functional pEC50 = 5.4 5.4 -9 3
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 145730 None 0 Human Functional pEC50 = 5.4 5.4 -9 3
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 86557 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 86557 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 164374 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 164374 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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)(