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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ligand		 Fold
selectivity		 Tested
GPCRs		 Species

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

 Assay
Description		 Source

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weight		 Rot
Bonds		 H don

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 DOI
164616580 185325 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4859651 185325 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
17754443 180250 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at GPR40 expressed in CHO cells by FLIPR assayAgonist activity at GPR40 expressed in CHO cells by FLIPR assay
ChEMBL 370 3 1 3 4.7 O=C(O)[C@@H]1[C@H]2c3ccc(Oc4ccc(C(F)(F)F)cc4Cl)cc3O[C@H]21 10.1016/j.bmcl.2008.10.085
CHEMBL475027 180250 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at GPR40 expressed in CHO cells by FLIPR assayAgonist activity at GPR40 expressed in CHO cells by FLIPR assay
ChEMBL 370 3 1 3 4.7 O=C(O)[C@@H]1[C@H]2c3ccc(Oc4ccc(C(F)(F)F)cc4Cl)cc3O[C@H]21 10.1016/j.bmcl.2008.10.085
155551422 173965 0 None -15 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4541658 173965 0 None -15 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
134465732 171473 0 None -1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4463571 171473 0 None -1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
164615766 185007 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1cc(Cl)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4854804 185007 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1cc(Cl)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
134465794 171076 0 None -4 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 171076 0 None -4 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
91827421 149257 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 529 9 1 3 7.0 CC(c1cc(C(F)(F)F)ccc1C(F)(F)F)N1CC(COc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)C1 10.1016/j.bmcl.2016.10.074
CHEMBL3944424 149257 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 529 9 1 3 7.0 CC(c1cc(C(F)(F)F)ccc1C(F)(F)F)N1CC(COc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)C1 10.1016/j.bmcl.2016.10.074
155551422 173965 0 None 15 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4541658 173965 0 None 15 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
134465794 171076 0 None 4 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 171076 0 None 4 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
24857286 1622 72 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
164613862 184604 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1c(Cl)cccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4848974 184604 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1c(Cl)cccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
89671280 146686 0 None 10 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3923877 146686 0 None 10 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmcl.2016.10.074
134465732 171473 0 None 1 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4463571 171473 0 None 1 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
164617551 185309 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c(C)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4859407 185309 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c(C)c1 10.1021/acs.jmedchem.1c00031
142738582 184518 0 None 42 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4847662 184518 0 None 42 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
137333449 167607 5 None 10 2 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165147 167607 5 None 10 2 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301092 167607 5 None 10 2 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
86288852 111252 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265149 111252 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
52936292 182108 27 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
164619456 186147 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1cccc(C)c1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4872298 186147 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1cccc(C)c1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
164610330 185195 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 357 4 2 1 4.9 Cc1cc(Br)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4857550 185195 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 357 4 2 1 4.9 Cc1cc(Br)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
137333449 167607 5 None -10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165147 167607 5 None -10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301092 167607 5 None -10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
118638016 167650 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163182 167650 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301725 167650 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
134465785 176109 0 None -15 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 176109 0 None -15 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
68194465 183304 0 None -3 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 183304 0 None -3 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
118151370 159101 0 None 7 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 159101 0 None 7 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
155549083 173666 0 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4534836 173666 0 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
118623101 167587 0 None -12 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167587 0 None -12 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167587 0 None -12 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
90357232 142250 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884803 142250 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
51049992 145617 5 None -23 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None -23 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
118638009 167651 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4160527 167651 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301726 167651 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
118623101 167587 0 None 12 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167587 0 None 12 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167587 0 None 12 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
15604310 111799 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287571 111799 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
46854655 395 47 None -8 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None -8 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None -8 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
68194476 182885 0 None -6 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182885 0 None -6 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
118638010 167563 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167563 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167563 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
90372613 167742 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167742 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167742 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
90655860 111247 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265144 111247 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
118637996 142168 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 142168 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 142168 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
118637996 142168 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 142168 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 142168 0 None -15 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
162668378 182505 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 182505 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
90372625 167719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
145980154 166635 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 372 9 1 3 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4281133 166635 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 372 9 1 3 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
44572097 189549 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 3 6.1 CC#CC(CC(=O)O)c1ccc(OC2CCc3cc(-c4cccs4)ccc32)cc1 10.1016/j.bmcl.2008.10.085
CHEMBL514337 189549 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 3 6.1 CC#CC(CC(=O)O)c1ccc(OC2CCc3cc(-c4cccs4)ccc32)cc1 10.1016/j.bmcl.2008.10.085
134144239 150465 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 543 8 1 3 7.9 COc1ccc(F)c(-c2ccc(Cc3cccc(N4C[C@H](c5cccc(Cl)c5)C[C@@H]4CC(=O)O)c3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3954235 150465 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 543 8 1 3 7.9 COc1ccc(F)c(-c2ccc(Cc3cccc(N4C[C@H](c5cccc(Cl)c5)C[C@@H]4CC(=O)O)c3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
131986136 163623 0 None 3 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203795 163623 0 None 3 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
3367 1155 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1016/j.bmcl.2009.10.052
46216676 1155 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1016/j.bmcl.2009.10.052
CHEMBL604126 1155 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1016/j.bmcl.2009.10.052
46232307 202564 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C2CC2C(=O)O)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL611821 202564 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C2CC2C(=O)O)cc1 10.1016/j.bmcl.2009.10.052
90644300 111965 0 None 31 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288358 111965 0 None 31 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
23111694 74057 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
CHEMBL2022256 74057 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
68194237 182204 0 None -4 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 182204 0 None -4 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
131986401 163982 0 None 1 2 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4208095 163982 0 None 1 2 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
134140733 147162 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 358 8 1 3 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCCOc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3927863 147162 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 358 8 1 3 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCCOc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2016.10.074
134137874 152979 0 None 1995 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISAAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152979 0 None 1995 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISAAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152979 0 None 1995 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISAAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 formation after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
44409843 140403 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380884 140403 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
57706620 163882 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 11 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)CC4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4206969 163882 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 11 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)CC4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
57707179 164503 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 534 10 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4214632 164503 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 534 10 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
46854655 395 47 None -8 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/jm2005699
6485 395 47 None -8 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/jm2005699
CHEMBL1829173 395 47 None -8 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/jm2005699
1050 1900 94 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2009.10.052
11595431 1900 94 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2009.10.052
CHEMBL207881 1900 94 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2009.10.052
122185437 122675 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 11 1 5 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OCOC)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604043 122675 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 11 1 5 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OCOC)c2)cc1 10.1016/j.bmc.2015.07.028
121294359 179584 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 14 1 7 6.4 COc1ccc(C(=O)N(CC(C)(C)OC)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4742099 179584 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 14 1 7 6.4 COc1ccc(C(=O)N(CC(C)(C)OC)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
121294251 179955 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 536 11 1 5 6.1 COc1ccc(C(=O)N(C)CC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4746614 179955 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 536 11 1 5 6.1 COc1ccc(C(=O)N(C)CC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
90151370 155913 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 525 7 1 6 5.6 COc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4060840 155913 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 525 7 1 6 5.6 COc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
145987015 167040 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#CC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4288867 167040 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#CC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
54583582 62162 0 None -2 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777872 62162 0 None -2 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
44409728 75050 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.4 CC(Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)C(=O)O 10.1016/j.bmcl.2006.01.007
CHEMBL203520 75050 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.4 CC(Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)C(=O)O 10.1016/j.bmcl.2006.01.007
44409670 75960 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 461 8 2 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205263 75960 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 461 8 2 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
20331242 87824 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL233835 87824 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2006.12.084
58319107 86545 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 326 4 1 1 4.8 O=C(O)CCc1ccc(C#Cc2ccccc2-c2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315546 86545 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 326 4 1 1 4.8 O=C(O)CCc1ccc(C#Cc2ccccc2-c2ccccc2)cc1 10.1021/jm301470a
71562312 86556 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 4 1 1 3.5 O=C(O)CCCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315557 86556 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 4 1 1 3.5 O=C(O)CCCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
146314511 180619 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 508 13 1 5 6.0 COc1ccc(CN(C)CC(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4754718 180619 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 508 13 1 5 6.0 COc1ccc(CN(C)CC(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
23136477 58828 3 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL1688455 58828 3 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL4213909 58828 3 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
137643339 158041 0 None -26 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4085843 158041 0 None -26 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
46232308 201084 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL602867 201084 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
134130696 142135 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 142135 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
142738543 162105 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 349 5 2 2 4.8 O=C(O)CCc1ccc2[nH]c(-c3ccccc3OC(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4161206 162105 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 349 5 2 2 4.8 O=C(O)CCc1ccc2[nH]c(-c3ccccc3OC(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
127046664 139824 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 453 9 1 5 6.0 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC2CCCC2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798992 139824 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 453 9 1 5 6.0 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC2CCCC2)c1 10.1016/j.ejmech.2016.03.054
155549391 173835 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 466 7 1 5 5.0 O=C(O)CC1(c2ccc(OC[C@H]3COc4ccc(-c5ccc(Cl)cc5)cc4O3)cc2)COC1 10.1016/j.bmcl.2019.01.014
CHEMBL4538821 173835 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 466 7 1 5 5.0 O=C(O)CC1(c2ccc(OC[C@H]3COc4ccc(-c5ccc(Cl)cc5)cc4O3)cc2)COC1 10.1016/j.bmcl.2019.01.014
145970056 164771 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 475 9 2 5 5.3 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccccc3F)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4218014 164771 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 475 9 2 5 5.3 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccccc3F)s2)cc1 10.1016/j.ejmech.2017.09.019
137643339 158041 0 None -26 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4085843 158041 0 None -26 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2017.01.034
122193743 123970 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 1 5 5.2 COCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628763 123970 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 1 5 5.2 COCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
145969681 164987 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 392 6 1 5 4.2 Cc1nn(C)c(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4225643 164987 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 392 6 1 5 4.2 Cc1nn(C)c(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
145984886 166437 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 415 7 1 6 4.2 O=C(O)CC(c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1)c1cnco1 10.1016/j.bmc.2018.10.019
CHEMBL4277516 166437 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 415 7 1 6 4.2 O=C(O)CC(c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1)c1cnco1 10.1016/j.bmc.2018.10.019
168290747 191921 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 420 10 1 5 4.9 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)cc3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5200259 191921 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 420 10 1 5 4.9 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)cc3)c2)cc1 10.1016/j.ejmech.2021.114061
90356885 167533 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 167533 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 167533 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
53248847 62145 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 62145 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
134150245 152243 0 None -117 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 374 7 1 3 5.1 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3968947 152243 0 None -117 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 374 7 1 3 5.1 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
118638016 167650 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163182 167650 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301725 167650 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
71612894 89979 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 408 3 1 4 4.1 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381292 89979 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 408 3 1 4 4.1 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
122193737 123968 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 438 10 1 4 5.9 CCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628757 123968 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 438 10 1 4 5.9 CCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
57521809 76262 0 None -13 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL2058520 76262 0 None -13 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL4210970 76262 0 None -13 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmc.2017.10.040
145971234 163079 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 453 7 1 3 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4176612 163079 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 453 7 1 3 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)cc2)cc1 10.1016/j.ejmech.2018.04.023
127051302 140314 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3806208 140314 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3)s2)cc1 10.1016/j.bmc.2016.04.065
127049498 140239 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(Cl)c3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805377 140239 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(Cl)c3)s2)cc1 10.1016/j.bmc.2016.04.065
131986147 164777 0 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218110 164777 0 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
25150121 185180 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1ccc(C#Cc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm8010178
CHEMBL485738 185180 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1ccc(C#Cc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm8010178
75511303 122453 3 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(F)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600997 122453 3 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(F)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
54757735 65343 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 341 4 1 2 4.5 Cc1ccccc1-c1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
CHEMBL1829163 65343 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 341 4 1 2 4.5 Cc1ccccc1-c1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
54582150 61808 0 None 22 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773259 61808 0 None 22 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
54582630 62156 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 62156 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
131986297 164203 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210878 164203 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
122189677 123353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616657 123353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
46231436 200397 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 5 1 3 3.4 O=C1NC(=O)C(Cc2ccc(CCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598040 200397 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 5 1 3 3.4 O=C1NC(=O)C(Cc2ccc(CCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
46231655 201112 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccnc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL603065 201112 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccnc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
145951164 162792 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 473 8 2 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172250 162792 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 473 8 2 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
122193972 123976 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 2 5 4.9 Cc1cc(OCCCO)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3629046 123976 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 454 11 2 5 4.9 Cc1cc(OCCCO)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
57521917 76273 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL2058530 76273 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1 10.1021/jm300215x
168298569 192677 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1cccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)c1 10.1016/j.ejmech.2022.114645
CHEMBL5219055 192677 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1cccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)c1 10.1016/j.ejmech.2022.114645
25150113 171632 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 265 3 2 2 2.7 Nc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL446575 171632 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 265 3 2 2 2.7 Nc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
54757515 65326 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 296 4 1 4 2.4 O=C(O)CCc1ccc(C#Cc2ncccc2[N+](=O)[O-])cc1 10.1021/jm2005699
CHEMBL1829147 65326 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 296 4 1 4 2.4 O=C(O)CCc1ccc(C#Cc2ncccc2[N+](=O)[O-])cc1 10.1021/jm2005699
146314448 180125 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 507 12 1 4 7.3 COc1ccc(CCCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4748702 180125 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 507 12 1 4 7.3 COc1ccc(CCCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
134538585 163633 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4203974 163633 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
15603842 111798 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287570 111798 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
91809187 147122 13 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 147122 13 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
118645715 181485 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764729 181485 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
162668241 182504 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4787007 182504 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
67087041 182369 0 None -14 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 182369 0 None -14 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183583 0 None -10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183583 0 None -10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194237 182204 0 None -4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 182204 0 None -4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
45107312 119131 5 None -2 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427712 119131 5 None -2 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
118642390 162682 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4170346 162682 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
155544661 174943 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
CHEMBL4565467 174943 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
127045659 139691 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1ccc(F)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798044 139691 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1ccc(F)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
71613520 89976 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381289 89976 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
57706778 80795 29 None 8 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL2152070 80795 29 None 8 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
147329931 175400 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 409 9 2 4 5.3 CCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4575598 175400 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 409 9 2 4 5.3 CCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
134137874 152979 0 None 1995 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152979 0 None 1995 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152979 0 None 1995 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular Ca2+ flux preincubated for 40 mins measured for 180 secs by fluo-4 NW dye-based assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
168273613 190266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 468 6 1 5 5.6 O=C(O)C[C@@H]1COc2cc(OCc3ccc4nc(-c5ccc(C(F)(F)F)cc5)cn4c3)ccc21 10.1016/j.bmcl.2021.127969
CHEMBL5175525 190266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 468 6 1 5 5.6 O=C(O)C[C@@H]1COc2cc(OCc3ccc4nc(-c5ccc(C(F)(F)F)cc5)cn4c3)ccc21 10.1016/j.bmcl.2021.127969
57705555 163598 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 518 11 1 3 8.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4203561 163598 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 518 11 1 3 8.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
57400637 70021 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939650 70021 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.10.118
137644989 158513 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 391 7 1 4 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C#N)CC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4091211 158513 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 391 7 1 4 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C#N)CC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
132606863 157821 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157821 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218709 158416 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
CHEMBL4090240 158416 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
90151764 157000 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 526 7 1 7 5.0 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4073270 157000 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 526 7 1 7 5.0 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
77845055 159783 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4105324 159783 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
145990980 166757 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)ccc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4283655 166757 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)ccc3O2)cc1 10.1016/j.bmc.2018.10.019
122193742 123969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 396 7 2 4 4.9 Cc1cc(O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628762 123969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 396 7 2 4 4.9 Cc1cc(O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
23136315 58829 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccccc2Oc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688456 58829 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccccc2Oc2ccccc2)cc1 10.1021/jm101405t
25261464 80796 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152071 80796 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
57395404 70008 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 286 7 1 3 3.3 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939637 70008 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 286 7 1 3 3.3 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
58218607 155938 0 None -7 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4061093 155938 0 None -7 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137661475 159456 0 None 1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4101348 159456 0 None 1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
137651153 157202 0 None -1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.7 CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4076004 157202 0 None -1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.7 CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
90644294 111959 0 None -13 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288352 111959 0 None -13 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
124011385 166858 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4285594 166858 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
137635388 155822 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4059947 155822 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
137646043 157785 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 385 6 1 2 5.4 Cc1ccccc1Cc1ccc(N2CC[C@H](c3ccccc3)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4082975 157785 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 385 6 1 2 5.4 Cc1ccccc1Cc1ccc(N2CC[C@H](c3ccccc3)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145985122 165906 0 None -17 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 456 11 1 4 5.5 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4250132 165906 0 None -17 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 456 11 1 4 5.5 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
1049 363 75 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
4618 363 75 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
5280934 363 75 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
CHEMBL8739 363 75 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
DB00132 363 75 None 1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.ejmech.2018.08.075
71613515 89971 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381283 89971 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
86803185 122462 5 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601006 122462 5 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
137629942 161023 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1 10.1016/j.ejmech.2017.01.005
CHEMBL4071849 161023 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1 10.1016/j.ejmech.2017.01.005
CHEMBL4116363 161023 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1 10.1016/j.ejmech.2017.01.005
54757626 65337 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
CHEMBL1829157 65337 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
24825481 75923 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205090 75923 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
134141270 146808 0 None -35 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 334 8 1 3 4.6 CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3924759 146808 0 None -35 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 334 8 1 3 4.6 CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
15605424 200564 3 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccccc2Oc2ccccc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599067 200564 3 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccccc2Oc2ccccc2)S1 10.1016/j.bmcl.2009.10.052
53248847 62145 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 62145 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
145950728 162768 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4171827 162768 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
86803196 122463 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601007 122463 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)cc1 10.1016/j.bmcl.2015.06.018
145966017 164341 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1C 10.1016/j.ejmech.2017.09.019
CHEMBL4212573 164341 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1C 10.1016/j.ejmech.2017.09.019
145954950 161643 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccc(C(F)(F)F)cc3)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4130213 161643 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccc(C(F)(F)F)cc3)cc2)S1 10.1016/j.bmcl.2018.03.051
145953265 162625 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccnc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4169459 162625 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccnc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
54580625 62163 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777873 62163 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
127045658 139777 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 437 7 1 4 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(C(F)(F)F)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798642 139777 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 437 7 1 4 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(C(F)(F)F)c1 10.1016/j.ejmech.2016.03.054
145958971 162184 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 500 8 1 4 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4162561 162184 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 500 8 1 4 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
44409702 140984 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 1 3 5.6 O=C(CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)N1CCCC1 10.1016/j.bmcl.2006.01.007
CHEMBL382341 140984 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 1 3 5.6 O=C(CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)N1CCCC1 10.1016/j.bmcl.2006.01.007
137630875 161120 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4091587 161120 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4117177 161120 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
57521813 76266 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 400 7 1 2 6.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1 10.1021/jm300215x
CHEMBL2058524 76266 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 400 7 1 2 6.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1 10.1021/jm300215x
23346507 88286 1 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/jm300215x
CHEMBL234834 88286 1 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/jm300215x
3893 2285 98 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
4642 2285 98 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
5534 2285 98 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
CHEMBL108766 2285 98 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
DB03017 2285 98 None -1 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1039/C7MD00130D
643684 107513 63 None -8 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 298 15 2 2 5.1 CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O 10.1039/C7MD00130D
CHEMBL3186422 107513 63 None -8 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 298 15 2 2 5.1 CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O 10.1039/C7MD00130D
122189680 123355 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 8 2 4 3.4 CC(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616660 123355 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 8 2 4 3.4 CC(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
127025284 137744 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 417 6 1 4 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
CHEMBL3759212 137744 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 417 6 1 4 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
82051616 159455 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
CHEMBL4101323 159455 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
134130823 154436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3890182 154436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990066 154436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
118129974 157192 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 157192 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
145994052 167353 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 425 7 1 5 4.6 O=C(O)CC(c1ccncc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294582 167353 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 425 7 1 5 4.6 O=C(O)CC(c1ccncc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145966485 164348 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 9 2 6 3.9 CCc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4212664 164348 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 9 2 6 3.9 CCc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
1051 1454 63 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
4289 1454 63 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
445580 1454 63 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
57417355 1454 63 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
CHEMBL367149 1454 63 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
DB03756 1454 63 None -14 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR40 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/acsmedchemlett.6b00025
127030730 138812 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1cccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)c1 10.1016/j.ejmech.2016.02.040
CHEMBL3781145 138812 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1cccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)c1 10.1016/j.ejmech.2016.02.040
90151568 157569 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 7 1 5 5.5 CCc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4080516 157569 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 7 1 5 5.5 CCc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
137633536 156293 0 None -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
CHEMBL4065397 156293 0 None -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
46231549 200495 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598674 200495 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
91809187 147122 13 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3927519 147122 13 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1016/j.bmcl.2016.10.074
127050768 140287 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805903 140287 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
131986116 163822 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206318 163822 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58173002 122668 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1F 10.1016/j.bmc.2015.07.028
CHEMBL3604037 122668 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1F 10.1016/j.bmc.2015.07.028
122185439 122679 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604047 122679 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)cc2)cc1 10.1016/j.bmc.2015.07.028
45107317 122693 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 8 1 3 4.9 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(CC)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604061 122693 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 8 1 3 4.9 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(CC)cccc32)cc1 10.1016/j.bmc.2015.07.028
122185451 122694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.4 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C(C)C)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604062 122694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.4 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C(C)C)cccc32)cc1 10.1016/j.bmc.2015.07.028
127046961 140055 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 383 7 1 4 5.0 Cc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3800362 140055 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 383 7 1 4 5.0 Cc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
90479828 183082 10 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4794409 183082 10 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
57413288 75821 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048614 75821 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
51357276 182005 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194127 183193 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 183193 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
52936292 182108 27 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
131986179 164795 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218348 164795 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
11245322 77140 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL207753 77140 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
162646017 179470 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4740846 179470 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
11773976 74779 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 2 3 5.7 CC(C)NC(=O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL203126 74779 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 400 8 2 3 5.7 CC(C)NC(=O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
46941175 61810 26 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL1773261 61810 26 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
44409878 140857 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 419 7 2 4 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(N)=O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL381958 140857 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 419 7 2 4 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(N)=O)cc1 10.1016/j.bmcl.2006.01.007
51350270 58837 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
CHEMBL1688463 58837 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
51350274 58857 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1021/jm101405t
CHEMBL1688483 58857 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1021/jm101405t
57705851 163782 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1F 10.1021/acsmedchemlett.8b00213
CHEMBL4205882 163782 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1F 10.1021/acsmedchemlett.8b00213
155516879 170097 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 446 7 1 4 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4443509 170097 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 446 7 1 4 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
155522406 170624 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 456 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4c(C)cccc4C)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4451050 170624 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 456 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4c(C)cccc4C)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
46231597 200193 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 352 4 1 5 3.9 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc(C)c1C#N 10.1016/j.bmcl.2009.10.052
CHEMBL596667 200193 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 352 4 1 5 3.9 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc(C)c1C#N 10.1016/j.bmcl.2009.10.052
57398937 70012 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 340 8 1 3 4.8 COc1ccc(COc2ccc(C(C=C(C)C)CC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939641 70012 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 340 8 1 3 4.8 COc1ccc(COc2ccc(C(C=C(C)C)CC(=O)O)cc2)cc1 10.1016/j.bmcl.2011.10.118
122185450 122692 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 341 7 1 5 4.5 CCO[C@@H](CC(=O)O)c1ccc(Oc2noc3c(C)cccc23)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604060 122692 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 341 7 1 5 4.5 CCO[C@@H](CC(=O)O)c1ccc(Oc2noc3c(C)cccc23)cc1 10.1016/j.bmc.2015.07.028
90644298 111963 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 391 8 1 4 4.6 COC(Cc1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1)C(=O)O 10.1016/j.bmcl.2014.04.065
CHEMBL3288356 111963 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 391 8 1 4 4.6 COC(Cc1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1)C(=O)O 10.1016/j.bmcl.2014.04.065
121294346 180122 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.6 COCC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4748658 180122 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.6 COCC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
146314488 181139 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 451 10 1 4 6.1 COc1ccc(C(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4760668 181139 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 451 10 1 4 6.1 COc1ccc(C(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
67085761 157023 0 None 12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4073525 157023 0 None 12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
58218640 158920 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4095599 158920 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145979171 166525 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4279126 166525 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
54757737 65345 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1F 10.1021/jm2005699
CHEMBL1829165 65345 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1F 10.1021/jm2005699
51350273 58856 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688482 58856 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
71613094 89985 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381298 89985 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
75511307 122464 4 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3Cl)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601008 122464 4 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3Cl)no2)cc1 10.1016/j.bmcl.2015.06.018
71460190 80662 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2)c1 10.1021/ml300133f
CHEMBL2151292 80662 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2)c1 10.1021/ml300133f
71454737 80673 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 512 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)c4ccccc4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151302 80673 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 512 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)c4ccccc4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
1050 1900 94 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1900 94 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1900 94 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
57391958 70013 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 326 7 1 3 4.5 COc1ccc(COc2ccc(C(CC(=O)O)=C(C)C)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939642 70013 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 326 7 1 3 4.5 COc1ccc(COc2ccc(C(CC(=O)O)=C(C)C)cc2)cc1 10.1016/j.bmcl.2011.10.118
57391960 70022 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939651 70022 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
130253300 159109 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4097617 159109 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
137659366 159429 0 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 391 5 1 4 5.1 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4101071 159429 0 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 391 5 1 4 5.1 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12 10.1021/acs.jmedchem.7b00210
145946817 167591 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4248694 167591 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4300846 167591 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
118642390 162682 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4170346 162682 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
142738575 162983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 283 4 2 1 4.0 O=C(O)CCc1ccc2[nH]c(-c3ccccc3F)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4175260 162983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 283 4 2 1 4.0 O=C(O)CCc1ccc2[nH]c(-c3ccccc3F)cc2c1 10.1021/acsmedchemlett.7b00460
46231546 200605 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c(C)c1 10.1016/j.bmcl.2009.10.052
CHEMBL599280 200605 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c(C)c1 10.1016/j.bmcl.2009.10.052
118719473 115533 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 498 12 1 6 4.8 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353261 115533 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 498 12 1 6 4.8 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
122189682 123356 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 375 7 2 4 3.6 CC(C)(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616662 123356 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 375 7 2 4 3.6 CC(C)(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
137642174 161216 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4091100 161216 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117940 161216 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
90372616 142231 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
71615467 89988 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 538 9 1 7 4.9 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381301 89988 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 538 9 1 7 4.9 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
1646307 95001 12 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 385 7 1 4 4.7 O=C(O)CCCCCN1C(=O)/C(=C\c2cccc3ccccc23)SC1=S 10.1021/jm7012425
CHEMBL254859 95001 12 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 385 7 1 4 4.7 O=C(O)CCCCCN1C(=O)/C(=C\c2cccc3ccccc23)SC1=S 10.1021/jm7012425
118623088 142125 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883407 142125 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
134130352 142143 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 142143 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
58319098 86540 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1ccc(C)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315541 86540 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1ccc(C)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
145976935 163909 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 434 7 1 4 6.2 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)SCC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4207283 163909 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 434 7 1 4 6.2 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)SCC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
127029851 138860 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
CHEMBL3781779 138860 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
24825489 87321 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 317 6 2 2 4.6 O=C(O)Cc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL233223 87321 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 317 6 2 2 4.6 O=C(O)Cc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
46231485 200314 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccccc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL597436 200314 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccccc1Oc1ccc(CC2SC(=O)NC2=O)cc1 10.1016/j.bmcl.2009.10.052
53248848 62166 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 62166 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
54580625 62163 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777873 62163 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
54586485 62155 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777865 62155 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
71615470 89991 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)ccc2F)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381304 89991 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)ccc2F)c(Cl)c1 10.1016/j.bmcl.2013.03.060
145976845 163729 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 484 11 1 6 4.4 COCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4205241 163729 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 484 11 1 6 4.4 COCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
54583099 61809 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccc(-c2cccc(CNc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
CHEMBL1773260 61809 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccc(-c2cccc(CNc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
44409699 140341 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.7 CC(CC(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380719 140341 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 361 8 2 3 5.7 CC(CC(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
134130859 142181 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 416 6 1 2 6.9 CC1(C)CCC=C1c1cccc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883983 142181 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 416 6 1 2 6.9 CC1(C)CCC=C1c1cccc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)c1 10.1021/acsmedchemlett.6b00443
24825505 148273 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 285 7 2 3 3.3 COc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL393661 148273 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 285 7 2 3 3.3 COc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
10131213 179327 3 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 252 3 1 2 2.6 O=C(O)COc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
CHEMBL473459 179327 3 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 252 3 1 2 2.6 O=C(O)COc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
137633536 156293 0 None -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
CHEMBL4065397 156293 0 None -173 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
137647721 157828 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4083440 157828 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
82051616 159455 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
CHEMBL4101323 159455 1 None -12 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl 10.1016/j.bmcl.2017.01.034
54584097 61799 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 382 6 1 2 3.9 O=C(O)CCc1ccc(OCc2ccccc2)c(I)c1 10.1021/ml100106c
CHEMBL1773250 61799 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 382 6 1 2 3.9 O=C(O)CCc1ccc(OCc2ccccc2)c(I)c1 10.1021/ml100106c
75511312 122501 3 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 402 7 1 5 4.1 O=C(O)CCc1ccc(OCc2nc(-c3cccc(Br)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601049 122501 3 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 402 7 1 5 4.1 O=C(O)CCc1ccc(OCc2nc(-c3cccc(Br)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
137629014 160983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4063785 160983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116078 160983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
54580624 62150 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777860 62150 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
118623101 167587 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167587 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167587 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
118642344 142120 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883380 142120 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
91801188 169573 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4435837 169573 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
134151755 154449 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3976110 154449 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990146 154449 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137630599 161091 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1 10.1016/j.ejmech.2017.01.005
CHEMBL4072869 161091 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1 10.1016/j.ejmech.2017.01.005
CHEMBL4116895 161091 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1 10.1016/j.ejmech.2017.01.005
131986090 164290 0 None 5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4212041 164290 0 None 5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145967994 164786 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 399 7 1 5 3.5 Cc1ccc(C)n1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4218236 164786 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 399 7 1 5 3.5 Cc1ccc(C)n1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
127048827 140281 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 371 6 2 5 3.6 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccc(F)cc3)c2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805879 140281 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 371 6 2 5 3.6 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccc(F)cc3)c2)s1 10.1016/j.bmc.2016.04.065
142738582 184518 0 None 42 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4847662 184518 0 None 42 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
46854655 395 47 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.ejmech.2018.09.071
6485 395 47 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.ejmech.2018.09.071
CHEMBL1829173 395 47 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.ejmech.2018.09.071
46854655 395 47 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2016.10.074
6485 395 47 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2016.10.074
CHEMBL1829173 395 47 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2016.10.074
57706778 80795 29 None -8 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
CHEMBL2152070 80795 29 None -8 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
24857285 75617 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047157 75617 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
131986027 163936 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207592 163936 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986061 164114 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209834 164114 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
67058307 122632 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3cc(C(F)(F)F)ccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3603843 122632 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3cc(C(F)(F)F)ccc32)cc1 10.1016/j.bmc.2015.07.028
67058222 122684 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(F)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604052 122684 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(F)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
122185447 122689 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604057 122689 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2F)cc1 10.1016/j.bmc.2015.07.028
45107324 122695 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 366 8 1 3 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C4CC4)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604063 122695 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 366 8 1 3 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C4CC4)cccc32)cc1 10.1016/j.bmc.2015.07.028
1050 1900 94 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
11595431 1900 94 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
CHEMBL207881 1900 94 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
134138870 147670 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 491 9 2 5 5.2 Cc1cc(OCCC(C)O)cc(C)c1-c1ccc(F)c(COc2cc3c(cn2)[C@@H]2C(C(=O)O)[C@@H]2C3)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3931755 147670 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 491 9 2 5 5.2 Cc1cc(OCCC(C)O)cc(C)c1-c1ccc(F)c(COc2cc3c(cn2)[C@@H]2C(C(=O)O)[C@@H]2C3)c1 10.1016/j.bmcl.2016.10.074
57413290 75824 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048617 75824 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
46854655 395 47 None 1 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
6485 395 47 None 1 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
CHEMBL1829173 395 47 None 1 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
145947998 167714 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167714 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167714 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
11245322 77140 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL207753 77140 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
71575419 89970 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381282 89970 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
54584572 62168 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777878 62168 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
90644292 111957 0 None 10 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288350 111957 0 None 10 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
145983698 166418 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 382 7 1 5 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4277181 166418 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 382 7 1 5 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC)cc3O2)cc1 10.1016/j.bmc.2018.10.019
67087160 182342 0 None -6 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 182342 0 None -6 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
90644293 111958 0 None -13 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
CHEMBL3288351 111958 0 None -13 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
90644301 111966 0 None -9 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288359 111966 0 None -9 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
57706778 80795 29 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL2152070 80795 29 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
57706778 80795 29 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
CHEMBL2152070 80795 29 None -8 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
134157016 154435 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3985181 154435 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990065 154435 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137655619 158696 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 340 6 1 4 4.0 CN(C)c1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4093180 158696 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 340 6 1 4 4.0 CN(C)c1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
87265393 159279 0 None -4 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4099410 159279 0 None -4 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
58218699 159414 0 None 2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4100898 159414 0 None 2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
137631654 156298 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 449 8 1 5 5.7 O=C(O)CCc1ccc(-c2ccc3c(OCc4ccccc4)nn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
CHEMBL4065429 156298 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 449 8 1 5 5.7 O=C(O)CCc1ccc(-c2ccc3c(OCc4ccccc4)nn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
137641734 158040 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4085805 158040 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
142738556 162766 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 333 4 2 1 4.9 O=C(O)CCc1ccc2[nH]c(-c3ccccc3C(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4171817 162766 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 333 4 2 1 4.9 O=C(O)CCc1ccc2[nH]c(-c3ccccc3C(F)(F)F)cc2c1 10.1021/acsmedchemlett.7b00460
71458348 80671 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 9 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151300 80671 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 9 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
75511315 122510 4 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601058 122510 4 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
137647721 157828 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4083440 157828 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
44634022 65322 1 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccn2)cc1 10.1021/jm2005699
CHEMBL1829143 65322 1 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccn2)cc1 10.1021/jm2005699
71615671 90003 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cc(C)cc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381316 90003 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cc(C)cc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
122189737 123390 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 7 2 4 3.3 Cc1ccc(OC(C)C(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1C 10.1016/j.bmc.2015.09.010
CHEMBL3616719 123390 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 361 7 2 4 3.3 Cc1ccc(OC(C)C(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1C 10.1016/j.bmc.2015.09.010
145956160 162494 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 522 8 1 5 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(Cl)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167397 162494 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 522 8 1 5 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(Cl)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
145972020 163123 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 457 8 2 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)o2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4177506 163123 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 457 8 2 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)o2)cc1 10.1016/j.ejmech.2018.04.023
118637974 162036 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4160127 162036 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
131986164 164617 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216016 164617 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
51049992 145617 5 None -23 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL3915620 145617 5 None -23 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
54757738 65346 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 299 3 1 2 3.5 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
CHEMBL1829166 65346 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 299 3 1 2 3.5 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
23136411 58830 0 None 11 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
CHEMBL1688457 58830 0 None 11 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
90151518 156912 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 6 1 5 5.6 Cc1cccc(C)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4072314 156912 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 489 6 1 5 5.6 Cc1cccc(C)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
46231598 202197 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 4 4.5 O=C1NC(=O)C(Cc2ccc(Oc3cccc4ccccc34)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL609615 202197 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 4 4.5 O=C1NC(=O)C(Cc2ccc(Oc3cccc4ccccc34)cc2)S1 10.1016/j.bmcl.2009.10.052
122189672 123351 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.7 CC(Oc1ccccc1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616652 123351 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.7 CC(Oc1ccccc1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
122189676 123352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 351 7 2 4 2.8 CC(Oc1ccccc1F)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616656 123352 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 351 7 2 4 2.8 CC(Oc1ccccc1F)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
134149615 148574 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
CHEMBL3939004 148574 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
145973937 164584 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 487 10 2 6 5.2 COc1ccc(C(Cc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c2ccccc2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4215600 164584 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 487 10 2 6 5.2 COc1ccc(C(Cc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c2ccccc2)cc1 10.1016/j.ejmech.2017.09.019
145980455 166710 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 365 6 2 4 3.7 O=C(O)CCc1ccc(NCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4282779 166710 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 365 6 2 4 3.7 O=C(O)CCc1ccc(NCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
20993091 62146 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 310 5 1 2 4.8 O=C(O)CCc1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777856 62146 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 310 5 1 2 4.8 O=C(O)CCc1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
54584572 62168 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777878 62168 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
134149615 148574 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
CHEMBL3939004 148574 0 None -23 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1016/j.bmcl.2016.10.054
127033820 138776 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780713 138776 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
118637996 142168 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 142168 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 142168 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
145949955 162908 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccn4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4173953 162908 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccn4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
71562317 86537 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
CHEMBL2315538 86537 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
71562423 86542 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 298 3 1 1 4.1 Cc1cc(Cl)ccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315543 86542 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 298 3 1 1 4.1 Cc1cc(Cl)ccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
145972304 164542 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 423 8 2 6 3.9 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc4c(c3)CCC4)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4215103 164542 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 423 8 2 6 3.9 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc4c(c3)CCC4)s2)cc1 10.1016/j.ejmech.2017.09.019
118637996 142168 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 142168 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 142168 0 None -15 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
46231843 200503 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 5 1 6 4.4 COc1cc(Oc2ncc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL598732 200503 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 432 5 1 6 4.4 COc1cc(Oc2ncc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
134130352 142143 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 142143 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
134143899 150237 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 5 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
CHEMBL3952316 150237 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 5 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
24857286 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
6484 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
CHEMBL1829174 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
DB12491 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
146948845 185878 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 522 11 1 5 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CCc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4868224 185878 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 522 11 1 5 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CCc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/acs.jmedchem.1c00031
57414539 75618 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047158 75618 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
24857286 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
6484 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
CHEMBL1829174 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
DB12491 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.7b00460
24857286 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
6484 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
CHEMBL1829174 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
DB12491 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
90644301 111966 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288359 111966 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1 10.1016/j.bmcl.2014.04.065
11190525 75823 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048616 75823 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
162667620 182555 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 182555 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
162644059 181822 0 None 45 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None 45 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
67087100 182596 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182596 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
145952952 162489 0 None 1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167323 162489 0 None 1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
131986027 163936 0 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207592 163936 0 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 606 11 1 7 7.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986112 164415 0 None 3 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213548 164415 0 None 3 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986072 164450 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213937 164450 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
134131511 142156 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 142156 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
24857286 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
6484 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
CHEMBL1829174 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
DB12491 1622 72 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm2005699
44409843 140403 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380884 140403 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 473 7 2 4 6.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC(C)C)cc1 10.1016/j.bmcl.2006.01.007
51350138 58847 0 None 660 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL1688473 58847 0 None 660 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
46941175 61810 26 None -1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61810 26 None -1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
60195037 81720 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 495 12 2 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
CHEMBL2163925 81720 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 495 12 2 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
44409676 75001 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 7 3 4 4.7 O=C(NO)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL203297 75001 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 7 3 4 4.7 O=C(NO)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
57705749 164850 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4218995 164850 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
121294749 182739 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 542 11 1 5 6.2 COc1ccc(C(=O)N(C)c2ccccc2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4789994 182739 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 542 11 1 5 6.2 COc1ccc(C(=O)N(C)c2ccccc2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
58218607 155938 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4061093 155938 0 None 7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57325842 74104 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022580 74104 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
58230598 183117 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 183117 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
122189683 123357 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 389 7 2 4 4.0 CC(Oc1cccc(C(C)(C)C)c1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616663 123357 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 389 7 2 4 4.0 CC(Oc1cccc(C(C)(C)C)c1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1 10.1016/j.bmc.2015.09.010
137649555 157328 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4077507 157328 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
90644292 111957 0 None -10 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288350 111957 0 None -10 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
137658391 159646 0 None -1 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
CHEMBL4103681 159646 0 None -1 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
54586485 62155 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777865 62155 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
46231842 200502 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 397 5 1 5 4.7 COc1cc(Oc2ccc(Cl)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL598731 200502 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 397 5 1 5 4.7 COc1cc(Oc2ccc(Cl)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
66562389 90365 0 None 58 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 286 3 1 1 3.4 O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
CHEMBL2386360 90365 0 None 58 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 286 3 1 1 3.4 O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
145965968 164244 0 None -4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4211335 164244 0 None -4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
137656526 159751 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4105013 159751 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
127046662 140038 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 10 1 5 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC(C)C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3800255 140038 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 10 1 5 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC(C)C)c1 10.1016/j.ejmech.2016.03.054
46231779 200876 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 350 4 1 5 3.9 O=C1NC(=O)C(Cc2ccc(Oc3cc4ccccc4cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL601420 200876 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 350 4 1 5 3.9 O=C1NC(=O)C(Cc2ccc(Oc3cc4ccccc4cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
145962064 162235 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 474 8 2 5 5.1 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4163436 162235 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 474 8 2 5 5.1 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)NC3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
71562316 86536 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.3 O=C(O)[C@H]1C[C@@H]1c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315537 86536 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.3 O=C(O)[C@H]1C[C@@H]1c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
66562390 90363 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 10.1021/ml4000673
CHEMBL2386358 90363 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 10.1021/ml4000673
44409929 76423 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 345 7 2 3 5.2 O=C(O)/C=C/c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205960 76423 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 345 7 2 3 5.2 O=C(O)/C=C/c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
127033352 139018 0 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 272 8 1 1 4.4 CCCCCCCC#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3785789 139018 0 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 272 8 1 1 4.4 CCCCCCCC#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
66562387 90371 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386366 90371 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
71613096 89987 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381300 89987 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
168278906 191029 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 438 10 1 4 5.9 Cc1ccc(OCC(C)C)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5186963 191029 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 438 10 1 4 5.9 Cc1ccc(OCC(C)C)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
2214962 94658 8 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 283 7 2 3 3.6 C=CCOc1ccc(CNc2cccc(C(=O)O)c2)cc1 10.1021/jm7012425
CHEMBL252528 94658 8 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 283 7 2 3 3.6 C=CCOc1ccc(CNc2cccc(C(=O)O)c2)cc1 10.1021/jm7012425
91824140 151074 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 425 7 1 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(-c3ccccc3C)cn3ncnc23)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3958983 151074 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 425 7 1 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(-c3ccccc3C)cn3ncnc23)cc1 10.1016/j.bmcl.2016.10.074
118623101 167587 0 None -12 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167587 0 None -12 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167587 0 None -12 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
90357232 142250 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884803 142250 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
122185446 122688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1cccc(OCc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmc.2015.07.028
CHEMBL3604056 122688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1cccc(OCc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmc.2015.07.028
122189685 123327 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 349 8 2 5 2.3 COc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3616479 123327 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 349 8 2 5 2.3 COc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
6483 3884 54 None -13 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assayAgonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3884 54 None -13 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assayAgonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3884 54 None -13 4 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assayAgonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
145987974 167076 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 362 7 1 5 3.1 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CO2 10.1016/j.bmc.2018.10.019
CHEMBL4289597 167076 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 362 7 1 5 3.1 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CO2 10.1016/j.bmc.2018.10.019
137655393 158732 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4093521 158732 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
137529979 164173 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 473 6 3 4 5.2 CNC(=O)c1cc(C)c(-c2ccc(F)c3c2CC[C@H]3Nc2ccc([C@H]3C[C@@H]3C(=O)O)nc2)c(C)c1 10.1021/acsmedchemlett.8b00343
CHEMBL4210588 164173 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 473 6 3 4 5.2 CNC(=O)c1cc(C)c(-c2ccc(F)c3c2CC[C@H]3Nc2ccc([C@H]3C[C@@H]3C(=O)O)nc2)c(C)c1 10.1021/acsmedchemlett.8b00343
122189678 123354 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1ccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1 10.1016/j.bmc.2015.09.010
CHEMBL3616658 123354 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 333 7 2 4 2.6 Cc1ccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1 10.1016/j.bmc.2015.09.010
137629795 161181 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4063221 161181 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117645 161181 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
137633561 156349 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(COc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4065921 156349 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(COc2cn(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
54582631 62157 0 None -1 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777867 62157 0 None -1 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
54581633 62159 0 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777869 62159 0 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
131986072 164450 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213937 164450 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986179 164795 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218348 164795 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
57413289 75822 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048615 75822 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11398822 75830 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048624 75830 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
46854655 395 47 None -8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None -8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None -8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
118145140 175383 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4575265 175383 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
145967748 163509 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 496 12 1 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4202452 163509 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 496 12 1 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
118645526 182978 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4793322 182978 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
155569585 176207 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 419 7 2 3 5.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4593950 176207 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 419 7 2 3 5.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1F 10.1016/j.ejmech.2019.06.087
127047527 139870 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1Cl 10.1016/j.ejmech.2016.03.054
CHEMBL3799274 139870 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1Cl 10.1016/j.ejmech.2016.03.054
155527415 171222 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 453 7 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C#N)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4459626 171222 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 453 7 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C#N)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
57706778 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
CHEMBL2152070 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
162674275 182989 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 491 10 1 4 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4793427 182989 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 491 10 1 4 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1021/acs.jmedchem.0c00843
58218740 156443 0 None 45 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4067052 156443 0 None 45 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
137646482 157749 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082459 157749 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218551 159045 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4096887 159045 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137633394 156422 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 541 8 1 6 5.4 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4066815 156422 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 541 8 1 6 5.4 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
90151501 158753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 510 7 1 7 4.5 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(F)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4093944 158753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 510 7 1 7 4.5 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(F)cn1 10.1021/acs.jmedchem.7b00982
145980470 166734 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 420 6 1 4 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4283222 166734 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 420 6 1 4 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
156703595 191911 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 438 10 1 5 5.1 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5200141 191911 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 438 10 1 5 5.1 COc1ccc(/C=C/c2cc(OC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
58172971 122666 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 8 1 3 5.4 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(C)c1 10.1016/j.bmc.2015.07.028
CHEMBL3604035 122666 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 8 1 3 5.4 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(C)c1 10.1016/j.bmc.2015.07.028
67085761 157023 0 None -12 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4073525 157023 0 None -12 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137651358 157141 0 None -2 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 375 5 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4075162 157141 0 None -2 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 375 5 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12 10.1021/acs.jmedchem.7b00210
118144953 175646 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2ccc3c(n2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4581212 175646 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2ccc3c(n2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
58319121 86546 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 284 3 1 1 3.8 O=C(O)CCc1ccc(C#Cc2ccccc2Cl)cc1 10.1021/jm301470a
CHEMBL2315547 86546 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 284 3 1 1 3.8 O=C(O)CCc1ccc(C#Cc2ccccc2Cl)cc1 10.1021/jm301470a
1855223 94633 15 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 404 8 1 7 4.8 COc1ccc(CSc2nnc(SCc3ccc(C(=O)O)cc3)s2)cc1 10.1021/jm7012425
CHEMBL252330 94633 15 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 404 8 1 7 4.8 COc1ccc(CSc2nnc(SCc3ccc(C(=O)O)cc3)s2)cc1 10.1021/jm7012425
71257551 150591 24 None -14 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3955132 150591 24 None -14 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1016/j.bmcl.2016.10.074
127051660 140265 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccccc1NC(=O)c1nnc(COc2ccc(CCC(=O)O)cc2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805668 140265 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccccc1NC(=O)c1nnc(COc2ccc(CCC(=O)O)cc2)s1 10.1016/j.bmc.2016.04.065
145975293 163584 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccccc1OCc1nnc(C(=O)Nc2ccc(CCC(=O)O)cc2)s1 10.1016/j.ejmech.2017.09.019
CHEMBL4203402 163584 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccccc1OCc1nnc(C(=O)Nc2ccc(CCC(=O)O)cc2)s1 10.1016/j.ejmech.2017.09.019
118719717 115660 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.1 Cc1cc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)ccc1OCC(=O)O 10.1016/j.bmc.2014.11.016
CHEMBL3353738 115660 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.1 Cc1cc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)ccc1OCC(=O)O 10.1016/j.bmc.2014.11.016
168276115 190271 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 450 10 1 4 6.0 Cc1ccc(OCC2CCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5175597 190271 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 450 10 1 4 6.0 Cc1ccc(OCC2CCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
145977707 163954 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(C)c(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
CHEMBL4207787 163954 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(C)c(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
90372616 142231 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
51349861 58827 0 None 77 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
CHEMBL1688454 58827 0 None 77 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
25150119 186384 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 274 3 1 1 3.1 C#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL487570 186384 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 274 3 1 1 3.1 C#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
137636167 155985 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
CHEMBL4061630 155985 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
145954794 162521 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 9 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(Cc4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167766 162521 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 9 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(Cc4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
155561223 175680 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2cc3c(cc2F)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4581859 175680 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2cc3c(cc2F)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
54582631 62157 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777867 62157 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
145968322 165018 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 380 6 1 4 5.3 Cc1ccsc1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4226029 165018 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 380 6 1 4 5.3 Cc1ccsc1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
145976267 163587 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4203431 163587 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
54583581 62158 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777868 62158 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
24825487 153276 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 345 8 2 2 5.4 O=C(O)CCCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL397776 153276 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 345 8 2 2 5.4 O=C(O)CCCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
137636167 155985 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
CHEMBL4061630 155985 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O 10.1016/j.bmcl.2017.01.034
137657972 159602 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4103243 159602 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
137656526 159751 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL4105013 159751 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 10.1016/j.bmcl.2017.01.034
24857286 1622 72 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
6484 1622 72 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
CHEMBL1829174 1622 72 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
DB12491 1622 72 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
57414267 75609 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047149 75609 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
23642299 75627 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047168 75627 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857375 75628 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047169 75628 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
131986051 163881 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206968 163881 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
155526793 171192 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4459220 171192 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
15603946 111656 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
CHEMBL3286409 111656 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
118129998 157321 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 157321 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
71613518 89974 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381287 89974 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
131986147 164777 0 None 6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218110 164777 0 None 6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
90644290 111955 0 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288348 111955 0 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
118642384 142163 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883790 142163 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
155551584 173997 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4542487 173997 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
164611439 185231 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1ccc(Cl)cc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4858086 185231 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 313 4 2 1 4.8 Cc1ccc(Cl)cc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
51350272 58839 0 None 107 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL1688465 58839 0 None 107 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
66562386 90368 0 None 562 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 3 1 2 3.4 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386363 90368 0 None 562 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 3 1 2 3.4 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
122184685 122450 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2coc(-c3cccc(Cl)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600994 122450 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2coc(-c3cccc(Cl)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
57706778 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.1c00031
CHEMBL2152070 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.1c00031
57706778 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL2152070 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
57706778 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152070 80795 29 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
155533810 171863 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 428 7 1 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4469136 171863 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 428 7 1 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
121294307 180416 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 610 13 1 7 6.6 COc1ccc(C(=O)N(CC(C)(C)C#N)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4752289 180416 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 610 13 1 7 6.6 COc1ccc(C(=O)N(CC(C)(C)C#N)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
24857286 1622 72 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None -3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
86803191 122454 3 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2ncc(-c3ccccc3)o2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600998 122454 3 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2ncc(-c3ccccc3)o2)cc1 10.1016/j.bmcl.2015.06.018
122185434 122663 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 2 3 3.8 CCOC(CC(=O)O)c1ccc(NC(=O)c2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604032 122663 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 2 3 3.8 CCOC(CC(=O)O)c1ccc(NC(=O)c2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
818213 155474 9 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 345 5 2 3 3.9 O=C(O)c1ccc(NC(=O)c2ccc(C(=O)c3ccccc3)cc2)cc1 10.1021/jm7012425
CHEMBL404008 155474 9 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 345 5 2 3 3.9 O=C(O)c1ccc(NC(=O)c2ccc(C(=O)c3ccccc3)cc2)cc1 10.1021/jm7012425
58319138 86549 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2ccccc2O)cc1 10.1021/jm301470a
CHEMBL2315550 86549 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2ccccc2O)cc1 10.1021/jm301470a
134130696 142135 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 142135 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
155516498 170120 0 None -3 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4443853 170120 0 None -3 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
137657972 159602 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4103243 159602 0 None -40 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
46231654 201682 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cccc(C(F)(F)F)n3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL606213 201682 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cccc(C(F)(F)F)n3)cc2)S1 10.1016/j.bmcl.2009.10.052
127052270 140231 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 343 6 2 6 3.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccco3)c2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805303 140231 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 343 6 2 6 3.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccco3)c2)s1 10.1016/j.bmc.2016.04.065
118637973 162741 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171391 162741 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
54585039 61801 5 None 17 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/jm300215x
CHEMBL1773252 61801 5 None 17 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/jm300215x
24825482 87988 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 7 2 3 5.3 CC(C(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234268 87988 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 7 2 3 5.3 CC(C(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
127027729 137688 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.5 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3Cl)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758719 137688 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.5 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3Cl)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
127025867 137775 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 395 6 1 6 4.1 CC(C)n1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
CHEMBL3759448 137775 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 395 6 1 6 4.1 CC(C)n1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
797771 94656 14 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 312 6 0 7 3.1 COC(=O)CSc1nnc(SCc2ccccc2)s1 10.1021/jm7012425
CHEMBL252526 94656 14 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 312 6 0 7 3.1 COC(=O)CSc1nnc(SCc2ccccc2)s1 10.1021/jm7012425
1201156 155124 17 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 297 5 1 5 2.3 O=C(O)CCCN1C(=O)/C(=C\c2ccco2)SC1=S 10.1021/jm7012425
CHEMBL402053 155124 17 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 297 5 1 5 2.3 O=C(O)CCCN1C(=O)/C(=C\c2ccco2)SC1=S 10.1021/jm7012425
46854655 395 47 None -8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
6485 395 47 None -8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL1829173 395 47 None -8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
145965455 164140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 546 12 1 7 4.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4210139 164140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 546 12 1 7 4.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
127048843 140254 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 387 6 2 5 4.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3cccc(Cl)c3)c2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3805558 140254 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 387 6 2 5 4.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3cccc(Cl)c3)c2)s1 10.1016/j.bmc.2016.04.065
118623088 142125 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 142125 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
57414540 75620 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047160 75620 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414676 75622 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047163 75622 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414677 75623 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047164 75623 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857376 75629 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047170 75629 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
121294284 181355 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 613 12 1 6 7.4 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4763105 181355 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 613 12 1 6 7.4 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
121294846 183550 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc(C(CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4800194 183550 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc(C(CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
162664735 182084 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 182084 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
67087041 182369 0 None -14 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 182369 0 None -14 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194159 183059 0 None -4 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 183059 0 None -4 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
162674998 183389 0 None -5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 183389 0 None -5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
118645756 181460 7 None -2 3 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 181460 7 None -2 3 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
60195036 81719 0 None 630 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 481 12 2 5 5.1 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
CHEMBL2163924 81719 0 None 630 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 481 12 2 5 5.1 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
60195040 81792 0 None 5248 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 7 2 2 5.7 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL2164241 81792 0 None 5248 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 7 2 2 5.7 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
51350135 58844 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688470 58844 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cc2)c1 10.1021/jm101405t
51350136 58845 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688471 58845 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cc2)c1 10.1021/jm101405t
145974173 164597 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 490 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4215771 164597 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 490 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
168294830 192231 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
CHEMBL5205109 192231 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
87262743 158779 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4094160 158779 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
145989151 167200 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3c(Cl)cccc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4291567 167200 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3c(Cl)cccc3O2)cc1 10.1016/j.bmc.2018.10.019
51031010 156629 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4069191 156629 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
23082861 58865 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 298 9 1 2 4.1 O=C(O)CCc1ccc(OCCCCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688491 58865 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 298 9 1 2 4.1 O=C(O)CCc1ccc(OCCCCc2ccccc2)cc1 10.1021/jm101405t
23111708 74047 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/ml1000855
CHEMBL2022246 74047 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/ml1000855
122185431 122660 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 338 8 1 5 3.4 CCOC(Cc1nnn[nH]1)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604029 122660 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 338 8 1 5 3.4 CCOC(Cc1nnn[nH]1)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
58218671 157196 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 7 1 4 4.3 CCOc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4075885 157196 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 7 1 4 4.3 CCOc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137661475 159456 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4101348 159456 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
54582629 62154 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 62154 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
145950126 162858 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 511 7 1 4 6.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4173085 162858 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 511 7 1 4 6.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
24825492 149540 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/ml100106c
CHEMBL394666 149540 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/ml100106c
44409698 76753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 8 1 3 5.1 CN(C)C(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206779 76753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 374 8 1 3 5.1 CN(C)C(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
145967263 164443 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 469 11 1 7 3.6 CO/N=C(\COc1ccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2017.07.001
CHEMBL4213829 164443 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 469 11 1 7 3.6 CO/N=C(\COc1ccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2017.07.001
54757736 65344 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
CHEMBL1829164 65344 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
3367 1155 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/ml100106c
46216676 1155 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/ml100106c
CHEMBL604126 1155 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/ml100106c
127049161 140296 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
CHEMBL3806055 140296 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
145963593 161411 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 4.8 COc1ccc(C(OCCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)cc1 10.1016/j.bmcl.2018.03.051
CHEMBL4126802 161411 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 4.8 COc1ccc(C(OCCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)cc1 10.1016/j.bmcl.2018.03.051
155517179 170141 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
CHEMBL4444223 170141 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
1050 1900 94 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1900 94 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1900 94 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
145962072 162366 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 505 7 1 3 6.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4165184 162366 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 505 7 1 3 6.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.ejmech.2018.04.023
127048844 140196 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1nnc(C(=O)Nc2ccc(OCc3ccccc3)cc2)s1 10.1016/j.bmc.2016.04.065
CHEMBL3804883 140196 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 383 8 2 6 3.4 O=C(O)CCc1nnc(C(=O)Nc2ccc(OCc3ccccc3)cc2)s1 10.1016/j.bmc.2016.04.065
57414402 75612 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047152 75612 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414543 75621 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
CHEMBL2047162 75621 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
57414679 75625 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
CHEMBL2047166 75625 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
131986115 164713 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4217348 164713 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
46231780 200803 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 415 4 1 4 5.4 Cc1cc(Oc2ccc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL600799 200803 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 415 4 1 4 5.4 Cc1cc(Oc2ccc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
90644299 111964 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288357 111964 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
162667620 182555 0 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 182555 0 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
131986075 163907 0 None 2 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207273 163907 0 None 2 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
11674915 58860 1 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL1688486 58860 1 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
118645715 181485 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764729 181485 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
118623088 142125 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 142125 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
73345869 90360 0 None 75 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 321 5 1 2 3.7 N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386355 90360 0 None 75 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 321 5 1 2 3.7 N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
66562488 90369 0 None 64 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 4 1 1 4.3 O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F 10.1021/ml4000673
CHEMBL2386364 90369 0 None 64 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 4 1 1 4.3 O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F 10.1021/ml4000673
145970463 165174 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
CHEMBL4228406 165174 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
46941175 61810 26 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
CHEMBL1773261 61810 26 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
46941175 61810 26 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61810 26 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
46941175 61810 26 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
CHEMBL1773261 61810 26 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm3002026
57402427 70019 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 6 1 2 4.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939648 70019 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 6 1 2 4.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.10.118
121294843 182502 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 543 11 1 6 5.6 COc1ccc(C(=O)N(C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4786992 182502 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 543 11 1 6 5.6 COc1ccc(C(=O)N(C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
137638341 156767 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 544 7 1 7 5.0 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4070721 156767 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 544 7 1 7 5.0 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
23111671 74055 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
CHEMBL2022254 74055 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
58230552 182217 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
853224 94573 11 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94573 11 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
51350134 58843 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 7 1 2 6.3 Cc1cccc(C)c1-c1cccc(CSc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688469 58843 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 7 1 2 6.3 Cc1cccc(C)c1-c1cccc(CSc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
168289957 191627 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 398 13 1 4 5.7 COc1ccc(/C=C/c2cc(OC)cc(OCCCCCCCC(=O)O)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5195742 191627 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 398 13 1 4 5.7 COc1ccc(/C=C/c2cc(OC)cc(OCCCCCCCC(=O)O)c2)cc1 10.1016/j.ejmech.2021.114061
142738583 162352 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 293 5 2 1 4.4 CCc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
CHEMBL4165039 162352 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 293 5 2 1 4.4 CCc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
142738569 162742 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3cccc(Br)c3)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4171403 162742 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3cccc(Br)c3)cc2c1 10.1021/acsmedchemlett.7b00460
1052 2319 85 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2319 85 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2319 85 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2319 85 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2319 85 None -5 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
145987969 167067 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 346 4 1 2 4.5 O=C(O)C#Cc1ccc(OCc2cccc(-c3cccc(F)c3)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4289432 167067 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 346 4 1 2 4.5 O=C(O)C#Cc1ccc(OCc2cccc(-c3cccc(F)c3)c2)cc1 10.1016/j.ejmech.2018.08.075
137638355 156827 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4071290 156827 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
60195125 3886 8 None -4 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3886 8 None -4 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3886 8 None -4 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at GPR40 in rat INS-1E cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
24825509 87944 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL234057 87944 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
127033353 139149 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 5 1 1 3.7 O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3787151 139149 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 5 1 1 3.7 O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
134134229 143253 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 assessed as induction of IP1 accumulationAgonist activity at human GPR40 assessed as induction of IP1 accumulation
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1021/acsmedchemlett.6b00360
CHEMBL3896657 143253 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 assessed as induction of IP1 accumulationAgonist activity at human GPR40 assessed as induction of IP1 accumulation
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1021/acsmedchemlett.6b00360
134134229 143253 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1016/j.bmcl.2016.10.054
CHEMBL3896657 143253 0 None -61 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 10.1016/j.bmcl.2016.10.054
57706097 163740 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4205339 163740 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
58319126 86515 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 292 4 1 2 3.3 CC(=O)c1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315248 86515 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 292 4 1 2 3.3 CC(=O)c1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
54757734 65342 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 327 4 1 2 4.2 O=C(O)CCc1ccc(C#Cc2ccnc(-c3ccccc3)c2)cc1 10.1021/jm2005699
CHEMBL1829162 65342 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 327 4 1 2 4.2 O=C(O)CCc1ccc(C#Cc2ccnc(-c3ccccc3)c2)cc1 10.1021/jm2005699
54586984 61805 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
CHEMBL1773256 61805 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
23136477 58828 3 None -15 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL1688455 58828 3 None -15 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL4213909 58828 3 None -15 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
37289 166520 19 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCC(O)CCCCC(=O)O 10.1039/C7MD00130D
CHEMBL4279005 166520 19 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCC(O)CCCCC(=O)O 10.1039/C7MD00130D
127051856 140725 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL3817889 140725 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at eYFP-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
145956671 162064 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4160566 162064 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
46231715 200947 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 334 4 1 5 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL601850 200947 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 334 4 1 5 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
25766502 122513 3 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 6 1 5 3.6 O=C(O)Cc1ccc(OCc2nc(-c3cccc(Cl)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601061 122513 3 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 6 1 5 3.6 O=C(O)Cc1ccc(OCc2nc(-c3cccc(Cl)c3)no2)cc1 10.1016/j.bmcl.2015.06.018
127027011 137627 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 7 1 6 4.2 CC(C)Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
CHEMBL3758197 137627 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 7 1 6 4.2 CC(C)Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
51350406 58861 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1C 10.1021/jm101405t
CHEMBL1688487 58861 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1C 10.1021/jm101405t
10668 1951 16 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.bmcl.2021.127969
139600331 1951 16 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.bmcl.2021.127969
CHEMBL5169614 1951 16 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 10.1016/j.bmcl.2021.127969
44572033 179574 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 548 13 1 5 7.8 O=C(O)CCc1ccc(OCc2ccc(CC(CCc3ccccn3)c3nc(-c4ccccc4)cs3)cc2)cc1 10.1016/j.bmcl.2008.10.085
CHEMBL474195 179574 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 548 13 1 5 7.8 O=C(O)CCc1ccc(OCc2ccc(CC(CCc3ccccn3)c3nc(-c4ccccc4)cs3)cc2)cc1 10.1016/j.bmcl.2008.10.085
90655862 111249 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265146 111249 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
57414680 75626 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047167 75626 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414542 77214 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047161 77214 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2079433 77214 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
131986140 163518 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202612 163518 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
67058227 119132 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427713 119132 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
122185436 122673 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604041 122673 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
67087246 182875 5 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
131986140 163518 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202612 163518 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986132 163857 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206640 163857 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986051 163881 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206968 163881 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118642372 162462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166943 162462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
71613314 89995 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381308 89995 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
149454889 169729 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3Cl)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4438440 169729 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3Cl)c2)cc1F 10.1016/j.ejmech.2019.06.087
67072752 86527 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315528 86527 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
67072752 86527 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL2315528 86527 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
58172999 122696 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 356 8 1 4 4.3 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3c(OC)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604064 122696 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 356 8 1 4 4.3 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3c(OC)cccc32)cc1 10.1016/j.bmc.2015.07.028
58218571 157478 0 None 17 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079421 157478 0 None 17 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
90151435 159716 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 554 8 1 7 5.6 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4104467 159716 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 554 8 1 7 5.6 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
162666840 182452 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 182452 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
58172989 111967 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288360 111967 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
71613519 89975 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381288 89975 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1ccc(Cl)c(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
71562770 86528 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315529 86528 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
145965707 164201 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4210871 164201 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
71451164 80661 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3ccc(CCC(=O)O)cc3)cc2)c1 10.1021/ml300133f
CHEMBL2151291 80661 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3ccc(CCC(=O)O)cc3)cc2)c1 10.1021/ml300133f
57706588 80668 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151298 80668 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
137638269 156874 0 None -8 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4071899 156874 0 None -8 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218640 158920 0 None -15 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4095599 158920 0 None -15 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
1202260 95034 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 313 5 1 5 2.8 O=C(O)CCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL255071 95034 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 313 5 1 5 2.8 O=C(O)CCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
25098573 2745 8 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm800970b
5587 2745 8 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm800970b
CHEMBL463785 2745 8 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm800970b
137633489 156598 0 None -9 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
CHEMBL4068825 156598 0 None -9 2 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
137647888 157716 0 None - 1 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 369 4 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@H]4C(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4082057 157716 0 None - 1 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 369 4 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@H]4C(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
23136477 58828 3 None -15 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
CHEMBL1688455 58828 3 None -15 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
CHEMBL4213909 58828 3 None -15 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/ml100106c
127046834 139657 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1ccnc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797836 139657 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1ccnc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
90151202 157369 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 461 6 1 5 5.0 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4078050 157369 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 461 6 1 5 5.0 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
24825509 87944 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234057 87944 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
145976145 163811 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 412 8 1 5 3.8 COc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4206179 163811 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 412 8 1 5 3.8 COc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
145971779 164470 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 378 7 1 3 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(SCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4214140 164470 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 378 7 1 3 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(SCC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
66562388 90372 0 None 33 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386367 90372 0 None 33 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 360 5 1 3 2.8 CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
60195125 3886 8 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3886 8 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3886 8 None 4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
127027726 137826 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 5.2 COc1cccc(O[C@@H](CCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)c1 10.1016/j.ejmech.2015.12.049
CHEMBL3759866 137826 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 463 10 1 6 5.2 COc1cccc(O[C@@H](CCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)c1 10.1016/j.ejmech.2015.12.049
137641343 157055 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4074009 157055 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
153211729 172898 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 405 9 2 4 5.4 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4516052 172898 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 405 9 2 4 5.4 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
57705575 164150 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4210239 164150 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
134465785 176109 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 176109 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
54586984 61805 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
CHEMBL1773256 61805 0 None 34 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
71562314 86534 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.7 CC(CC(=O)O)c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315535 86534 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.7 CC(CC(=O)O)c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
25149901 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm2005699
CHEMBL488384 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm2005699
127030714 139084 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 254 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2=CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786524 139084 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 254 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2=CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
25149901 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL488384 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
25149901 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml4000673
CHEMBL488384 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml4000673
25149901 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml100106c
CHEMBL488384 186684 1 None 61 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/ml100106c
24825494 88030 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234468 88030 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2006.12.084
24825493 149850 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 295 6 2 3 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)s2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL394900 149850 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 295 6 2 3 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)s2)cc1 10.1016/j.bmcl.2006.12.084
137638911 156727 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4070298 156727 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
137638355 156827 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4071290 156827 0 None -97 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
137641343 157055 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4074009 157055 0 None -117 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 342 8 1 3 4.7 Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
164626510 186335 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 549 8 1 4 7.1 C[C@H](C(=O)O)[C@@H](c1ccc2c(c1)O[C@@H](C1CCN([C@@H](C)c3cc(F)ccc3OC(F)(F)F)CC1)CC2)C1CC1 10.1021/acs.jmedchem.1c00031
CHEMBL4874972 186335 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 549 8 1 4 7.1 C[C@H](C(=O)O)[C@@H](c1ccc2c(c1)O[C@@H](C1CCN([C@@H](C)c3cc(F)ccc3OC(F)(F)F)CC1)CC2)C1CC1 10.1021/acs.jmedchem.1c00031
134465732 171473 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4463571 171473 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
137529972 164761 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 556 8 3 8 5.2 Cc1cc(-c2nnn(CC(C)(C)O)n2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4217914 164761 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 556 8 3 8 5.2 Cc1cc(-c2nnn(CC(C)(C)O)n2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
118129999 157765 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157765 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
118645685 179866 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4745513 179866 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
118645756 181460 7 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 181460 7 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
131986061 164114 0 None 6 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209834 164114 0 None 6 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1 10.1016/j.bmcl.2017.12.022
155528372 171315 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4461095 171315 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
67087095 183373 0 None -6 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 183373 0 None -6 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134465730 172801 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4513748 172801 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
162674998 183389 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 183389 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
118637996 142168 0 None 15 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 142168 0 None 15 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 142168 0 None 15 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
164625212 185981 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3c(Cl)cccc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
CHEMBL4869870 185981 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3c(Cl)cccc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
44409722 141014 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382381 141014 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
118645789 180055 0 None 11 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
CHEMBL4747793 180055 0 None 11 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
118623101 167587 0 None -12 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4159416 167587 0 None -12 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4300796 167587 0 None -12 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
118642344 142120 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883380 142120 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc([C@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
90356885 167533 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 167533 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 167533 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
68194127 183193 0 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 183193 0 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194465 183304 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 183304 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
51350404 58858 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1021/jm101405t
CHEMBL1688484 58858 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1021/jm101405t
67072752 86527 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315528 86527 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
66562288 139007 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3785637 139007 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
131986401 163982 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4208095 163982 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986050 164484 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4214289 164484 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
45107307 111969 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1021/ml500391n
CHEMBL3288362 111969 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1021/ml500391n
45107307 111969 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3288362 111969 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
122185452 122699 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 395 7 1 4 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
CHEMBL3604067 122699 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 395 7 1 4 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
45107307 111969 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288362 111969 4 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
155549083 173666 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4534836 173666 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
145952952 162489 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167323 162489 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
23082877 75820 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
CHEMBL2048613 75820 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
162668378 182505 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 182505 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
131986065 163851 0 None 4 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206579 163851 0 None 4 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986050 164484 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4214289 164484 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
66562288 139007 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3785637 139007 0 None 1000 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
164618830 185759 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
CHEMBL4866406 185759 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
155519364 170375 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 476 8 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4F)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4447826 170375 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 476 8 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4F)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
145987796 167124 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 464 6 1 4 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Br)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4290397 167124 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 464 6 1 4 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Br)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
118645367 181660 0 None -5 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4776217 181660 0 None -5 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
134153546 152579 0 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 371 6 1 4 4.4 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3971857 152579 0 None -8 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 371 6 1 4 4.4 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
137632610 156344 0 None 2 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4065890 156344 0 None 2 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 368 5 1 5 4.0 N#Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
134139528 154536 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3921121 154536 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990894 154536 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137657027 159578 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 373 7 1 4 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccncc3Cl)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4102878 159578 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 373 7 1 4 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccncc3Cl)c2)s1 10.1021/acs.jmedchem.6b01357
46231486 200342 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL597638 200342 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
145949924 162866 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 507 8 1 6 4.4 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4173246 162866 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 507 8 1 6 4.4 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
51349861 58827 0 None 77 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL1688454 58827 0 None 77 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/ml100106c
44409883 141227 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 500 7 3 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCNC2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382884 141227 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 500 7 3 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCNC2)cc1 10.1016/j.bmcl.2006.01.007
44409906 76784 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2019.06.087
CHEMBL206880 76784 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2019.06.087
57521814 76267 0 None -10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 362 8 1 3 5.0 COc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058525 76267 0 None -10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 362 8 1 3 5.0 COc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
58319089 86517 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CCO)cc1 10.1021/jm301470a
CHEMBL2315250 86517 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CCO)cc1 10.1021/jm301470a
44409906 76784 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206880 76784 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 349 8 2 4 4.6 O=C(O)COc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
71615469 89990 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(F)cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381303 89990 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(F)cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
137630008 161029 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 561 12 1 5 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4077784 161029 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 561 12 1 5 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116425 161029 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 561 12 1 5 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
46231595 200192 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3cc(Cl)cc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL596666 200192 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3cc(Cl)cc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
127031002 139085 0 None 165 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C/C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3786526 139085 0 None 165 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C/C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
10466 166668 80 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 272 15 2 2 4.5 O=C(O)CCCCCCCCCCCCCCCO 10.1039/C7MD00130D
CHEMBL4281719 166668 80 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay
ChEMBL 272 15 2 2 4.5 O=C(O)CCCCCCCCCCCCCCCO 10.1039/C7MD00130D
46231435 200604 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 309 4 1 3 3.8 O=C1NC(=O)C(Cc2ccc(/C=C/c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599271 200604 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 309 4 1 3 3.8 O=C1NC(=O)C(Cc2ccc(/C=C/c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
45107320 122698 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 396 7 1 4 4.8 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604066 122698 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 396 7 1 4 4.8 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
23111791 74053 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022252 74053 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
67087095 183373 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 183373 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
131986250 163683 0 None 3 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204776 163683 0 None 3 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986130 164423 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213597 164423 0 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
162652399 180226 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4749949 180226 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
71460547 81718 27 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
CHEMBL2163923 81718 27 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
75511310 122456 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 352 8 1 5 3.9 CCc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601000 122456 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 352 8 1 5 3.9 CCc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
145973329 164733 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(OCc2ccc(-c3cc(OC)ccc3F)c(C3CCCC3(C)C)c2)ccc1F 10.1021/acsmedchemlett.8b00213
CHEMBL4217580 164733 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(OCc2ccc(-c3cc(OC)ccc3F)c(C3CCCC3(C)C)c2)ccc1F 10.1021/acsmedchemlett.8b00213
137648439 157878 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 396 8 1 4 5.8 COC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4083960 157878 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 396 8 1 4 5.8 COC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
137654021 158790 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 404 7 1 3 6.2 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4094216 158790 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 404 7 1 3 6.2 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
58172998 122665 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(F)c1 10.1016/j.bmc.2015.07.028
CHEMBL3604034 122665 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(F)c1 10.1016/j.bmc.2015.07.028
75204360 157615 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 7 1 5 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4081072 157615 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 7 1 5 5.1 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
145982132 166567 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 370 6 1 4 3.6 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4279826 166567 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 370 6 1 4 3.6 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145993162 166979 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Br)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4287731 166979 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Br)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145988796 167297 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(F)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4293798 167297 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 6 1 4 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(F)c(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
132606863 157821 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157821 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
90644287 111952 0 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288345 111952 0 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
71449363 80672 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 518 9 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151301 80672 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 518 9 1 3 8.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
25261467 80793 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(F)(F)F)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2152068 80793 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 504 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(F)(F)F)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
168273292 190531 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 409 7 1 5 5.1 O=C(O)COc1ccc(COc2cccc(-c3nc4ccccc4s3)c2)cc1F 10.1016/j.ejmech.2021.114061
CHEMBL5179638 190531 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 409 7 1 5 5.1 O=C(O)COc1ccc(COc2cccc(-c3nc4ccccc4s3)c2)cc1F 10.1016/j.ejmech.2021.114061
122185441 122682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 315 8 1 4 3.5 CCOC(CC(=O)O)c1ccc(OCc2cccnc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604050 122682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 315 8 1 4 3.5 CCOC(CC(=O)O)c1ccc(OCc2cccnc2C)cc1 10.1016/j.bmc.2015.07.028
137637488 155915 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 4.5 O=C(O)C1CCN(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4060859 155915 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 4.5 O=C(O)C1CCN(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
134155480 151249 0 None -38 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 384 5 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3960231 151249 0 None -38 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 384 5 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
145989566 167154 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 377 6 1 5 3.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C#N)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4290886 167154 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 377 6 1 5 3.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C#N)cc3O2)cc1 10.1016/j.bmc.2018.10.019
137651638 157219 0 None -7 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4076190 157219 0 None -7 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
90644297 111962 0 None -32 2 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288355 111962 0 None -32 2 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
25109512 189762 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 382 10 1 5 4.8 O=C(O)CCCc1ccc(OCCN(c2ccccc2)c2nccs2)cc1 10.1021/jm800970b
CHEMBL515995 189762 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 382 10 1 5 4.8 O=C(O)CCCc1ccc(OCCN(c2ccccc2)c2nccs2)cc1 10.1021/jm800970b
127025866 137711 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 7 1 6 3.7 C=CCn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
CHEMBL3758885 137711 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 7 1 6 3.7 C=CCn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21 10.1016/j.ejmech.2015.12.049
145956069 162695 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4170517 162695 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 502 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
145989900 167021 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 360 7 1 4 3.6 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
CHEMBL4288499 167021 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 360 7 1 4 3.6 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
86803188 122502 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 356 7 1 5 3.8 Cc1cc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)ccc1F 10.1016/j.bmcl.2015.06.018
CHEMBL3601050 122502 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 356 7 1 5 3.8 Cc1cc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)ccc1F 10.1016/j.bmcl.2015.06.018
131986164 164617 0 None -1 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216016 164617 0 None -1 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145966699 164272 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1cc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)ccc1Cl 10.1016/j.ejmech.2017.07.001
CHEMBL4211760 164272 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1cc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)ccc1Cl 10.1016/j.ejmech.2017.07.001
145972079 164564 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 417 7 1 6 3.9 Cc1cccc(-c2nc(C)c(COc3ccc(S(=O)(=O)CC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4215289 164564 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 417 7 1 6 3.9 Cc1cccc(-c2nc(C)c(COc3ccc(S(=O)(=O)CC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.07.001
145960453 161490 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 433 9 1 5 4.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccccc3)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4127972 161490 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 433 9 1 5 4.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccccc3)cc2)S1 10.1016/j.bmcl.2018.03.051
71655225 90361 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)cn1 10.1021/ml4000673
CHEMBL2386356 90361 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)cn1 10.1021/ml4000673
54586010 61796 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(CNc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773247 61796 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(CNc2ccccc2)cc1 10.1021/ml100106c
127045888 139666 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 393 6 1 4 4.4 Cc1noc(C)c1C#Cc1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797889 139666 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 393 6 1 4 4.4 Cc1noc(C)c1C#Cc1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
118145019 173654 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 464 8 1 3 6.7 COc1ccc(F)c(-c2cc(F)c3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4534543 173654 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 464 8 1 3 6.7 COc1ccc(F)c(-c2cc(F)c3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
145976702 163952 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4207755 163952 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
137638911 156727 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4070298 156727 0 None -32 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 384 7 1 3 5.5 Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
46231716 201678 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(C(F)(F)F)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
CHEMBL606207 201678 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(C(F)(F)F)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
24825484 87989 0 None 208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm300215x
CHEMBL234269 87989 0 None 208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm300215x
58319118 86551 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315552 86551 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
71613517 89973 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381286 89973 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
154005 163279 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 366 6 1 5 3.6 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL418695 163279 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 366 6 1 5 3.6 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
90655863 111251 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265148 111251 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
57414405 75615 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047155 75615 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111781 74048 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022247 74048 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
134465730 172801 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4513748 172801 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
11674915 58860 1 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL1688486 58860 1 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
68194476 182885 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182885 0 None -6 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
134131511 142156 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 142156 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
71655227 90367 0 None 173 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386362 90367 0 None 173 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
155548258 173764 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 399 7 2 3 5.5 Cc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(Cl)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4537190 173764 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 399 7 2 3 5.5 Cc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(Cl)c1 10.1016/j.ejmech.2019.06.087
127047528 139767 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(COc2ccc(CCC(=O)O)c(F)c2)cc1-c1c(C)noc1C 10.1016/j.ejmech.2016.03.054
CHEMBL3798575 139767 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(COc2ccc(CCC(=O)O)c(F)c2)cc1-c1c(C)noc1C 10.1016/j.ejmech.2016.03.054
168269875 190016 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 410 9 1 4 5.2 CCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5171641 190016 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 410 9 1 4 5.2 CCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
155511380 169554 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4435633 169554 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
155526126 171047 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 429 7 1 5 4.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccnc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4456918 171047 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 429 7 1 5 4.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccnc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
137633101 156576 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 380 6 1 4 4.4 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cn1 10.1021/acs.jmedchem.6b01559
CHEMBL4068606 156576 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 380 6 1 4 4.4 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cn1 10.1021/acs.jmedchem.6b01559
137638269 156874 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4071899 156874 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
90151625 157725 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 523 8 1 6 5.5 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4082133 157725 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 523 8 1 6 5.5 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
155551422 173965 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4541658 173965 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 454 9 1 3 6.8 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(C)(C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
57706720 80667 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 9 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(C)C)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151297 80667 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 9 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C(C)C)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
16738034 85764 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretionAgonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretion
ChEMBL 326 9 1 2 5.1 CCC(CC)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm070130j
CHEMBL229225 85764 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretionAgonist activity at GPR40 in mouse MIN6 cells assessed as stimulation of 25 mM glucose-mediated insulin secretion
ChEMBL 326 9 1 2 5.1 CCC(CC)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm070130j
1050 1900 94 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1900 94 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1900 94 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
134155847 151100 0 None -63 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 418 5 1 3 5.6 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3959144 151100 0 None -63 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 418 5 1 3 5.6 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 10.1021/acsmedchemlett.6b00394
145985116 165894 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 7 1 4 6.1 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(C(=O)c4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4249862 165894 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 7 1 4 6.1 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(C(=O)c4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
46231484 200313 3 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 283 3 1 3 3.2 O=C1NC(=O)C(Cc2ccc(-c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL597435 200313 3 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 283 3 1 3 3.2 O=C1NC(=O)C(Cc2ccc(-c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
71562527 86553 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2ccccc2OC(F)(F)F)cc1 10.1021/jm301470a
CHEMBL2315554 86553 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2ccccc2OC(F)(F)F)cc1 10.1021/jm301470a
1050 1900 94 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1900 94 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1900 94 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
53248848 62166 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 62166 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
145992642 166893 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3ccc(Br)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4286165 166893 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3ccc(Br)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
149378333 171881 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 370 7 2 5 4.2 Cc1noc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4469534 171881 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 370 7 2 5 4.2 Cc1noc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
1201222 155125 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 325 5 1 4 2.9 O=C(O)CCCN1C(=O)/C(=C\c2ccc(F)cc2)SC1=S 10.1021/jm7012425
CHEMBL402054 155125 9 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 325 5 1 4 2.9 O=C(O)CCCN1C(=O)/C(=C\c2ccc(F)cc2)SC1=S 10.1021/jm7012425
46231651 199417 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ncccc3C(F)(F)F)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL591214 199417 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ncccc3C(F)(F)F)cc2)S1 10.1016/j.bmcl.2009.10.052
71562313 86533 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.5 Cc1ccccc1C#Cc1ccc(/C=C/C(=O)O)cc1 10.1021/jm301470a
CHEMBL2315534 86533 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 262 2 1 1 3.5 Cc1ccccc1C#Cc1ccc(/C=C/C(=O)O)cc1 10.1021/jm301470a
131986057 163653 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204345 163653 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23111704 74045 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022244 74045 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
58172961 122676 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 392 10 1 4 5.6 CCOC(CC(=O)O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604044 122676 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 392 10 1 4 5.6 CCOC(CC(=O)O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmc.2015.07.028
11236925 75826 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048619 75826 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
12002202 75832 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048626 75832 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
67087160 182342 0 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 182342 0 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182984 0 None -13 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182984 0 None -13 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
145952952 162489 0 None -1 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167323 162489 0 None -1 3 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
46854655 395 47 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
6485 395 47 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
CHEMBL1829173 395 47 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2011.10.118
118637972 162315 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4164618 162315 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
90372616 142231 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
60195039 81791 0 None 181 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 8 2 2 5.7 CCc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL2164240 81791 0 None 181 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 377 8 2 2 5.7 CCc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
118645392 180107 0 None -2 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4748392 180107 0 None -2 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
90644302 111968 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288361 111968 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
71456495 80657 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
CHEMBL2151287 80657 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
71449362 80660 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 418 8 1 3 5.7 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cc(OC)ccc3F)cc2)cc1 10.1021/ml300133f
CHEMBL2151290 80660 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 418 8 1 3 5.7 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cc(OC)ccc3F)cc2)cc1 10.1021/ml300133f
58218655 156163 0 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4063889 156163 0 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
145955723 162534 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4167970 162534 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
127025858 137734 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3ccc(Br)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759133 137734 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3ccc(Br)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
137635513 156108 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2csc(CCC(=O)O)c2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4063167 156108 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2csc(CCC(=O)O)c2)c1 10.1021/acs.jmedchem.6b01357
164609159 184471 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN3CCC4(CCc5ccccc54)CC3)c2)cc1 10.1021/acs.jmedchem.1c00031
CHEMBL4846948 184471 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN3CCC4(CCc5ccccc54)CC3)c2)cc1 10.1021/acs.jmedchem.1c00031
51049992 145617 5 None -23 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmcl.2016.10.074
CHEMBL3915620 145617 5 None -23 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by calcium-4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmcl.2016.10.074
145976748 163546 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 5.7 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(=O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4202936 163546 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 5.7 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(=O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
145976172 163874 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4206875 163874 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 435 7 1 6 4.0 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
46231922 201338 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 452 4 1 5 5.6 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)c3ccccc23)S1 10.1016/j.bmcl.2009.10.052
CHEMBL604317 201338 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 452 4 1 5 5.6 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)c3ccccc23)S1 10.1016/j.bmcl.2009.10.052
137628912 160978 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 594 12 1 6 7.1 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc5ccccc5n3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4101806 160978 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 594 12 1 6 7.1 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc5ccccc5n3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116012 160978 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 594 12 1 6 7.1 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc5ccccc5n3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
46231652 201110 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cc(C(F)(F)F)ccn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL603063 201110 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cc(C(F)(F)F)ccn3)cc2)S1 10.1016/j.bmcl.2009.10.052
145991968 166835 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 10 1 5 3.6 COCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
CHEMBL4285148 166835 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 404 10 1 5 3.6 COCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
46231547 202125 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(C)c(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL609034 202125 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(C)c(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
145986696 167212 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)C[C@@H]1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4291932 167212 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)C[C@@H]1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
131986162 164834 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218822 164834 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
24825492 149540 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/jm300215x
CHEMBL394666 149540 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1021/jm300215x
75511298 122503 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.9 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccccc2)no1 10.1016/j.bmcl.2015.06.018
CHEMBL3601051 122503 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.9 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccccc2)no1 10.1016/j.bmcl.2015.06.018
145975621 163752 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4205508 163752 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
145974509 164747 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4217742 164747 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 7 2 5 4.1 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(Cl)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
57414401 75611 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047151 75611 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
23111693 74056 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
CHEMBL2022255 74056 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
162676881 183583 0 None -10 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183583 0 None -10 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
131986115 164713 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4217348 164713 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145947998 167714 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167714 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167714 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
149144496 175189 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 9 2 4 5.6 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4570807 175189 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 9 2 4 5.6 CCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
127045864 139736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(-c2c(C)noc2C)cc1COc1ccc(CCC(=O)O)c(F)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798341 139736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1ccc(-c2c(C)noc2C)cc1COc1ccc(CCC(=O)O)c(F)c1 10.1016/j.ejmech.2016.03.054
127046960 139989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799946 139989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL4227915 139989 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
51350271 58838 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
CHEMBL1688464 58838 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
149231065 175433 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4576378 175433 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
46231594 200901 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL601504 200901 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
57390188 70023 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939652 70023 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
137648780 157598 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4080911 157598 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
5353640 161489 15 None - 1 Human 6.6 pEC50 = 6.6 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C/C/C=C/C/C=C/CCCCC(=O)O 10.1016/j.bmcl.2018.03.051
CHEMBL4127920 161489 15 None - 1 Human 6.6 pEC50 = 6.6 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C/C/C=C/C/C=C/CCCCC(=O)O 10.1016/j.bmcl.2018.03.051
132606864 157744 0 None 2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157744 0 None 2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assayAgonist activity at human GPR40 transfected in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 to 45 mins by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
137635715 156074 0 None -9 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4062765 156074 0 None -9 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
132606864 157744 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157744 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
137652992 158647 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(OCc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4092577 158647 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(OCc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
90356885 167533 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 167533 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 167533 0 None -16 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
145976979 163996 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 413 9 2 7 3.4 COc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4208272 163996 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 413 9 2 7 3.4 COc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
145985686 165428 0 None -354 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 358 7 1 3 4.2 COc1cc(F)c(F)c(-c2cc(F)c(OCCCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2018.06.047
CHEMBL4238809 165428 0 None -354 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 358 7 1 3 4.2 COc1cc(F)c(F)c(-c2cc(F)c(OCCCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2018.06.047
54580627 62165 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777875 62165 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
155528372 171315 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4461095 171315 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 479 8 1 4 6.3 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c(F)cn1 10.1016/j.bmcl.2019.04.050
54586983 61800 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 266 4 1 2 4.1 O=C(O)CCc1ccc2oc(-c3ccccc3)cc2c1 10.1021/ml100106c
CHEMBL1773251 61800 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 266 4 1 2 4.1 O=C(O)CCc1ccc2oc(-c3ccccc3)cc2c1 10.1021/ml100106c
763016 95035 26 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 271 4 2 4 2.7 O=C(O)c1ccc(NCc2ccc3c(c2)OCO3)cc1 10.1021/jm7012425
CHEMBL255073 95035 26 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 271 4 2 4 2.7 O=C(O)c1ccc(NCc2ccc3c(c2)OCO3)cc1 10.1021/jm7012425
145947998 167714 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167714 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167714 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
54582629 62154 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 62154 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
118637996 142168 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 142168 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 142168 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
118637996 142168 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 142168 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 142168 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
21322577 62149 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 324 5 1 2 5.4 CC(CC(=O)O)c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777859 62149 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 324 5 1 2 5.4 CC(CC(=O)O)c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
53248848 62166 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 62166 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
131986300 163625 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203837 163625 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
57393692 70025 11 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939654 70025 11 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.118
11226058 75828 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048622 75828 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
11203294 75829 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048623 75829 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
145950347 162836 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172828 162836 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
11203294 75829 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
FLIPR functional assay (Ca influx activity of CHO cells)FLIPR functional assay (Ca influx activity of CHO cells)
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 75829 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
FLIPR functional assay (Ca influx activity of CHO cells)FLIPR functional assay (Ca influx activity of CHO cells)
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
90372616 142231 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
127045866 140035 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1F 10.1016/j.ejmech.2016.03.054
CHEMBL3800232 140035 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1F 10.1016/j.ejmech.2016.03.054
71460547 81718 27 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
CHEMBL2163923 81718 27 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSAAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.05% BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
127045865 139729 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1F 10.1016/j.ejmech.2016.03.054
CHEMBL3798274 139729 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1F 10.1016/j.ejmech.2016.03.054
162671590 182959 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 479 12 1 4 6.5 COc1ccc(CCCC(C)(C)C)c(N2CC(COc3cccc(C(CC(=O)O)C4CC4)c3)C2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4792979 182959 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 479 12 1 4 6.5 COc1ccc(CCCC(C)(C)C)c(N2CC(COc3cccc(C(CC(=O)O)C4CC4)c3)C2)c1 10.1021/acs.jmedchem.0c00843
90151466 156274 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 529 6 1 5 6.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4065150 156274 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 529 6 1 5 6.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
90644296 111961 0 None -29 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288354 111961 0 None -29 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
90644295 111960 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288353 111960 0 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
73777156 152713 0 None -18 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 396 4 1 4 4.7 N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 10.1021/acsmedchemlett.6b00360
CHEMBL3973034 152713 0 None -18 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 396 4 1 4 4.7 N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 10.1021/acsmedchemlett.6b00360
134151115 152197 0 None -72 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 336 6 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
CHEMBL3968537 152197 0 None -72 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 336 6 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 10.1016/j.bmcl.2016.10.054
24825490 87479 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.6 O=C(O)CCc1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL233402 87479 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 323 6 2 2 4.6 O=C(O)CCc1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2006.12.084
24825484 87989 0 None 208 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234269 87989 0 None 208 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
145966632 164159 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 437 7 1 6 4.2 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4210351 164159 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 437 7 1 6 4.2 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54757624 65335 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 256 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccs2)cc1 10.1021/jm2005699
CHEMBL1829155 65335 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 256 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccs2)cc1 10.1021/jm2005699
71655226 90362 0 None 36 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 10.1021/ml4000673
CHEMBL2386357 90362 0 None 36 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 10.1021/ml4000673
118642384 142163 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883790 142163 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
145973781 164731 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c(C)c1 10.1016/j.ejmech.2017.09.019
CHEMBL4217530 164731 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c(C)c1 10.1016/j.ejmech.2017.09.019
90151537 156445 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 479 6 1 5 5.1 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(F)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4067111 156445 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 479 6 1 5 5.1 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(F)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
137645353 161212 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cccnc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4083311 161212 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cccnc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117885 161212 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cccnc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
118642372 162462 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166943 162462 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
145965138 164459 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 400 7 1 4 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4214028 164459 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 400 7 1 4 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3F)c2)cc1 10.1016/j.ejmech.2017.07.001
75511308 122504 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 330 7 1 6 3.4 O=C(O)CCc1ccc(OCc2nc(-c3cccs3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601052 122504 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 330 7 1 6 3.4 O=C(O)CCc1ccc(OCc2nc(-c3cccs3)no2)cc1 10.1016/j.bmcl.2015.06.018
46231781 200804 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 436 4 1 5 5.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
CHEMBL600800 200804 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 436 4 1 5 5.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
121294363 183078 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 599 12 1 6 7.0 COc1ccc(C(=O)N(CC(C)(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4794401 183078 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 599 12 1 6 7.0 COc1ccc(C(=O)N(CC(C)(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
71460547 81718 27 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
CHEMBL2163923 81718 27 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm3002026
23157282 77218 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048628 77218 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2079469 77218 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
131986182 164619 0 None 3 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216026 164619 0 None 3 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23136411 58830 0 None 11 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688457 58830 0 None 11 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm101405t
51349991 58852 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 10 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCCc3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688478 58852 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 10 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCCc3ccccc3)c2)cc1 10.1021/jm101405t
44572095 14910 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 5 4.0 Cc1cccc(C)c1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2008.10.085
CHEMBL1208013 14910 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 5 4.0 Cc1cccc(C)c1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2008.10.085
CHEMBL475053 14910 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 402 6 1 5 4.0 Cc1cccc(C)c1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2008.10.085
168284831 191290 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 8 1 4 4.9 COc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5190883 191290 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 8 1 4 4.9 COc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
42603138 70014 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939643 70014 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
137630491 161078 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1cccc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4098843 161078 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1cccc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
CHEMBL4116766 161078 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 558 12 1 6 6.2 Cc1cccc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1 10.1016/j.ejmech.2017.01.005
137635715 156074 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4062765 156074 0 None 9 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01559
137638184 156754 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070619 156754 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
145981983 166667 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4281717 166667 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
118737974 119134 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427715 119134 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
137642248 158151 0 None 1 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
CHEMBL4087308 158151 0 None 1 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 10.1021/acs.jmedchem.7b00210
137641818 158205 0 None -10 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 373 6 1 5 4.1 COc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4087992 158205 0 None -10 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 373 6 1 5 4.1 COc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 10.1021/acs.jmedchem.7b00210
137643731 158384 0 None -5 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 361 5 1 4 4.2 O=C(O)CCc1ccc(-c2cc(F)c3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
CHEMBL4089919 158384 0 None -5 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 361 5 1 4 4.2 O=C(O)CCc1ccc(-c2cc(F)c3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
90151624 156143 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccn4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4063627 156143 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccn4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
46231714 201019 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
CHEMBL602289 201019 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)n1 10.1016/j.bmcl.2009.10.052
71562772 86530 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315531 86530 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
51350272 58839 0 None 107 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58839 0 None 107 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
75511299 122505 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2noc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601053 122505 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2noc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
53248848 62166 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 62166 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
75511306 122506 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 354 8 1 6 3.3 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601054 122506 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 354 8 1 6 3.3 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)c1 10.1016/j.bmcl.2015.06.018
145977404 163845 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 401 7 1 6 3.4 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4206505 163845 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 401 7 1 6 3.4 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
51350272 58839 0 None 107 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688465 58839 0 None 107 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
24857286 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
6484 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
CHEMBL1829174 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
DB12491 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b01357
58172979 122664 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 367 8 2 3 5.2 CCOC(CC(=O)O)c1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604033 122664 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 367 8 2 3 5.2 CCOC(CC(=O)O)c1ccc(NCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
23111704 74045 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022244 74045 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
23111781 74048 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022247 74048 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
145968204 165185 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 379 6 1 5 4.5 Cc1noc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4228620 165185 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 379 6 1 5 4.5 Cc1noc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
24857286 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
6484 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
CHEMBL1829174 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
DB12491 1622 72 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2016.03.054
168271964 190107 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 432 8 1 4 5.7 COc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
CHEMBL5173019 190107 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 432 8 1 4 5.7 COc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
57414403 75613 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047153 75613 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
146314264 182315 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 423 9 1 4 5.3 COc1ccc(C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4784293 182315 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 423 9 1 4 5.3 COc1ccc(C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
58218726 159136 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097951 159136 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
23159839 58853 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 333 7 1 3 4.3 O=C(O)CCc1ccc(OCc2cccc(-c3ccccn3)c2)cc1 10.1021/jm101405t
CHEMBL1688479 58853 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 333 7 1 3 4.3 O=C(O)CCc1ccc(OCc2cccc(-c3ccccn3)c2)cc1 10.1021/jm101405t
23159846 58855 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 339 7 1 4 4.4 O=C(O)CCc1ccc(OCc2cccc(-c3nccs3)c2)cc1 10.1021/jm101405t
CHEMBL1688481 58855 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 339 7 1 4 4.4 O=C(O)CCc1ccc(OCc2cccc(-c3nccs3)c2)cc1 10.1021/jm101405t
57391959 70020 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 362 6 1 2 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939649 70020 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 362 6 1 2 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2011.10.118
137635143 156252 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 7 1 3 6.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4064922 156252 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 7 1 3 6.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)s1 10.1021/acs.jmedchem.6b01357
145977043 163631 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 491 9 2 5 5.8 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4203929 163631 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 491 9 2 5 5.8 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc(Cl)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
145979329 166724 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 7 1 6 2.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(S(C)(=O)=O)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4283015 166724 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 430 7 1 6 2.9 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(S(C)(=O)=O)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145976136 163793 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4205991 163793 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54757622 65333 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)nc(Cl)n1 10.1021/jm2005699
CHEMBL1829153 65333 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)nc(Cl)n1 10.1021/jm2005699
145990303 167023 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3cccc(-c4ccccc4)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4288513 167023 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3cccc(-c4ccccc4)c3)ccc21 10.1016/j.ejmech.2018.09.071
131986113 164823 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218709 164823 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23111668 74044 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022243 74044 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
23111682 74100 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022576 74100 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23111734 74101 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022577 74101 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
145953365 162459 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166892 162459 0 None 1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40Agonist activity at rat GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
155549083 173666 0 None -6 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4534836 173666 0 None -6 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
118645789 180055 0 None -11 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
CHEMBL4747793 180055 0 None -11 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 478 12 1 5 6.2 CCCCc1nc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)cnc1-c1cc(OC)ccc1F 10.1016/j.bmcl.2018.01.013
1050 1900 94 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm300215x
11595431 1900 94 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm300215x
CHEMBL207881 1900 94 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm300215x
131842087 164845 29 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 416 7 1 4 4.4 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4218946 164845 29 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 416 7 1 4 4.4 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2017.07.001
1050 1900 94 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
11595431 1900 94 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
CHEMBL207881 1900 94 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
145947987 167732 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4228673 167732 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4302779 167732 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.04.019
134136960 154465 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 543 11 1 5 6.3 COc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3893207 154465 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 543 11 1 5 6.3 COc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990279 154465 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 543 11 1 5 6.3 COc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
90151023 158214 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 538 8 1 7 5.1 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(F)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4088102 158214 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 538 8 1 7 5.1 CCOc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(F)cn1 10.1021/acs.jmedchem.7b00982
145993644 167327 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 8 1 5 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(C)C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294274 167327 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 8 1 5 4.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(C)C)cc3O2)cc1 10.1016/j.bmc.2018.10.019
132578495 182884 2 None -13 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182884 2 None -13 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
71612897 89981 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381294 89981 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
54580626 62164 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777874 62164 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
75202601 158382 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 482 7 1 5 4.7 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4089881 158382 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 482 7 1 5 4.7 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
145988554 167257 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 412 5 1 3 5.3 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4292911 167257 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 412 5 1 3 5.3 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.ejmech.2018.08.075
145987167 167210 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 4 1 2 5.3 Cc1cc(C)c(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4291858 167210 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 4 1 2 5.3 Cc1cc(C)c(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2018.08.075
145975628 163773 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 382 7 1 4 3.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4205774 163773 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 382 7 1 4 3.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
11316164 76787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 422 7 2 5 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(OCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206881 76787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 422 7 2 5 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(OCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
1049 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
4618 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
5280934 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
CHEMBL8739 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
DB00132 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm300215x
145974295 163023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 518 9 1 6 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(OC)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4175826 163023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 518 9 1 6 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(OC)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
57414678 75624 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
CHEMBL2047165 75624 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
131986132 163857 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206640 163857 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
45107318 119128 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1021/ml500391n
CHEMBL3427709 119128 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1021/ml500391n
45107318 119128 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427709 119128 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.6 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C)cccc32)cc1 10.1016/j.bmc.2015.07.028
121294254 180128 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 585 13 1 6 6.7 COc1ccc(C(=O)N(CC(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4748739 180128 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 585 13 1 6 6.7 COc1ccc(C(=O)N(CC(C)C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
12002201 75833 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048627 75833 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
23111689 74058 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022257 74058 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
90372365 142140 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883504 142140 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.09.010
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2016.03.014
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2015.10.011
155552554 174058 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 512 8 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4544058 174058 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 512 8 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC(F)(F)F)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
57414268 75610 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047150 75610 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57414538 75616 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047156 75616 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
137646830 158005 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4085420 158005 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.6b01559
58172957 111658 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3286417 111658 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
145986046 165910 0 None -19 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 437 10 1 6 4.3 CO[C@H]1C[C@H](Oc2ccc([N+](=O)[O-])c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4250196 165910 0 None -19 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 437 10 1 6 4.3 CO[C@H]1C[C@H](Oc2ccc([N+](=O)[O-])c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
44634024 65339 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2)cc1 10.1021/jm2005699
CHEMBL1829159 65339 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2)cc1 10.1021/jm2005699
134139171 146261 0 None -104 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 6 1 3 5.4 Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3920591 146261 0 None -104 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 350 6 1 3 5.4 Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 10.1016/j.bmcl.2016.10.054
134130787 142264 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884916 142264 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
71257551 150591 24 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3955132 150591 24 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
91801188 169573 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4435837 169573 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2F)c1 10.1016/j.bmcl.2019.04.050
155565379 175564 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4579146 175564 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
134465794 171076 0 None -4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 171076 0 None -4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
118637996 142168 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883819 142168 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4162778 142168 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.8b00149
118637996 142168 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883819 142168 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL4162778 142168 0 None -15 2 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
59590781 111250 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265147 111250 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
90644286 111951 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288344 111951 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
57706778 80795 29 None -8 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL2152070 80795 29 None -8 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
67087173 182458 0 None -8 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 182458 0 None -8 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
24897670 111802 23 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
CHEMBL3287574 111802 23 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
45107312 119131 5 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427712 119131 5 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
45107312 119131 5 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427712 119131 5 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1016/j.bmc.2015.07.028
90644290 111955 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288348 111955 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
15602772 111801 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
CHEMBL3287573 111801 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
45107282 119122 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
CHEMBL3427703 119122 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
45107282 119122 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427703 119122 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
118144982 170350 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4447353 170350 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
51350139 58848 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
CHEMBL1688474 58848 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
51350140 58849 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
CHEMBL1688475 58849 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ccc1CCC(=O)O 10.1021/jm101405t
51350405 58859 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 8 1 2 6.1 CC(C)c1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688485 58859 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 8 1 2 6.1 CC(C)c1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
23111734 74101 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2022577 74101 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
131986035 164055 0 None -5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209136 164055 0 None -5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
122185435 122672 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 3 4.0 CCOC(CC(=O)O)c1ccc(OCc2cccc(F)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604040 122672 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 3 4.0 CCOC(CC(=O)O)c1ccc(OCc2cccc(F)c2)cc1 10.1016/j.bmc.2015.07.028
51350138 58847 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL1688473 58847 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
131986057 163653 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204345 163653 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118638001 142118 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883355 142118 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
71613312 89993 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381306 89993 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
71613521 89977 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381290 89977 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
51349860 58826 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm101405t
CHEMBL1688453 58826 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm101405t
51349990 58851 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 9 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCc3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688477 58851 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 9 1 3 4.9 O=C(O)CCc1ccc(OCc2cccc(OCc3ccccc3)c2)cc1 10.1021/jm101405t
86803193 122457 5 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.6 Cc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601001 122457 5 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 338 7 1 5 3.6 Cc1ccc(-c2noc(COc3ccc(CCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2015.06.018
155569570 176199 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)c(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4593742 176199 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)c(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
75511316 122507 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 388 8 1 6 4.0 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601055 122507 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 388 8 1 6 4.0 COc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
1049 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
4618 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
5280934 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
CHEMBL8739 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
DB00132 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
85472225 162759 0 None -64 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 by calcium flux assayAgonist activity at human GPR40 by calcium flux assay
ChEMBL 495 7 1 4 6.5 O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 10.1021/acsmedchemlett.7b00233
CHEMBL4171724 162759 0 None -64 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 by calcium flux assayAgonist activity at human GPR40 by calcium flux assay
ChEMBL 495 7 1 4 6.5 O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 10.1021/acsmedchemlett.7b00233
67085353 159233 0 None -9 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4098892 159233 0 None -9 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
145947309 167675 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 491 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4241974 167675 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 491 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4302072 167675 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 491 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
145965968 164244 0 None 4 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4211335 164244 0 None 4 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1 10.1016/j.bmcl.2017.12.022
86803219 122511 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 426 7 1 5 5.0 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601059 122511 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 426 7 1 5 5.0 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)c(Cl)c1 10.1016/j.bmcl.2015.06.018
24860552 143286 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 312 8 1 2 4.7 CC[C@H](C)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm2005699
CHEMBL389699 143286 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 312 8 1 2 4.7 CC[C@H](C)COc1ccc(C(CC(=O)O)c2ccccc2)cc1 10.1021/jm2005699
11750823 76831 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206942 76831 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
145980573 166589 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 384 8 1 4 4.8 CC(C)(C)c1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
CHEMBL4280212 166589 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 384 8 1 4 4.8 CC(C)(C)c1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
118642391 162960 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)n1 10.1021/acsmedchemlett.8b00149
CHEMBL4174833 162960 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 429 7 1 4 5.8 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)n1 10.1021/acsmedchemlett.8b00149
53248847 62145 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 62145 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
90151464 155934 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 519 7 1 6 5.6 COc1cc(C)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(C)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4061053 155934 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 519 7 1 6 5.6 COc1cc(C)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c(C)c1 10.1021/acs.jmedchem.7b00982
145986662 167171 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1cncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4291179 167171 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1cncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
12830931 202442 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL611065 202442 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
145984906 166390 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)CC1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4276781 166390 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 362 8 1 4 4.1 O=C(O)CC1COc2cc(OCCCOc3cccc(Cl)c3)ccc21 10.1016/j.ejmech.2018.09.071
145955179 162408 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 490 8 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)o2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166005 162408 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 490 8 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)o2)cc1 10.1016/j.ejmech.2018.04.023
71562422 86539 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)cc1 10.1021/jm301470a
CHEMBL2315540 86539 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1ccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)cc1 10.1021/jm301470a
145974478 164685 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 451 8 2 6 4.4 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(C(F)(F)F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4217082 164685 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 451 8 2 6 4.4 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(C(F)(F)F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
58172986 119124 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1021/ml500391n
CHEMBL3427705 119124 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1021/ml500391n
58172986 119124 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427705 119124 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
54586486 62160 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777870 62160 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
57413375 77217 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2048620 77217 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2079468 77217 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
145950347 162836 0 None -1 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172828 162836 0 None -1 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
118645541 180641 0 None -4 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4754974 180641 0 None -4 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.12.030
51349861 58827 0 None 77 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm101405t
CHEMBL1688454 58827 0 None 77 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm101405t
57706502 164313 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4212284 164313 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
67085353 159233 0 None 9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4098892 159233 0 None 9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 435 7 1 4 6.0 COc1ccc(F)c(-c2cccc(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
87265393 159279 0 None 4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4099410 159279 0 None 4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 433 5 1 3 5.7 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
90644291 111956 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288349 111956 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
58172988 122667 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 413 9 1 5 5.0 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c([N+](=O)[O-])c1 10.1016/j.bmc.2015.07.028
CHEMBL3604036 122667 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 413 9 1 5 5.0 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c([N+](=O)[O-])c1 10.1016/j.bmc.2015.07.028
90372458 142222 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884347 142222 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
54757739 65347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 325 5 1 2 3.9 C=CCc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
CHEMBL1829167 65347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 325 5 1 2 3.9 C=CCc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl 10.1021/jm2005699
24825481 75923 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL205090 75923 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
1049 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
4618 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
5280934 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
CHEMBL8739 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
DB00132 363 75 None 1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/acs.jmedchem.5b01962
12830934 202396 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3cccc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL610787 202396 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3cccc(Cl)c3)cc2)S1 10.1016/j.bmcl.2009.10.052
134133675 143260 0 None -22 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 318 8 1 3 4.1 CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3896714 143260 0 None -22 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 318 8 1 3 4.1 CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 10.1016/j.bmcl.2016.10.054
51350137 58846 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688472 58846 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 374 7 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cc2)c1 10.1021/jm101405t
25150014 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
3952 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
CHEMBL449588 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
90644288 111953 0 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL3288346 111953 0 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1021/acs.jmedchem.6b01357
11489259 75827 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048621 75827 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
162674654 183453 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 183453 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
131986082 164152 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210243 164152 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986378 164579 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4215544 164579 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118645685 179866 0 None -15 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4745513 179866 0 None -15 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 492 10 1 5 6.4 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1 10.1016/j.bmcl.2018.01.013
25150014 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
3952 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
CHEMBL449588 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm8010178
127046960 139989 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL3799946 139989 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4227915 139989 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.07.050
51351414 58842 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 358 7 1 1 5.8 Cc1cccc(C)c1-c1cccc(CCc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688468 58842 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 358 7 1 1 5.8 Cc1cccc(C)c1-c1cccc(CCc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
90161101 158784 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4094183 158784 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
90644300 111965 0 None -31 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288358 111965 0 None -31 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
1622278 95002 10 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 95002 10 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
22036572 165298 73 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 242 5 1 2 3.5 O=C(O)CCc1ccc(Oc2ccccc2)cc1 10.1021/jm101405t
CHEMBL423319 165298 73 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 242 5 1 2 3.5 O=C(O)CCc1ccc(Oc2ccccc2)cc1 10.1021/jm101405t
57397248 70009 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 314 8 1 3 4.2 CCC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939638 70009 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 314 8 1 3 4.2 CCC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
122185442 122683 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 5 2.9 CCOC(CC(=O)O)c1ccc(OCc2cc(C)nn2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604051 122683 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 318 8 1 5 2.9 CCOC(CC(=O)O)c1ccc(OCc2cc(C)nn2C)cc1 10.1016/j.bmc.2015.07.028
58218581 159122 0 None -8 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097826 159122 0 None -8 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
137640417 157099 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCn2cc(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4074547 157099 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCn2cc(CCC(=O)O)nn2)c1 10.1021/acs.jmedchem.6b01357
44409697 76719 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 365 8 2 4 5.3 O=C(O)CSc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL206572 76719 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 365 8 2 4 5.3 O=C(O)CSc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
168283014 190874 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 393 7 1 5 4.7 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ncoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5184830 190874 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 393 7 1 5 4.7 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ncoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
155527626 171229 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459709 171229 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
145966219 164295 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1cccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
CHEMBL4212106 164295 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 397 8 2 6 3.7 Cc1cccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.ejmech.2017.09.019
118638009 167651 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4160527 167651 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301726 167651 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
145948007 167736 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 334 9 1 3 4.2 O=C(O)CCc1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4284549 167736 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 334 9 1 3 4.2 O=C(O)CCc1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4302817 167736 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 334 9 1 3 4.2 O=C(O)CCc1ccc(OCCCOc2cccc(Cl)c2)cc1 10.1016/j.ejmech.2018.09.071
23111668 74044 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022243 74044 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
23111766 74059 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022258 74059 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
131986113 164823 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218709 164823 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 590 7 1 5 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(I)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
66562385 90366 0 None 47 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386361 90366 0 None 47 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 282 3 1 1 3.6 Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
127046962 139934 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(F)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799639 139934 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 387 7 1 4 4.8 Cc1noc(C)c1-c1cc(F)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
24857286 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
6484 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
CHEMBL1829174 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
DB12491 1622 72 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2017.10.040
118737973 119133 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
CHEMBL3427714 119133 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 394 7 1 3 5.3 CCO[C@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1 10.1021/ml500391n
58218651 158317 0 None -4 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4089171 158317 0 None -4 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145965467 164164 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4210415 164164 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54583097 61798 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 270 6 1 2 3.8 CC(Oc1ccc(CCC(=O)O)cc1)c1ccccc1 10.1021/ml100106c
CHEMBL1773249 61798 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 270 6 1 2 3.8 CC(Oc1ccc(CCC(=O)O)cc1)c1ccccc1 10.1021/ml100106c
118145140 175383 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4575265 175383 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cc3c(cn2)[C@H](Oc2cccc([C@H](C4CC4)[C@H](C)C(=O)O)c2)CC3)c1 10.1016/j.bmcl.2019.04.050
46231545 201068 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1C 10.1016/j.bmcl.2009.10.052
CHEMBL602731 201068 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1C 10.1016/j.bmcl.2009.10.052
85470884 164002 2 None -36 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40Agonist activity at human GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
CHEMBL4208325 164002 2 None -36 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40Agonist activity at human GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
137630696 161098 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 612 12 1 6 6.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(C(F)(F)F)cn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4064196 161098 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 612 12 1 6 6.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(C(F)(F)F)cn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116961 161098 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 612 12 1 6 6.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccc(C(F)(F)F)cn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
134156096 151445 0 None -100 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 400 8 1 3 6.2 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3961950 151445 0 None -100 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 400 8 1 3 6.2 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 10.1016/j.bmcl.2016.10.054
71562526 86548 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2ccccc2C(F)(F)F)cc1 10.1021/jm301470a
CHEMBL2315549 86548 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2ccccc2C(F)(F)F)cc1 10.1021/jm301470a
23136363 58831 0 None 14 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm101405t
CHEMBL1688458 58831 0 None 14 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm101405t
146314300 181438 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 493 11 1 4 6.9 COc1ccc(CCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4764150 181438 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 493 11 1 4 6.9 COc1ccc(CCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
155526793 171192 0 None -2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4459220 171192 0 None -2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 462 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)C(F)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
71613516 89972 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381285 89972 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 346 3 1 4 3.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Cl)c1)O3 10.1016/j.bmcl.2013.03.060
46941175 61810 26 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61810 26 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
51350138 58847 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL1688473 58847 0 None 660 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
127031412 138725 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 407 7 1 5 4.6 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
CHEMBL3780042 138725 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 407 7 1 5 4.6 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
168283114 191058 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 436 10 1 4 5.6 Cc1ccc(OCC2CC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5187322 191058 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 436 10 1 4 5.6 Cc1ccc(OCC2CC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
58218630 159653 0 None 13 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103729 159653 0 None 13 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
145978975 166561 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4279744 166561 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
58218571 157478 0 None -17 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079421 157478 0 None -17 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
25261464 80796 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152071 80796 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
145992078 167004 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 406 8 1 4 4.2 O=C(O)CC1COc2cc(OCCCOc3cccc(Br)c3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4288124 167004 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 406 8 1 4 4.2 O=C(O)CC1COc2cc(OCCCOc3cccc(Br)c3)ccc21 10.1016/j.ejmech.2018.09.071
71562315 86535 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 O=C(O)CC1CCc2cc(C#Cc3ccccc3)ccc21 10.1021/jm301470a
CHEMBL2315536 86535 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 O=C(O)CC1CCc2cc(C#Cc3ccccc3)ccc21 10.1021/jm301470a
145983824 165737 0 None 6 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 484 13 1 4 6.3 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4246334 165737 0 None 6 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 484 13 1 4 6.3 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
118642379 142117 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 142117 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
53248847 62145 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 62145 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
23082739 58850 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 396 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2cc(F)c(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
CHEMBL1688476 58850 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 396 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2cc(F)c(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
90644303 111970 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3288363 111970 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmc.2015.07.028
122185440 122681 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 306 8 1 3 4.2 CCOC(CC(=O)O)c1ccc(OCC2CCCCC2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604049 122681 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 306 8 1 3 4.2 CCOC(CC(=O)O)c1ccc(OCC2CCCCC2)cc1 10.1016/j.bmc.2015.07.028
90644303 111970 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288363 111970 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
137333449 167607 5 None -10 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165147 167607 5 None -10 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301092 167607 5 None -10 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc([C@@H]3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
90372616 142231 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
71562773 86531 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 301 3 1 2 3.3 N#CCc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
CHEMBL2315532 86531 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 301 3 1 2 3.3 N#CCc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1021/jm301470a
66562286 90364 0 None 223 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
CHEMBL2386359 90364 0 None 223 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F 10.1021/ml4000673
71615667 89999 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 420 4 1 4 5.3 Cc1cc(F)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381312 89999 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 420 4 1 4 5.3 Cc1cc(F)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
19705952 58863 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 270 7 1 2 3.3 O=C(O)CCc1ccc(OCCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688489 58863 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 270 7 1 2 3.3 O=C(O)CCc1ccc(OCCc2ccccc2)cc1 10.1021/jm101405t
23082789 58864 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 284 8 1 2 3.7 O=C(O)CCc1ccc(OCCCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688490 58864 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 284 8 1 2 3.7 O=C(O)CCc1ccc(OCCCc2ccccc2)cc1 10.1021/jm101405t
145982616 165744 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 470 12 1 4 5.9 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4246529 165744 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 470 12 1 4 5.9 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
58218699 159414 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4100898 159414 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
85470884 164002 2 None -38 5 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
CHEMBL4208325 164002 2 None -38 5 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 459 7 1 3 6.0 O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2018.02.013
25150011 186687 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 4 1 2 2.9 O=Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL488395 186687 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 4 1 2 2.9 O=Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
44409729 140208 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.0 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CC(C)C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL380504 140208 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.0 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CC(C)C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
57521915 76270 0 None -15 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 378 8 1 3 5.7 CSc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058528 76270 0 None -15 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 378 8 1 3 5.7 CSc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
155544661 174943 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
CHEMBL4565467 174943 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1 10.1016/j.bmcl.2019.04.050
127027659 137668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3cccc(Br)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758549 137668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 391 5 1 4 3.9 O=C1NC(=O)C(Cc2ccc(OCc3cccc(Br)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
134157586 154161 0 None -123 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 366 8 1 3 5.5 O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3985509 154161 0 None -123 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 366 8 1 3 5.5 O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
145989198 167244 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
CHEMBL4292598 167244 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1cccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
122185453 122700 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 397 7 1 5 4.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
CHEMBL3604068 122700 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 397 7 1 5 4.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2COc3c2cccc3C(F)(F)F)nc1 10.1016/j.bmc.2015.07.028
118638009 167651 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4160527 167651 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301726 167651 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 479 7 1 4 6.3 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
118623088 142125 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 142125 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
155549085 173667 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 425 10 3 5 4.2 Cc1cc(OCCO)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4534840 173667 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 425 10 3 5 4.2 Cc1cc(OCCO)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
145964042 164081 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 4.8 Cc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4209491 164081 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 430 7 1 4 4.8 Cc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
44409933 75982 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 418 6 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205434 75982 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 418 6 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
71612685 89978 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 352 4 1 4 4.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(C2CC2)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381291 89978 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 352 4 1 4 4.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(C2CC2)c1)O3 10.1016/j.bmcl.2013.03.060
155535186 172006 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 369 7 2 3 4.7 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3F)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4471403 172006 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 369 7 2 3 4.7 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3F)c2)cc1F 10.1016/j.ejmech.2019.06.087
168276253 190451 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
CHEMBL5178528 190451 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1ccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.bmc.2022.116615
67058186 119123 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
CHEMBL3427704 119123 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
57394144 69849 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 356 6 1 2 5.7 CC#CC(CC(=O)O)c1ccc(Oc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1938409 69849 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 356 6 1 2 5.7 CC#CC(CC(=O)O)c1ccc(Oc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
67058186 119123 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427704 119123 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCO[C@H](CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
58218581 159122 0 None 8 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097826 159122 0 None 8 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 5 1 3 5.2 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
90151400 156133 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4063492 156133 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
90151222 156903 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 6 1 5 5.9 Cc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4072229 156903 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 6 1 5 5.9 Cc1ccc(Cl)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
132578495 182884 2 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182884 2 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
23136477 58828 3 None -15 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688455 58828 3 None -15 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm101405t
CHEMBL4213909 58828 3 None -15 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 10.1021/jm101405t
853224 94573 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94573 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
134154473 152372 0 None -218 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 370 6 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
CHEMBL3970238 152372 0 None -218 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 370 6 1 3 5.0 O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 10.1021/acsmedchemlett.6b00394
1051 1454 63 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
4289 1454 63 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
445580 1454 63 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
57417355 1454 63 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
CHEMBL367149 1454 63 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
DB03756 1454 63 None -14 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 10.1021/ml300133f
90151309 155942 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)cc1F 10.1021/acs.jmedchem.7b00982
CHEMBL4061146 155942 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1ccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)cc1F 10.1021/acs.jmedchem.7b00982
145979602 166510 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 466 11 1 6 3.4 CS(=O)(=O)CCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
CHEMBL4278799 166510 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 466 11 1 6 3.4 CS(=O)(=O)CCCOc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CC2 10.1016/j.bmc.2018.10.019
145977668 163877 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1C 10.1016/j.ejmech.2017.07.001
CHEMBL4206915 163877 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1noc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1C 10.1016/j.ejmech.2017.07.001
73345870 90374 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386369 90374 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
54586982 61797 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 254 6 1 1 3.5 O=C(O)CCc1ccc(CCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773248 61797 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 254 6 1 1 3.5 O=C(O)CCc1ccc(CCc2ccccc2)cc1 10.1021/ml100106c
145974382 164538 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 367 7 2 5 3.4 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccccc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4215054 164538 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 367 7 2 5 3.4 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3ccccc3)s2)cc1 10.1016/j.ejmech.2017.09.019
127051975 140291 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(Cl)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805971 140291 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(Cl)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
131986075 163907 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4207273 163907 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118645367 181660 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4776217 181660 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
24857286 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
6484 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
CHEMBL1829174 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
DB12491 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2019.06.087
66562289 139017 0 None 707 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(\C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3785764 139017 0 None 707 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 246 3 1 1 3.2 C/C=C(\C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
127046960 139989 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL3799946 139989 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
CHEMBL4227915 139989 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 1 hr by Fluo 4-AM dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmcl.2019.04.019
142738567 162540 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4168059 162540 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3)cc2c1 10.1021/acsmedchemlett.7b00460
58380220 111254 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265151 111254 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
57706588 80668 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151298 80668 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
58172957 111658 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3286417 111658 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmc.2015.07.028
58172957 111658 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3286417 111658 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1 10.1016/j.bmcl.2014.04.065
90151283 159481 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 6 1 6 4.8 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)n1 10.1021/acs.jmedchem.7b00982
CHEMBL4101678 159481 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 6 1 6 4.8 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)n1 10.1021/acs.jmedchem.7b00982
54585512 62161 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777871 62161 0 None -1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
73348895 90377 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386371 90377 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
25150018 185430 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1016/j.ejmech.2019.06.087
CHEMBL486145 185430 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1016/j.ejmech.2019.06.087
25150018 185430 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1021/jm8010178
CHEMBL486145 185430 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1ccccc1C#Cc1ccc(OCC(=O)O)cc1 10.1021/jm8010178
145990731 167018 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 328 4 1 2 4.4 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4288438 167018 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 328 4 1 2 4.4 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2018.08.075
137637576 156061 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4062640 156061 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
23083193 58835 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccccc1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688461 58835 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccccc1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
118645756 181460 7 None 1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40 assessed as increase in intracellular calcium levelAgonist activity at mouse GPR40 assessed as increase in intracellular calcium level
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 181460 7 None 1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40 assessed as increase in intracellular calcium levelAgonist activity at mouse GPR40 assessed as increase in intracellular calcium level
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
90644286 111951 0 None -10 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288344 111951 0 None -10 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
71562639 86519 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315252 86519 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
66562392 90370 0 None 83 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 3 1 1 4.6 O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F 10.1021/ml4000673
CHEMBL2386365 90370 0 None 83 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 336 3 1 1 4.6 O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F 10.1021/ml4000673
145947987 167732 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmc.2017.12.030
CHEMBL4228673 167732 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmc.2017.12.030
CHEMBL4302779 167732 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 351 7 1 4 4.6 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmc.2017.12.030
23111781 74048 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
CHEMBL2022247 74048 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
24857286 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
6484 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
CHEMBL1829174 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
DB12491 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2014.11.016
147747458 170579 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 437 10 2 4 6.0 CCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4450552 170579 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 437 10 2 4 6.0 CCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
71615668 90000 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381313 90000 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
127045657 139885 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(Cl)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799341 139885 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1cc(Cl)cc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
57787398 143749 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 448 9 2 7 3.1 Cc1cc(OCCO)ccc1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3900797 143749 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay
ChEMBL 448 9 2 7 3.1 Cc1cc(OCCO)ccc1-c1cccc(COc2ccc(Cn3oc(=O)[nH]c3=O)cc2)c1 10.1016/j.bmcl.2016.10.074
67972848 166640 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 356 4 1 2 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4281238 166640 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 356 4 1 2 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
122185432 122661 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 350 8 1 3 4.4 CCOC(c1ccc(OCc2ccccc2C)cc1)C(F)(F)C(=O)O 10.1016/j.bmc.2015.07.028
CHEMBL3604030 122661 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 350 8 1 3 4.4 CCOC(c1ccc(OCc2ccccc2C)cc1)C(F)(F)C(=O)O 10.1016/j.bmc.2015.07.028
137660172 159111 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 C[C@@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O 10.1021/acs.jmedchem.7b00210
CHEMBL4097652 159111 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 357 5 1 4 4.4 C[C@@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O 10.1021/acs.jmedchem.7b00210
71460255 80794 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
CHEMBL2152069 80794 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
118638010 167563 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167563 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167563 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
90372613 167742 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167742 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167742 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
23136401 159133 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4097919 159133 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
145981599 166453 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 370 7 1 4 4.4 CC(C)(C)c1cccc(OCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
CHEMBL4277858 166453 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 370 7 1 4 4.4 CC(C)(C)c1cccc(OCCOc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.ejmech.2018.09.071
137629794 161180 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4093571 161180 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4117644 161180 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
145993490 167348 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 429 7 1 7 3.3 Cn1nncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294530 167348 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 429 7 1 7 3.3 Cn1nncc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
118144973 175282 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4572891 175282 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
127031569 139182 0 None 26 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 264 4 1 1 3.3 O=C(O)CCc1ccc(C#CCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3787580 139182 0 None 26 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 264 4 1 1 3.3 O=C(O)CCc1ccc(C#CCc2ccccc2)cc1 10.1021/acs.jmedchem.5b01962
118719474 115534 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OC(C)C(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353262 115534 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 512 12 1 6 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OC(C)C(=O)O)cc2)c1 10.1016/j.bmc.2014.11.016
54757623 65334 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 257 3 1 3 2.6 O=C(O)CCc1ccc(C#Cc2cncs2)cc1 10.1021/jm2005699
CHEMBL1829154 65334 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 257 3 1 3 2.6 O=C(O)CCc1ccc(C#Cc2cncs2)cc1 10.1021/jm2005699
57414404 75614 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047154 75614 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
131986130 164423 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213597 164423 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 572 11 1 7 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Cl)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145953365 162459 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166892 162459 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
23111666 74054 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
CHEMBL2022253 74054 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
58230552 182217 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
131986136 163623 0 None -3 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203795 163623 0 None -3 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
24857286 1622 72 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
6484 1622 72 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
CHEMBL1829174 1622 72 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
DB12491 1622 72 None -28 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.8b00444
24857286 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
6484 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
CHEMBL1829174 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
DB12491 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.08.075
71613313 89994 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381307 89994 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
145988414 165212 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL4229006 165212 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
24825485 88026 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 343 6 2 2 5.2 O=C(O)C1CC1c1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234450 88026 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 343 6 2 2 5.2 O=C(O)C1CC1c1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.12.084
71562769 86523 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315256 86523 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
44409665 75589 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 388 9 2 3 5.5 CC(C)NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL204671 75589 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 388 9 2 3 5.5 CC(C)NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
168271642 190311 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 486 11 1 4 6.5 Cc1ccc(OCCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5176157 190311 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 486 11 1 4 6.5 Cc1ccc(OCCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
168288738 191406 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 446 9 1 4 6.1 CCOc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
CHEMBL5192621 191406 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 446 9 1 4 6.1 CCOc1ccc2cc(-c3cccc(COc4ccc(OCC(=O)O)c(F)c4)c3)ccc2c1 10.1016/j.bmc.2022.116615
137653172 158531 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 480 6 1 6 4.5 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccc(F)n4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4091456 158531 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 480 6 1 6 4.5 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccc(F)n4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
145955263 162539 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4168048 162539 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
57706778 80795 29 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL2152070 80795 29 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
57706778 80795 29 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
CHEMBL2152070 80795 29 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2019.04.050
137640728 157030 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 8 1 3 6.6 Cc1cccc(C)c1-c1cccc(COc2ccc(C(CC(=O)O)C3CC3)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4073587 157030 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 406 8 1 3 6.6 Cc1cccc(C)c1-c1cccc(COc2ccc(C(CC(=O)O)C3CC3)s2)c1 10.1021/acs.jmedchem.6b01357
54581633 62159 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777869 62159 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
155530636 171533 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 438 11 2 6 4.3 CO/N=C(\COc1ccc(CNc2ccc(OCC(=O)O)c(F)c2)cc1)c1ccccc1 10.1016/j.ejmech.2019.06.087
CHEMBL4464317 171533 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 438 11 2 6 4.3 CO/N=C(\COc1ccc(CNc2ccc(OCC(=O)O)c(F)c2)cc1)c1ccccc1 10.1016/j.ejmech.2019.06.087
24825480 87987 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1cccc(NCc2cccc(Oc3ccccc3)c2)c1 10.1016/j.bmcl.2006.12.084
CHEMBL234267 87987 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1cccc(NCc2cccc(Oc3ccccc3)c2)c1 10.1016/j.bmcl.2006.12.084
145979123 166464 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 5 1 2 5.5 CC(C)c1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4278085 166464 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 370 5 1 2 5.5 CC(C)c1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
24825483 76878 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 7 2 3 4.7 O=C(O)Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL206972 76878 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 7 2 3 4.7 O=C(O)Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
24825495 88031 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccccc2Cl)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234469 88031 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccccc2Cl)cc1 10.1016/j.bmcl.2006.12.084
24825496 88032 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 269 6 2 2 3.6 Cc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234470 88032 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 269 6 2 2 3.6 Cc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1 10.1016/j.bmcl.2006.12.084
137637576 156061 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4062640 156061 0 None -63 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 298 6 1 2 4.2 Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 10.1016/j.bmcl.2017.01.034
23136401 159133 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
CHEMBL4097919 159133 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 362 8 1 3 5.4 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2017.01.034
168285919 191672 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 534 9 2 5 6.7 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@@H]2Oc1ccc2c(c1)OC[C@@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
CHEMBL5196447 191672 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 534 9 2 5 6.7 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@@H]2Oc1ccc2c(c1)OC[C@@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
134538585 163633 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4203974 163633 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 518 9 3 5 6.3 Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
145976639 163813 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 523 6 2 5 6.2 Cc1cc(-c2cccc(=O)n2C)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4206195 163813 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 523 6 2 5 6.2 Cc1cc(-c2cccc(=O)n2C)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
131986295 163540 0 None 2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202907 163540 0 None 2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986030 164812 0 None 1 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218596 164812 0 None 1 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
134465785 176109 0 None 15 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 176109 0 None 15 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
162673875 182984 0 None -13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182984 0 None -13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182812 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182812 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
90372625 167719 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167719 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167719 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
44409703 141199 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 431 6 2 4 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(N)=O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382831 141199 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 431 6 2 4 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(N)=O)cc1 10.1016/j.bmcl.2006.01.007
57413373 75825 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048618 75825 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
118645526 182978 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4793322 182978 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1 10.1016/j.bmcl.2018.01.013
118144973 175282 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4572891 175282 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
67087100 182596 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182596 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
164616320 185043 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
CHEMBL4855306 185043 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 333 4 2 1 5.2 O=C(O)CCc1ccc2[nH]c(-c3cccc(Cl)c3Cl)cc2c1 10.1021/acs.jmedchem.1c00031
147146439 171283 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 365 7 2 3 4.9 Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4460582 171283 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 365 7 2 3 4.9 Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
44409722 141014 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382381 141014 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)O)cc1 10.1016/j.bmcl.2006.01.007
162674654 183453 0 None -9 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 183453 0 None -9 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
134465730 172801 0 None 1 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4513748 172801 0 None 1 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 440 9 1 3 6.4 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@H](C)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
51349992 58832 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
CHEMBL1688459 58832 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1ccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/jm101405t
146840871 169523 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4434996 169523 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(OC)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
23083189 75817 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
CHEMBL2048610 75817 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
71562638 86518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315251 86518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 294 5 1 2 3.3 COCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
54669771 65350 8 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 319 3 1 2 3.8 O=C(O)CCc1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
CHEMBL1829170 65350 8 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 319 3 1 2 3.8 O=C(O)CCc1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
168285917 191671 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5196445 191671 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1ccc(-c2cccc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
155548030 173677 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4535007 173677 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(Cl)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
75511297 122508 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 7 1 6 4.0 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2cccs2)no1 10.1016/j.bmcl.2015.06.018
CHEMBL3601056 122508 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 344 7 1 6 4.0 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2cccs2)no1 10.1016/j.bmcl.2015.06.018
71461901 80659 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
CHEMBL2151289 80659 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
145946416 167539 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 9 1 4 6.5 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(CCc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4248812 167539 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 9 1 4 6.5 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(CCc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4300233 167539 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 519 9 1 4 6.5 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(CCc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
118642379 142117 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 142117 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
137636033 156174 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4063956 156174 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
46232309 201085 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 351 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)O1 10.1016/j.bmcl.2009.10.052
CHEMBL602868 201085 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 351 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)O1 10.1016/j.bmcl.2009.10.052
141747238 166442 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4277653 166442 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.ejmech.2018.08.075
118637972 162315 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4164618 162315 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 428 7 1 3 6.4 COc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
118638001 142118 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883355 142118 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
57521918 76274 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 380 7 1 2 5.9 Cc1ccc(-c2ccc(Cl)cc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058531 76274 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 380 7 1 2 5.9 Cc1ccc(-c2ccc(Cl)cc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
54757513 65324 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccncc2)cc1 10.1021/jm2005699
CHEMBL1829145 65324 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccncc2)cc1 10.1021/jm2005699
54582630 62156 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 62156 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
46854655 395 47 None -8 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
6485 395 47 None -8 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
CHEMBL1829173 395 47 None -8 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
146695343 171851 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 10 2 4 5.7 CCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4468987 171851 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 423 10 2 4 5.7 CCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
145754982 162460 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 510 10 1 6 4.9 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3C(=O)O)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4166922 162460 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 510 10 1 6 4.9 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3C(=O)O)c1 10.1016/j.ejmech.2017.07.001
24857286 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
6484 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
CHEMBL1829174 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
DB12491 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
155515835 169996 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 439 11 2 5 4.9 COCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4442354 169996 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 439 11 2 5 4.9 COCCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
132578494 154510 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3941821 154510 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990702 154510 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(F)cc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
137643956 158271 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4088797 158271 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
162659927 181380 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 500 12 1 3 8.3 COc1ccc(CCCC(C)(C)C)c(-c2ccc(COc3cccc(C(CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4763356 181380 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 500 12 1 3 8.3 COc1ccc(CCCC(C)(C)C)c(-c2ccc(COc3cccc(C(CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acs.jmedchem.0c00843
127027730 137713 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 443 7 1 6 4.6 O=C1NC(=O)C(Cc2ccc(OCc3nc4ccccc4n3Cc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758919 137713 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 443 7 1 6 4.6 O=C1NC(=O)C(Cc2ccc(OCc3nc4ccccc4n3Cc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
145965797 164383 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 501 9 2 7 4.9 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc4c(c3)OCO4)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4213089 164383 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 501 9 2 7 4.9 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccc4c(c3)OCO4)s2)cc1 10.1016/j.ejmech.2017.09.019
90372365 142140 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883504 142140 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 8 1 4 7.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2OC(F)(F)F)c1 10.1021/acsmedchemlett.6b00443
58319139 86541 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1cccc(C)c1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315542 86541 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 3 1 1 3.7 Cc1cccc(C)c1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
127030715 138996 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.6 C=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3785544 138996 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.6 C=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
24825484 87989 0 None 208 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL234269 87989 0 None 208 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
145959722 162188 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 544 8 1 5 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C(C)(C)C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4162588 162188 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 544 8 1 5 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(C(C)(C)C)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
134135852 144379 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 502 9 1 8 3.6 CCOc1ccc(F)c(N2CC[C@@H](Oc3cnc(N4CC(OC)[C@@H](C)[C@@H]4CC(=O)O)cn3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3905856 144379 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 502 9 1 8 3.6 CCOc1ccc(F)c(N2CC[C@@H](Oc3cnc(N4CC(OC)[C@@H](C)[C@@H]4CC(=O)O)cn3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
54586484 62152 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 62152 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
145950402 162921 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4174136 162921 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 467 8 2 3 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
145953365 162459 0 None -1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166892 162459 0 None -1 3 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
ChEMBL 467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@H]3CCCc4ccccc43)cc2)cc1 10.1016/j.ejmech.2018.04.023
56680363 65352 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 331 2 1 2 4.0 O=C(O)C1CC1c1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
CHEMBL1829172 65352 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 331 2 1 2 4.0 O=C(O)C1CC1c1ccc(C#Cc2cc(Cl)nc(Cl)c2)cc1 10.1021/jm2005699
57706642 80669 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 490 9 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151299 80669 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 490 9 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
90644291 111956 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288349 111956 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nn2)c1 10.1016/j.bmcl.2014.04.065
168287667 191659 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 466 12 1 5 5.8 CCOc1ccc(/C=C/c2cc(OCC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
CHEMBL5196235 191659 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 466 12 1 5 5.8 CCOc1ccc(/C=C/c2cc(OCC)cc(OCc3ccc(OCC(=O)O)c(F)c3)c2)cc1 10.1016/j.ejmech.2021.114061
134142866 145640 0 None -9 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 358 7 1 3 4.6 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3915765 145640 0 None -9 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 358 7 1 3 4.6 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
71562641 86521 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 400 9 1 4 3.3 CS(=O)(=O)CCCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315254 86521 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 400 9 1 4 3.3 CS(=O)(=O)CCCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
145964802 164277 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4211807 164277 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 415 7 1 6 3.7 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
66562391 138987 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 262 4 2 2 2.1 C/C(C#Cc1ccc(CCC(=O)O)c(F)c1)=C/CO 10.1021/acs.jmedchem.5b01962
CHEMBL3785413 138987 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 262 4 2 2 2.1 C/C(C#Cc1ccc(CCC(=O)O)c(F)c1)=C/CO 10.1021/acs.jmedchem.5b01962
145980608 166642 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3ccc(-c4ccccc4)cc3)ccc21 10.1016/j.ejmech.2018.09.071
CHEMBL4281316 166642 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 404 9 1 4 5.2 O=C(O)CC1COc2cc(OCCCOc3ccc(-c4ccccc4)cc3)ccc21 10.1016/j.ejmech.2018.09.071
54757621 65321 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cnc(Cl)nc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
CHEMBL1829142 65321 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 300 3 1 3 2.9 Cc1cnc(Cl)nc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
46231656 201113 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccnc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL603066 201113 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccnc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
134130696 142135 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 142135 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
118638001 142118 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883355 142118 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)nc2)c1 10.1021/acsmedchemlett.6b00443
122193975 123977 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3629049 123977 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
25150120 174002 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL454257 174002 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 264 3 1 1 3.4 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
54757831 65351 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 333 3 1 2 4.1 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)cc(Cl)nc1Cl 10.1021/jm2005699
CHEMBL1829171 65351 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 333 3 1 2 4.1 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)cc(Cl)nc1Cl 10.1021/jm2005699
58218673 157523 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079930 157523 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
853224 94573 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94573 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
127050771 140227 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805246 140227 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 397 8 2 6 3.7 Cc1ccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
145979252 166646 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 442 7 1 4 5.3 O=C(O)CC(c1ccc(F)cc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4281376 166646 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 442 7 1 4 5.3 O=C(O)CC(c1ccc(F)cc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
145962164 161475 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 367 6 1 6 3.0 O=C1NC(=O)C(Cc2ccc(OCCn3cnc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4127761 161475 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 367 6 1 6 3.0 O=C1NC(=O)C(Cc2ccc(OCCn3cnc4ccccc43)cc2)S1 10.1016/j.bmcl.2018.03.051
53248846 62151 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 62151 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
46941175 61810 26 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61810 26 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
162659599 181196 0 None -4 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4761101 181196 0 None -4 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
90151205 157284 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4076882 157284 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
162666840 182452 0 None -3 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 182452 0 None -3 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
137638184 156754 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070619 156754 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 365 6 1 3 4.6 O=C(O)C[C@@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
134129938 142438 0 None -263 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 414 6 1 4 5.0 COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F 10.1021/acsmedchemlett.6b00394
CHEMBL3890089 142438 0 None -263 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
ChEMBL 414 6 1 4 5.0 COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F 10.1021/acsmedchemlett.6b00394
58319127 86550 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm301470a
CHEMBL2315551 86550 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm301470a
54580132 61802 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/ml100106c
CHEMBL1773253 61802 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/ml100106c
57521913 76268 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 9 1 3 5.3 CCOc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058526 76268 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 9 1 3 5.3 CCOc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
142738545 162274 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 279 4 2 1 4.2 Cc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
CHEMBL4164008 162274 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 279 4 2 1 4.2 Cc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acsmedchemlett.7b00460
46231713 201034 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc1 10.1016/j.bmcl.2009.10.052
CHEMBL602457 201034 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 314 4 1 5 3.1 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc1 10.1016/j.bmcl.2009.10.052
51349993 58834 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1cccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
CHEMBL1688460 58834 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.4 Cc1cccc(Oc2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1 10.1021/jm101405t
24857286 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
6484 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
CHEMBL1829174 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
DB12491 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.09.071
24857286 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
6484 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
CHEMBL1829174 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
DB12491 1622 72 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2021.114061
155550483 174301 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 501 12 2 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4550165 174301 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 501 12 2 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
127046960 139989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2017.12.030
CHEMBL3799946 139989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2017.12.030
CHEMBL4227915 139989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 369 7 1 4 4.7 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2017.12.030
25150014 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm2005699
3952 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm2005699
CHEMBL449588 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm2005699
25150014 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/ml4000673
3952 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/ml4000673
CHEMBL449588 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/ml4000673
60195125 3886 8 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3886 8 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3886 8 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
145963855 164197 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 476 9 1 3 7.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4210827 164197 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 476 9 1 3 7.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
168285924 191673 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 392 7 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5196452 191673 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 392 7 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccoc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
137639817 156802 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 504 10 1 5 6.6 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCC4(C)COC4)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4071066 156802 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 504 10 1 5 6.6 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCC4(C)COC4)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
137653896 158543 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
CHEMBL4091552 158543 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
90151652 158672 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 507 7 1 5 5.7 CCc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4092937 158672 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 507 7 1 5 5.7 CCc1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
90151514 159659 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4103854 159659 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccccc4Cl)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
58218630 159653 0 None -13 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103729 159653 0 None -13 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
137637243 155887 0 None -4 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 343 5 1 4 4.1 O=C(O)CCc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
CHEMBL4060517 155887 0 None -4 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 343 5 1 4 4.1 O=C(O)CCc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1 10.1021/acs.jmedchem.7b00210
134143394 154478 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 545 11 1 7 5.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3nc(C5CC5)no3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3917858 154478 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 545 11 1 7 5.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3nc(C5CC5)no3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990389 154478 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 545 11 1 7 5.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3nc(C5CC5)no3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
53248846 62151 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 62151 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
54580132 61802 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/jm300215x
CHEMBL1773253 61802 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 10.1021/jm300215x
145966167 164221 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 407 7 1 5 3.7 N#Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4211064 164221 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 407 7 1 5 3.7 N#Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
561372 58825 65 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1688452 58825 65 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
75511317 122509 4 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.3 Cc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
CHEMBL3601057 122509 4 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.3 Cc1cccc(-c2noc(COc3ccc(CCC(=O)O)cc3Cl)n2)c1 10.1016/j.bmcl.2015.06.018
145955263 162539 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4168048 162539 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 414 6 2 3 6.1 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(O)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
145990715 166995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4288001 166995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
25150014 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm301470a
3952 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm301470a
CHEMBL449588 3883 55 None 44 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/jm301470a
162668241 182504 0 None -4 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4787007 182504 0 None -4 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
71612898 89982 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381295 89982 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
71562771 86529 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315530 86529 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 305 5 1 3 3.0 N#CCOc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
145974495 164723 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 396 7 1 4 4.1 Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4217477 164723 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 396 7 1 4 4.1 Cc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
127032539 138808 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
CHEMBL3781077 138808 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2016.03.014
155522452 170712 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
CHEMBL4452044 170712 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F 10.1016/j.bmcl.2019.01.014
137657002 159800 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 3 3.7 Cc1ccccc1C(=O)c1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4105565 159800 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 3 3.7 Cc1ccccc1C(=O)c1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
90372625 167719 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167719 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167719 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
5280933 178218 64 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O 10.1016/j.ejmech.2015.12.049
CHEMBL464982 178218 64 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O 10.1016/j.ejmech.2015.12.049
71562768 86522 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315255 86522 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 289 3 1 2 3.3 Cc1ccc(C#N)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
127050769 140266 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 413 9 2 7 3.4 COc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
CHEMBL3805670 140266 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 413 9 2 7 3.4 COc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1 10.1016/j.bmc.2016.04.065
23083190 58836 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 8 1 3 5.7 Cc1cccc(C)c1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688462 58836 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 376 8 1 3 5.7 Cc1cccc(C)c1Oc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
156013404 177457 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmcl.2021.127969
CHEMBL4638956 177457 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmcl.2021.127969
131986378 164579 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4215544 164579 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 552 11 1 7 6.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145950347 162836 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172828 162836 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
54586486 62160 0 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777870 62160 0 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayAgonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm8010178
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayAgonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm8010178
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayAgonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm8010178
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm2005699
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm2005699
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm2005699
127031003 139142 0 None 371 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C\C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3787072 139142 0 None 371 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C/C=C\C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
3681700 200312 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2cccc(Oc3ccccc3)c2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL597424 200312 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 299 4 1 4 3.4 O=C1NC(=O)C(Cc2cccc(Oc3ccccc3)c2)S1 10.1016/j.bmcl.2009.10.052
9995943 200535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2011.03.114
CHEMBL598935 200535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2011.03.114
86803183 122455 1 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(Cl)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600999 122455 1 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(Cl)c3)o2)cc1 10.1016/j.bmcl.2015.06.018
54757733 65341 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 343 5 1 3 4.3 O=C(O)CCc1ccc(C#Cc2ccnc(Oc3ccccc3)c2)cc1 10.1021/jm2005699
CHEMBL1829161 65341 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 343 5 1 3 4.3 O=C(O)CCc1ccc(C#Cc2ccnc(Oc3ccccc3)c2)cc1 10.1021/jm2005699
54582150 61808 0 None 22 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL1773259 61808 0 None 22 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 10.1021/jm300215x
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2018.06.047
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2018.06.047
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2018.06.047
11271473 74470 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022584 74470 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2027975 74470 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
54586484 62152 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 62152 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
118645671 180927 0 None -5 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4758060 180927 0 None -5 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
127034370 138839 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3781477 138839 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
44409664 77288 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 360 8 2 3 4.8 CNC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL208175 77288 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 360 8 2 3 4.8 CNC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
71460255 80794 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
CHEMBL2152069 80794 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/ml300133f
168276826 190122 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5173326 190122 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 396 9 1 4 4.9 CCOc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
168278602 190984 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.5 O=C(O)COc1ccc(OCc2cccc(-c3ccc4cc(OCC5CC5)ccc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5186275 190984 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.5 O=C(O)COc1ccc(OCc2cccc(-c3ccc4cc(OCC5CC5)ccc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
9995943 200535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598935 200535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.bmcl.2009.10.052
90151529 157766 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 497 6 1 5 5.2 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4082717 157766 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 497 6 1 5 5.2 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(F)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
1052 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
3323 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
5280450 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
CHEMBL267476 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
DB14104 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2019.01.014
1052 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
3323 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
5280450 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
CHEMBL267476 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
DB14104 2319 85 None -5 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmc.2018.10.019
127030344 139143 0 None 69 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.2 O=C(O)CCc1ccc(C#CC2CCCC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3787110 139143 0 None 69 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.2 O=C(O)CCc1ccc(C#CC2CCCC2)cc1 10.1021/acs.jmedchem.5b01962
51350270 58837 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
CHEMBL1688463 58837 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1 10.1021/ml100106c
11327107 74049 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
CHEMBL2022248 74049 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
122185444 122686 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 7 1 3 5.3 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604054 122686 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 354 7 1 3 5.3 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
58172989 111967 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288360 111967 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1 10.1016/j.bmcl.2014.04.065
122193735 123966 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628755 123966 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
168293256 192137 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 464 10 1 4 6.4 Cc1ccc(OCC2CCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5203672 192137 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 464 10 1 4 6.4 Cc1ccc(OCC2CCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
137631853 156310 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4065518 156310 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
132606864 157744 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157744 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
23111708 74047 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/jm2012968
CHEMBL2022246 74047 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1 10.1021/jm2012968
118145020 171067 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4457184 171067 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
127046666 140003 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cncc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3800040 140003 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cncc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
45107311 119130 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1021/ml500391n
CHEMBL3427711 119130 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1021/ml500391n
45107311 119130 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427711 119130 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 360 7 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(Cl)cccc32)cc1 10.1016/j.bmc.2015.07.028
68194449 182812 0 None -4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182812 0 None -4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
90356885 167533 0 None 16 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4168422 167533 0 None 16 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300181 167533 0 None 16 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
90372616 142231 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
45107476 118992 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1021/ml500391n
CHEMBL3425533 118992 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1021/ml500391n
45107476 118992 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3425533 118992 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
73051869 167437 4 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 521 10 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2cc3c(cn2)[C@@H]2[C@@H](C(=O)O)[C@@H]2C3)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4297471 167437 4 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 521 10 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2cc3c(cn2)[C@@H]2[C@@H](C(=O)O)[C@@H]2C3)c1 10.1021/acs.jmedchem.1c00031
51350138 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
CHEMBL1688473 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm101405t
51350138 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
CHEMBL1688473 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
51350138 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL1688473 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
6483 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
66553168 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL2386353 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
90372613 167742 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167742 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167742 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.1c00031
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.1c00031
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.1c00031
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00460
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00460
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00460
137653903 158565 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4091723 158565 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCO[C@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
145952673 162434 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 443 7 1 4 4.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)o2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4166397 162434 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 443 7 1 4 4.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)o2)cc1 10.1016/j.ejmech.2018.04.023
145990715 166995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4288001 166995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
24825479 147265 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 359 7 2 3 5.3 O=C(O)C1CC1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL392869 147265 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 359 7 2 3 5.3 O=C(O)C1CC1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.12.084
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2020.127650
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2020.127650
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assayAgonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2020.127650
51350272 58839 0 None 107 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58839 0 None 107 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
86817649 122458 2 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.5 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccc(Cl)cc2)no1 10.1016/j.bmcl.2015.06.018
CHEMBL3601002 122458 2 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 372 7 1 5 4.5 CC(Oc1ccc(CCC(=O)O)cc1)c1nc(-c2ccc(Cl)cc2)no1 10.1016/j.bmcl.2015.06.018
137636358 155884 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4060499 155884 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
90151428 158049 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 475 6 1 5 5.3 Cc1ccccc1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4085928 158049 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 475 6 1 5 5.3 Cc1ccccc1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
58218709 158416 0 None -4 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
CHEMBL4090240 158416 0 None -4 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
9995943 200535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Partial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assayPartial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL598935 200535 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Partial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assayPartial agonist activity at human GPR40 expressed in CHO cells assessed as fatty acid-induced calcium mobilization by FLIPR assay
ChEMBL 317 4 1 4 3.5 O=C1NC(=O)C(Cc2ccc(Oc3ccc(F)cc3)cc2)S1 10.1016/j.ejmech.2015.12.049
3514336 45980 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 4.0 O=C(O)C1CC(=O)N(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL1532576 45980 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 4.0 O=C(O)C1CC(=O)N(c2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.6b01559
24825486 86798 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1cccc(NCc2ccc(-c3ccccc3)cc2)c1 10.1016/j.bmcl.2006.12.084
CHEMBL232192 86798 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1cccc(NCc2ccc(-c3ccccc3)cc2)c1 10.1016/j.bmcl.2006.12.084
118623088 142125 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883407 142125 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
57522038 3885 60 None -1995 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assayAgonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
6490 3885 60 None -1995 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assayAgonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
CHEMBL2058533 3885 60 None -1995 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assayAgonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
24825498 153083 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 358 6 2 3 4.4 O=C(O)CCc1ccc(NCc2cc(C(F)(F)F)cnc2Cl)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL397613 153083 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 358 6 2 3 4.4 O=C(O)CCc1ccc(NCc2cc(C(F)(F)F)cnc2Cl)cc1 10.1016/j.bmcl.2006.12.084
24825497 161864 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 273 6 2 2 3.5 O=C(O)CCc1ccc(NCc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL414895 161864 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 273 6 2 2 3.5 O=C(O)CCc1ccc(NCc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.12.084
127033354 139129 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.5 O=C(O)CCc1ccc(C#CC2CC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786964 139129 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 214 3 1 1 2.5 O=C(O)CCc1ccc(C#CC2CC2)cc1 10.1021/acs.jmedchem.5b01962
145973087 164699 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 385 7 2 5 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4217225 164699 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 385 7 2 5 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(Cc3cccc(F)c3)s2)cc1 10.1016/j.ejmech.2017.09.019
145987309 167100 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4289942 167100 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@H](CC(=O)O)c1ccc(OC[C@@H]2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
127046665 139758 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)n1 10.1016/j.ejmech.2016.03.054
CHEMBL3798520 139758 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)n1 10.1016/j.ejmech.2016.03.054
145961656 161330 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 400 6 1 5 4.3 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccc(Cl)cc43)cc2)S1 10.1016/j.bmcl.2018.03.051
CHEMBL4125720 161330 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assayTransactivation of recombinant human FFAR1 expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium flux measured after 20 secs for 100 secs by FLIPR assay
ChEMBL 400 6 1 5 4.3 O=C1NC(=O)C(Cc2ccc(OCCn3ccc4ccc(Cl)cc43)cc2)S1 10.1016/j.bmcl.2018.03.051
46231433 200565 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 315 4 1 4 3.7 O=C1NC(=O)C(Cc2ccc(Sc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599068 200565 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 315 4 1 4 3.7 O=C1NC(=O)C(Cc2ccc(Sc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
54583582 62162 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777872 62162 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
145978511 163667 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 460 9 1 5 4.8 CCOc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4204628 163667 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 460 9 1 5 4.8 CCOc1ccc(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2017.07.001
44409877 75006 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 346 8 2 3 4.5 NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL203334 75006 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 346 8 2 3 4.5 NC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
148485044 175368 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 453 11 2 5 5.2 COCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4574808 175368 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 453 11 2 5 5.2 COCCOc1cc(C)c(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
155528599 171352 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2ccc(Cl)c(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4461611 171352 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 385 7 2 3 5.2 O=C(O)COc1ccc(NCc2ccc(Cl)c(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
561372 58825 65 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm101405t
CHEMBL1688452 58825 65 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm101405t
90151297 157198 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4075946 157198 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 513 6 1 5 5.7 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cc(Cl)ccc4F)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
57325916 74105 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022581 74105 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
24857286 1622 72 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
6484 1622 72 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
CHEMBL1829174 1622 72 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
DB12491 1622 72 None -3 3 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2018.07.048
57521811 76264 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Cl)cc2)cc1 10.1021/jm300215x
CHEMBL2058522 76264 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Cl)cc2)cc1 10.1021/jm300215x
25150114 185158 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1cccc(C#Cc2ccc(OCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL485713 185158 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 266 3 1 2 2.9 Cc1cccc(C#Cc2ccc(OCC(=O)O)cc2)c1 10.1021/jm8010178
54757627 65338 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 269 3 1 2 2.6 O=C(O)CCc1ccc(C#Cc2ccnc(F)c2)cc1 10.1021/jm2005699
CHEMBL1829158 65338 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 269 3 1 2 2.6 O=C(O)CCc1ccc(C#Cc2ccnc(F)c2)cc1 10.1021/jm2005699
127033020 139074 0 None 18 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 256 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786418 139074 0 None 18 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 256 3 1 1 3.6 O=C(O)CCc1ccc(C#CC2CCCCC2)cc1 10.1021/acs.jmedchem.5b01962
118637973 162741 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171391 162741 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
54586484 62152 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 62152 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serumAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 10% human serum
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
90644288 111953 0 None 20 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288346 111953 0 None 20 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
145965661 164096 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 450 7 1 4 4.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4209622 164096 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 450 7 1 4 4.8 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1 10.1016/j.ejmech.2017.07.001
71613311 89992 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381305 89992 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1cccc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
23157589 58841 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 373 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(CN(C)c2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688467 58841 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 373 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(CN(C)c2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
168285003 191523 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 492 11 1 4 7.2 Cc1ccc(OCCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5194153 191523 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 492 11 1 4 7.2 Cc1ccc(OCCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
137658243 159615 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 6 1 4 3.9 COc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103345 159615 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 6 1 4 3.9 COc1ccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)cc1 10.1021/acs.jmedchem.6b01559
145993621 167381 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cccc(Cl)c3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4294975 167381 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cccc(Cl)c3O2)cc1 10.1016/j.bmc.2018.10.019
1049 363 75 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
4618 363 75 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
5280934 363 75 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
CHEMBL8739 363 75 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
DB00132 363 75 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAgonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 10.1021/jm800970b
164616580 185325 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4859651 185325 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/CRE (Gs) assessed as firefly luciferase activity at 10 uM incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
90372613 167742 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4166625 167742 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302869 167742 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1 10.1021/acsmedchemlett.8b00149
57521808 76261 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL2058519 76261 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1cccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
71562424 86543 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccc(F)cc2)cc1 10.1021/jm301470a
CHEMBL2315544 86543 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccc(F)cc2)cc1 10.1021/jm301470a
54757732 65340 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 281 4 1 3 2.5 COc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
CHEMBL1829160 65340 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 281 4 1 3 2.5 COc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1 10.1021/jm2005699
54582149 61804 0 None 33 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773255 61804 0 None 33 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
57522038 3885 60 None -1995 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
6490 3885 60 None -1995 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
CHEMBL2058533 3885 60 None -1995 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
24857286 1622 72 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
6484 1622 72 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
CHEMBL1829174 1622 72 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
DB12491 1622 72 None -3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2021.127969
122185438 122677 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 325 8 1 4 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc(C#N)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604045 122677 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 325 8 1 4 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc(C#N)c2)cc1 10.1016/j.bmc.2015.07.028
54582629 62154 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 62154 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
137646482 157749 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082459 157749 0 None 2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
127047529 139816 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798881 139816 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 399 8 1 5 4.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
127032539 138808 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
CHEMBL3781077 138808 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 377 6 1 4 4.6 Cc1ccc(C)n1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1016/j.bmc.2017.12.030
145970371 165031 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 393 6 1 5 4.8 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.bmc.2017.12.030
CHEMBL4226180 165031 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 393 6 1 5 4.8 Cc1ccc(-c2c(C)noc2C)cc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.bmc.2017.12.030
54583098 61807 0 None 70 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
CHEMBL1773258 61807 0 None 70 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/ml100106c
44409927 77579 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 535 8 2 4 7.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N[C@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL208783 77579 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 535 8 2 4 7.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N[C@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2006.01.007
23159951 58854 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 338 7 1 3 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3cccs3)c2)cc1 10.1021/jm101405t
CHEMBL1688480 58854 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 338 7 1 3 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3cccs3)c2)cc1 10.1021/jm101405t
75202609 156736 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 7 1 4 5.5 COc1ccc(F)c(N2CCC(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4070443 156736 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 494 7 1 4 5.5 COc1ccc(F)c(N2CCC(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
46231483 200794 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 4 1 4 2.8 O=C1NC(=O)C(Cc2ccc(C(=O)c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL600658 200794 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 311 4 1 4 2.8 O=C1NC(=O)C(Cc2ccc(C(=O)c3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
145950191 162935 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 460 7 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4174315 162935 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 460 7 1 5 4.5 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
90372616 142231 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
145947998 167714 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4171104 167714 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL4302546 167714 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1 10.1021/acsmedchemlett.8b00149
155541840 173055 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 8 2 4 4.6 COc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4519415 173055 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 8 2 4 4.6 COc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
145975522 163539 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc(F)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
CHEMBL4202901 163539 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR methodAgonist activity at human GPR40/FFA1 expressed in CHO cells assessed as increase in calcium flux at 1 uM by Fluo-8 AM dye based FLIPR method
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc(F)cc3)s2)cc1 10.1016/j.ejmech.2017.09.019
131986112 164415 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4213548 164415 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
145950447 162984 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4175272 162984 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
155516498 170120 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4443853 170120 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 444 9 1 3 6.1 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@H](F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
132606863 157821 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157821 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
122193735 123966 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2018.07.050
CHEMBL3628755 123966 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 410 8 1 4 5.2 COc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2018.07.050
142738551 162039 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Cl)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4160141 162039 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Cl)cc2c1 10.1021/acsmedchemlett.7b00460
71612683 89969 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381281 89969 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
1052 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40Agonist activity at GPR40
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
122184686 122459 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccc(Cl)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601003 122459 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccc(Cl)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
168281295 190801 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc(OCC4CC4)cc3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5183783 190801 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3ccc(OCC4CC4)cc3)c2)cc1F 10.1016/j.bmc.2022.116615
168294961 192415 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5208111 192415 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 382 8 1 4 4.5 COc1cccc(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
23111754 74046 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022245 74046 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSAAgonist activity at human GPR40 expressed in CHO cells assessed as calcium influx by FLIPR assay in presence of 0.1 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
1052 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
90644289 111954 0 None -8 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288347 111954 0 None -8 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
145947764 167700 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4238097 167700 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4302391 167700 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4cccc5c4CCN(Cc4ccccc4)C5)c3)ccc21 10.1016/j.bmcl.2018.07.048
134153562 152721 0 None -758 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 394 7 1 3 4.9 O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F 10.1016/j.bmcl.2016.10.054
CHEMBL3973101 152721 0 None -758 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 394 7 1 3 4.9 O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F 10.1016/j.bmcl.2016.10.054
118637974 162036 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4160127 162036 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
134130787 142264 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884916 142264 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 471 7 1 4 6.4 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C#N)c1 10.1021/acsmedchemlett.6b00443
155527626 171229 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459709 171229 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 554 9 1 3 9.0 COc1ccc(F)c(-c2ccc3c(c2C2=CCCC2(C)C)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
46231844 200534 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 430 4 1 5 5.1 Cc1cc(Oc2ncc(C(F)(F)F)cc2Cl)cc(C)c1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
CHEMBL598934 200534 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 430 4 1 5 5.1 Cc1cc(Oc2ncc(C(F)(F)F)cc2Cl)cc(C)c1CC1SC(=O)NC1=O 10.1016/j.bmcl.2009.10.052
46231487 202445 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1 10.1016/j.bmcl.2009.10.052
CHEMBL611084 202445 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 4 1 4 3.7 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1 10.1016/j.bmcl.2009.10.052
118645756 181460 7 None -2 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 181460 7 None -2 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at rat GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
155527487 171214 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459517 171214 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
561372 58825 65 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm300215x
CHEMBL1688452 58825 65 None 20 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/jm300215x
145978233 163589 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 432 7 2 4 5.6 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4203471 163589 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 432 7 2 4 5.6 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)C(O)CC4CC(=O)O)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
145976608 163755 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccccc2F)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4205537 163755 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccccc2F)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2017.07.001
54585039 61801 5 None 17 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/ml100106c
CHEMBL1773252 61801 5 None 17 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 10.1021/ml100106c
1052 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
3323 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
5280450 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
CHEMBL267476 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
DB14104 2319 85 None -5 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 10.1016/j.bmcl.2008.10.085
134151151 154518 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 513 10 1 4 6.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3963542 154518 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 513 10 1 4 6.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990756 154518 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 513 10 1 4 6.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
51031010 156629 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4069191 156629 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
51357276 182005 0 None -10 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None -10 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
71612896 89980 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381293 89980 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 552 9 1 7 5.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
46231653 201111 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL603064 201111 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cn3)cc2)S1 10.1016/j.bmcl.2009.10.052
118642379 142117 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 142117 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
71615468 89989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2ccc(F)c(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381302 89989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2ccc(F)c(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
71613316 89997 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381310 89997 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
75511302 122451 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2coc(-c3cccc(F)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600995 122451 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2coc(-c3cccc(F)c3)n2)cc1 10.1016/j.bmcl.2015.06.018
122185445 122687 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 7 1 3 5.8 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604055 122687 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 7 1 3 5.8 CCOC(CC(=O)O)c1ccc(Oc2ccc(Cl)c3ccccc23)cc1 10.1016/j.bmc.2015.07.028
58218542 156764 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070703 156764 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
122185449 122691 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 1 4 3.7 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3ncccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604059 122691 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 327 7 1 4 3.7 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3ncccc32)cc1 10.1016/j.bmc.2015.07.028
58218638 157434 0 None -75 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4078852 157434 0 None -75 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
51350272 58839 0 None 107 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58839 0 None 107 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.5 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
11739868 75546 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@@H]1C[C@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL204455 75546 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 359 7 2 3 5.3 O=C(O)[C@@H]1C[C@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.007
25149900 172621 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 268 3 2 3 2.3 O=C(O)COc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm8010178
CHEMBL449321 172621 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 268 3 2 3 2.3 O=C(O)COc1ccc(C#Cc2cccc(O)c2)cc1 10.1021/jm8010178
23136363 58831 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2017.01.034
CHEMBL1688458 58831 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2017.01.034
137661929 159504 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4101950 159504 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 410 9 1 4 6.2 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)s1 10.1021/acs.jmedchem.6b01357
145959598 162353 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4165046 162353 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)s2)cc1 10.1016/j.ejmech.2018.04.023
24857286 1622 72 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
6484 1622 72 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL1829174 1622 72 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
DB12491 1622 72 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
145964820 164300 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 440 8 1 5 4.4 COc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4212170 164300 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 440 8 1 5 4.4 COc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
23136363 58831 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/ml100106c
CHEMBL1688458 58831 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/ml100106c
58218672 156719 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 3 4.6 Cc1ccccc1Sc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070270 156719 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 3 4.6 Cc1ccccc1Sc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57325678 74052 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 387 6 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(n2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022250 74052 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 387 6 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(n2)CCC3CC(=O)O)c1 10.1021/jm2012968
58319142 86516 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CO)cc1 10.1021/jm301470a
CHEMBL2315249 86516 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2ccccc2CO)cc1 10.1021/jm301470a
86803224 122449 24 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 337 7 1 4 4.2 Cc1oc(-c2ccccc2)nc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600993 122449 24 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 337 7 1 4 4.2 Cc1oc(-c2ccccc2)nc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2015.06.018
57398938 70024 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939653 70024 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2011.10.118
134130352 142143 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 142143 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
153213696 175511 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 351 7 2 3 4.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
CHEMBL4577954 175511 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 351 7 2 3 4.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3)c2)cc1F 10.1016/j.ejmech.2019.06.087
25150118 186688 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 295 4 1 3 3.0 O=C(O)CCc1ccc(C#Cc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm8010178
CHEMBL488396 186688 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 295 4 1 3 3.0 O=C(O)CCc1ccc(C#Cc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm8010178
44409916 138896 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C(C)CC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL378275 138896 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 434 7 2 4 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C(C)CC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
57393689 70011 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 380 8 1 3 5.0 COc1ccc(COc2ccc(C(CC(=O)O)c3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939640 70011 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 380 8 1 3 5.0 COc1ccc(COc2ccc(C(CC(=O)O)c3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2011.10.118
137632053 156355 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 386 8 1 4 5.2 COc1ccc(F)c(-c2cccc(COc3ccc(CCC(=O)O)s3)c2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4065959 156355 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 386 8 1 4 5.2 COc1ccc(F)c(-c2cccc(COc3ccc(CCC(=O)O)s3)c2)c1 10.1021/acs.jmedchem.6b01357
122185433 122662 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 391 9 1 5 3.1 CCOC(CC(=O)NS(C)(=O)=O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604031 122662 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 391 9 1 5 3.1 CCOC(CC(=O)NS(C)(=O)=O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmc.2015.07.028
127051658 140284 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3F)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805888 140284 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3F)s2)cc1 10.1016/j.bmc.2016.04.065
127050770 140289 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 419 8 2 6 3.7 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)c(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805952 140289 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 419 8 2 6 3.7 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)c(F)c3)s2)cc1 10.1016/j.bmc.2016.04.065
145991380 166983 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1ccnc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4287775 166983 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 428 7 1 6 3.9 Cn1ccnc1C(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
155513821 169812 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4439462 169812 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
146763588 173788 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 515 12 2 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4537797 173788 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 515 12 2 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
90151022 158328 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4089313 158328 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 509 7 1 6 5.1 COc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
118144976 171252 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4460109 171252 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
54586484 62152 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 62152 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albuminAgonist activity at human GPR40 expressed in HEK293 cells assessed as [3H]IP3 production in presence of 0.4% serum albumin
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
59541 176334 92 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assay
ChEMBL 168 3 1 2 1.9 O=C(O)CSc1ccccc1 10.1016/j.bmcl.2021.127969
CHEMBL459548 176334 92 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells by FLIPR calcium assay
ChEMBL 168 3 1 2 1.9 O=C(O)CSc1ccccc1 10.1016/j.bmcl.2021.127969
90655861 111248 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265145 111248 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
73891117 114261 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3330550 114261 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1016/j.bmcl.2016.10.074
6483 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
131986035 164055 0 None 5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4209136 164055 0 None 5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 612 10 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC5(C)CS(=O)(=O)C5)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
51350138 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2005699
CHEMBL1688473 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2005699
51350138 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL1688473 58847 0 None 660 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPRAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization in presence of 0.1% BSA by FLIPR
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
146316684 171563 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4464769 171563 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
68194743 182546 12 None -5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None -5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
6483 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
45107281 119121 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
CHEMBL3427702 119121 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1021/ml500391n
45107281 119121 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427702 119121 3 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
67087246 182875 5 None -12 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None -12 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
23157191 58840 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 359 7 2 2 5.6 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688466 58840 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 359 7 2 2 5.6 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
59590895 111253 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265150 111253 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
11674915 58860 1 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL1688486 58860 1 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1016/j.bmcl.2014.04.065
118638010 167563 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167563 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167563 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
146316684 171563 0 None 3 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4464769 171563 0 None 3 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
44409677 141229 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 447 6 3 5 5.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NO)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL382915 141229 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 447 6 3 5 5.4 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NO)cc1 10.1016/j.bmcl.2006.01.007
46854655 395 47 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300133f
6485 395 47 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300133f
CHEMBL1829173 395 47 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300133f
155527487 171214 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4459517 171214 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 460 8 1 3 6.8 COc1ccc(F)c(-c2ccc3c(c2)CC[C@@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
90150977 156167 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 521 7 1 5 6.2 CC(C)c1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4063905 156167 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 521 7 1 5 6.2 CC(C)c1ccc(F)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
15659413 98723 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL277845 98723 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
57521702 76260 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1ccccc1COc1ccc(CCC(=O)O)cc1 10.1021/jm300215x
CHEMBL2058518 76260 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1ccccc1COc1ccc(CCC(=O)O)cc1 10.1021/jm300215x
57521916 76271 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cc(Cl)ccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL2058529 76271 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2cc(Cl)ccc2-c2ccccc2)cc1 10.1021/jm300215x
54757516 65327 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccnc2Cl)cc1 10.1021/jm2005699
CHEMBL1829148 65327 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2cccnc2Cl)cc1 10.1021/jm2005699
44634023 65323 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2cccnc2)cc1 10.1021/jm2005699
CHEMBL1829144 65323 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2cccnc2)cc1 10.1021/jm2005699
15659413 98723 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL277845 98723 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 294 6 3 5 3.3 CC(C)CC(=O)c1c(O)cc(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
122193975 123977 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL3629049 123977 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 502 12 1 6 4.7 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
67087173 182458 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 182458 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134130696 142135 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
CHEMBL3883449 142135 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F 10.1021/acsmedchemlett.6b00443
127031413 138855 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 421 8 1 5 5.0 CCOc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
CHEMBL3781733 138855 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay
ChEMBL 421 8 1 5 5.0 CCOc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-n1c(C)ccc1C 10.1016/j.bmc.2016.03.014
145983006 165477 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 499 13 1 7 5.1 Cc1cc(OCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
CHEMBL4240026 165477 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 499 13 1 7 5.1 Cc1cc(OCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
71615669 90001 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 430 4 1 4 5.7 Cc1cc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381314 90001 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 430 4 1 4 5.7 Cc1cc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(C)c1 10.1016/j.bmcl.2013.03.060
86803186 122460 2 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3ccc(C(F)(F)F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601004 122460 2 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3ccc(C(F)(F)F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
168291030 191896 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 424 10 1 4 5.6 CCCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5199948 191896 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 424 10 1 4 5.6 CCCOc1ccc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c1 10.1016/j.bmc.2022.116615
145956739 162135 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 468 8 1 5 4.4 O=C(O)CCc1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4161630 162135 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 468 8 1 5 4.4 O=C(O)CCc1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
145986077 166449 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 342 4 1 2 4.7 Cc1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4277789 166449 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 342 4 1 2 4.7 Cc1ccccc1-c1cccc(COc2ccc(C#CC(=O)O)cc2)c1 10.1016/j.ejmech.2018.08.075
137629985 161022 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccncc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4101306 161022 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccncc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4116362 161022 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 544 12 1 6 5.9 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ccncc3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
137650498 157320 0 None -2 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 382 5 1 5 4.3 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3C#N)ccc12 10.1021/acs.jmedchem.7b00210
CHEMBL4077353 157320 0 None -2 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 382 5 1 5 4.3 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3C#N)ccc12 10.1021/acs.jmedchem.7b00210
137640163 156846 0 None -5 2 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 372 5 1 5 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(C(C)CC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
CHEMBL4071523 156846 0 None -5 2 Mouse 4.2 pEC50 = 4.2 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 372 5 1 5 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(C(C)CC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
127025285 137669 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 457 6 1 4 5.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccc(C(F)(F)F)cc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3758553 137669 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 457 6 1 4 5.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccc(C(F)(F)F)cc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
73356514 90373 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386368 90373 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 404 8 1 4 2.8 CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
54757514 65325 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
CHEMBL1829146 65325 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 265 3 1 2 2.8 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
44319268 107169 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL316370 107169 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
67058273 119127 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1021/ml500391n
CHEMBL3427708 119127 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1021/ml500391n
67058273 119127 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427708 119127 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 340 7 1 3 4.7 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
121294396 179658 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 603 12 1 7 6.5 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)OC)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4743254 179658 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 603 12 1 7 6.5 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C(CC(=O)O)OC)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
118719721 115662 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353742 115662 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2014.11.016
118719721 115662 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
CHEMBL3353742 115662 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR methodAgonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.09.010
118719721 115662 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
CHEMBL3353742 115662 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 516 12 1 6 5.0 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2015.10.011
57400636 70017 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 294 6 1 2 3.8 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939646 70017 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 294 6 1 2 3.8 CC#CC(CC(=O)O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
90151177 159730 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 491 7 1 6 5.0 COc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4104738 159730 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 491 7 1 6 5.0 COc1cccc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
57390187 70018 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 7 1 2 3.9 CC#CC(CC(=O)O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939647 70018 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 308 7 1 2 3.9 CC#CC(CC(=O)O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2011.10.118
137640032 156928 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2[C@@H](C)CC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4072491 156928 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2[C@@H](C)CC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
90151279 158238 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(Cl)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4088375 158238 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 495 6 1 5 5.6 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4ccc(Cl)cc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
118688890 190242 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)[C@H](CC(=O)O)CO3)c1 10.1016/j.bmc.2022.116615
CHEMBL5175124 190242 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)[C@H](CC(=O)O)CO3)c1 10.1016/j.bmc.2022.116615
131986297 164203 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210878 164203 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
46231840 200532 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
CHEMBL598917 200532 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2Cl)S1 10.1016/j.bmcl.2009.10.052
118737972 119129 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1021/ml500391n
CHEMBL3427710 119129 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1021/ml500391n
118737972 119129 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427710 119129 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 370 9 1 4 4.7 CCOc1cccc2c1CC[C@H]2Oc1ccc([C@H](CC(=O)O)OCC)cc1 10.1016/j.bmc.2015.07.028
58172969 122678 3 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 345 9 1 5 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc([N+](=O)[O-])c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604046 122678 3 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 345 9 1 5 3.7 CCOC(CC(=O)O)c1ccc(OCc2cccc([N+](=O)[O-])c2)cc1 10.1016/j.bmc.2015.07.028
23136363 58831 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm300215x
CHEMBL1688458 58831 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1021/jm300215x
145973478 164590 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 454 9 1 5 4.8 CCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4215675 164590 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 454 9 1 5 4.8 CCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
71612895 89930 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 398 3 1 4 4.3 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2380322 89930 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 398 3 1 4 4.3 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
75204487 158965 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4096102 158965 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
134144929 150447 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 418 5 2 4 6.2 O=C(O)CCc1ccc2oc(Nc3c(Cl)c(Cl)cc(Cl)c3Cl)nc2c1 10.1016/j.bmcl.2016.10.074
CHEMBL3954105 150447 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assayAgonist activity at rat GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4-AM dye based FLIPR assay
ChEMBL 418 5 2 4 6.2 O=C(O)CCc1ccc2oc(Nc3c(Cl)c(Cl)cc(Cl)c3Cl)nc2c1 10.1016/j.bmcl.2016.10.074
57521809 76262 0 None -13 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL2058520 76262 0 None -13 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
CHEMBL4210970 76262 0 None -13 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 10.1021/jm300215x
57521914 76269 0 None 6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 416 8 1 3 5.8 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300215x
CHEMBL2058527 76269 0 None 6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 416 8 1 3 5.8 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300215x
73777153 142821 0 None -81 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 355 3 1 2 5.2 O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 10.1021/acsmedchemlett.6b00360
CHEMBL3893026 142821 0 None -81 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 355 3 1 2 5.2 O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 10.1021/acsmedchemlett.6b00360
54582148 61795 4 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(COc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1773246 61795 4 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(COc2ccccc2)cc1 10.1021/ml100106c
134138318 148017 0 None -23 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 378 9 1 4 5.4 COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 10.1016/j.bmcl.2016.10.054
CHEMBL3934450 148017 0 None -23 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 378 9 1 4 5.4 COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 10.1016/j.bmcl.2016.10.054
57393691 70016 1 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939645 70016 1 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
118144976 171252 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4460109 171252 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 446 8 1 3 6.5 COc1ccc(F)c(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
162652399 180226 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4749949 180226 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
1050 1900 94 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.01.007
11595431 1900 94 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.01.007
CHEMBL207881 1900 94 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.01.007
127034369 138754 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2cccc(F)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780456 138754 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2cccc(F)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
137646308 157869 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 295 4 1 3 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4083913 157869 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 295 4 1 3 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)s1 10.1021/acs.jmedchem.6b01357
145992631 166863 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 392 8 1 5 4.1 CCOC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4285740 166863 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 392 8 1 5 4.1 CCOC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1 10.1016/j.bmc.2018.10.019
137635388 155822 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4059947 155822 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
145957539 162239 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4163496 162239 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
46231386 199230 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 3 4.0 O=C1CC(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)C(=O)N1 10.1016/j.bmcl.2009.10.052
CHEMBL589992 199230 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 349 4 1 3 4.0 O=C1CC(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)C(=O)N1 10.1016/j.bmcl.2009.10.052
8852666 192680 26 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
CHEMBL5219102 192680 26 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
57522038 3885 60 None -1995 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
6490 3885 60 None -1995 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
CHEMBL2058533 3885 60 None -1995 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1021/jm300215x
137658671 159446 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
CHEMBL4101219 159446 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 282 2 2 0 4.5 Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 10.1021/acs.jmedchem.6b01593
122185443 122685 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 9 1 3 5.2 CCOC(CC(=O)O)c1ccc(OCCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604053 122685 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 382 9 1 3 5.2 CCOC(CC(=O)O)c1ccc(OCCc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmc.2015.07.028
90644289 111954 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288347 111954 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 367 7 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
90644297 111962 0 None 32 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288355 111962 0 None 32 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.2 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
162676686 183484 0 None -11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 183484 0 None -11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
71615666 89998 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 388 4 1 4 4.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381311 89998 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 388 4 1 4 4.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2)c1)O3 10.1016/j.bmcl.2013.03.060
122193736 123967 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
CHEMBL3628756 123967 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.bmc.2015.10.011
71449361 80658 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
CHEMBL2151288 80658 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 400 8 1 3 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(-c3cccc(OC)c3)cc2)cc1 10.1021/ml300133f
168282466 191255 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 543 12 1 6 5.4 Cn1nc(COCc2ccccc2F)c2c1CCN(Cc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
CHEMBL5190303 191255 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 543 12 1 6 5.4 Cn1nc(COCc2ccccc2F)c2c1CCN(Cc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
155529599 171454 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(OC)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4463298 171454 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 458 8 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4cccc(OC)c4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
137646337 157926 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 353 5 1 3 5.2 CC(C)(C)c1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4084441 157926 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 353 5 1 3 5.2 CC(C)(C)c1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
44319268 107169 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL316370 107169 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 313 5 1 4 3.2 O=C1NC(=O)C(Cc2ccc(OCc3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
118638016 167650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163182 167650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301725 167650 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1 10.1021/acsmedchemlett.8b00149
145967091 164115 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 410 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4209845 164115 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 410 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
44409844 74487 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 459 6 1 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N(C)C)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL202835 74487 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 459 6 1 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)N(C)C)cc1 10.1016/j.bmcl.2006.01.007
71613315 89996 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381309 89996 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 422 4 1 4 5.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(-c2ccccc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
54757518 65330 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
CHEMBL1829150 65330 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 283 3 1 2 2.9 Cc1cnc(F)c(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2005699
1622278 95002 10 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 95002 10 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
127051659 140213 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
CHEMBL3805086 140213 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccc(F)cc3)s2)cc1 10.1016/j.bmc.2016.04.065
155565451 175593 11 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
CHEMBL4579901 175593 11 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assayAgonist activity at FFAR1 (unknown origin) expressed in CHO cells assessed as increase in calcium efflux by Fluo-4AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.bmcl.2021.127969
131986082 164152 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4210243 164152 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 454 7 1 7 4.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccnn4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58218608 156682 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4069764 156682 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
71613092 89983 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381296 89983 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1ccc(F)c([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
44409690 75571 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 420 7 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL204630 75571 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 420 7 2 4 5.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2006.01.007
168272362 190648 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3cccc(OCC4CC4)c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5181439 190648 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 422 10 1 4 5.3 O=C(O)COc1ccc(OCc2cccc(-c3cccc(OCC4CC4)c3)c2)cc1F 10.1016/j.bmc.2022.116615
162657311 180852 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 427 9 1 4 5.1 COc1ccc(F)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4757231 180852 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 427 9 1 4 5.1 COc1ccc(F)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
57393690 70015 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939644 70015 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 324 7 1 3 3.9 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
134136175 142678 0 None -51 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 388 7 1 3 5.5 Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
CHEMBL3892019 142678 0 None -51 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 388 7 1 3 5.5 Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
131986090 164290 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4212041 164290 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
23136411 58830 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
CHEMBL1688457 58830 0 None 11 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
5849 66 44 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
97783 66 44 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
CHEMBL4278254 66 44 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assayAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay
ChEMBL 216 10 2 2 3.0 CCCCCCCCCCC(C(=O)O)O 10.1039/C7MD00130D
134134149 143373 0 None -100 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 348 8 1 3 5.4 O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3897776 143373 0 None -100 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 348 8 1 3 5.4 O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2016.10.054
162644059 181822 0 None 45 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None 45 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
127033239 138737 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 387 6 1 6 4.7 Cc1nc(-c2ccsc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780232 138737 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 387 6 1 6 4.7 Cc1nc(-c2ccsc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
75511301 122461 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 342 7 1 5 3.5 O=C(O)CCc1ccc(OCc2nc(-c3ccc(F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3601005 122461 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 342 7 1 5 3.5 O=C(O)CCc1ccc(OCc2nc(-c3ccc(F)cc3)no2)cc1 10.1016/j.bmcl.2015.06.018
57705531 80665 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 464 9 1 3 7.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
CHEMBL2151295 80665 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 464 9 1 3 7.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
137640919 157070 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4074138 157070 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 331 5 1 3 4.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.6b01559
137659517 159257 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 500 6 1 6 5.1 Cc1ccc(C#N)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4099189 159257 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 500 6 1 6 5.1 Cc1ccc(C#N)c(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)CC2)c1 10.1021/acs.jmedchem.7b00982
168294722 192468 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 427 7 1 5 5.3 O=C(O)COc1ccc(COc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1F 10.1016/j.ejmech.2021.114061
CHEMBL5208754 192468 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assayAgonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay
ChEMBL 427 7 1 5 5.3 O=C(O)COc1ccc(COc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1F 10.1016/j.ejmech.2021.114061
1050 1900 94 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
11595431 1900 94 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
CHEMBL207881 1900 94 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumAgonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/jm0614782
164616580 185325 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
CHEMBL4859651 185325 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 297 4 2 1 4.3 Cc1cc(F)ccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1 10.1021/acs.jmedchem.1c00031
54584570 62147 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 344 5 1 2 5.2 O=C(O)CCc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777857 62147 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 344 5 1 2 5.2 O=C(O)CCc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
145983493 165502 0 None -371 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 442 10 1 4 5.1 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
CHEMBL4240607 165502 0 None -371 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo-4-AM dye based assay
ChEMBL 442 10 1 4 5.1 CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCC(=O)O)c(F)c3)c2)C1 10.1016/j.bmcl.2018.06.047
46231717 200945 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc(C(F)(F)F)c1 10.1016/j.bmcl.2009.10.052
CHEMBL601848 200945 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 382 4 1 5 4.1 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)nc(C(F)(F)F)c1 10.1016/j.bmcl.2009.10.052
46231718 201677 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.4 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL606206 201677 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 402 4 1 5 4.4 O=C1NC(=O)C(Cc2ccc(Oc3ncc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
118737971 119125 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1021/ml500391n
CHEMBL3427706 119125 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1021/ml500391n
118737971 119125 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427706 119125 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 4.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3ccccc32)cc1 10.1016/j.bmc.2015.07.028
57325674 74050 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022249 74050 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
127047530 139586 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 413 9 1 5 5.1 CCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797383 139586 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 413 9 1 5 5.1 CCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
145966647 164187 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 468 10 1 5 5.2 CCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4210719 164187 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 468 10 1 5 5.2 CCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1 10.1016/j.ejmech.2017.07.001
54582145 61791 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 361 8 2 3 5.0 COc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773167 61791 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 361 8 2 3 5.0 COc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
122193736 123967 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
CHEMBL3628756 123967 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 424 9 1 4 5.6 CCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1 10.1016/j.ejmech.2019.06.087
155558174 174764 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 7 3 4 4.6 Cc1cc(O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4561122 174764 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 381 7 3 4 4.6 Cc1cc(O)ccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
57706031 80666 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 10 1 3 7.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
CHEMBL2151296 80666 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 478 10 1 3 7.7 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c(C(C)(C)C)c2)c1 10.1021/ml300133f
145992604 166831 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 362 4 1 2 5.0 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2018.08.075
CHEMBL4285071 166831 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 362 4 1 2 5.0 O=C(O)C#Cc1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.ejmech.2018.08.075
58218740 156443 0 None -45 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4067052 156443 0 None -45 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
137529983 163875 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 516 8 2 5 6.2 Cc1cc(OCC2CCOC2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
CHEMBL4206879 163875 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 516 8 2 5 6.2 Cc1cc(OCC2CCOC2)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Nc1ccc([C@H]2C[C@@H]2C(=O)O)nc1 10.1021/acsmedchemlett.8b00343
131986294 163839 0 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206445 163839 0 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
118623088 142125 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
CHEMBL3883407 142125 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1 10.1021/acsmedchemlett.8b00149
10292451 122680 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604048 122680 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 368 8 1 3 4.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmc.2015.07.028
134131511 142156 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 142156 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
162664735 182084 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 182084 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
122185448 122690 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)c(F)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604058 122690 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)c(F)c2)cc1 10.1016/j.bmc.2015.07.028
118645541 180641 0 None 4 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4754974 180641 0 None 4 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 526 10 1 5 7.1 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2-c2cc(C)cc(C)c2)c1 10.1016/j.bmcl.2018.01.013
11961321 111797 4 None -4 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287569 111797 4 None -4 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
51350138 58847 0 None 660 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
CHEMBL1688473 58847 0 None 660 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
134131511 142156 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883627 142156 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 546 9 1 4 8.3 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/acsmedchemlett.6b00443
145987484 165208 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
CHEMBL4228985 165208 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay
ChEMBL 413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)ccc1Cl 10.1016/j.bmc.2017.12.030
155527805 171269 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4460425 171269 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 496 7 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
137635907 155946 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 527 7 1 6 5.0 COc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4061175 155946 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 527 7 1 6 5.0 COc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](F)C2)c1 10.1021/acs.jmedchem.7b00982
76900387 157543 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
CHEMBL4080226 157543 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 540 7 1 7 5.3 COc1cc(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1021/acs.jmedchem.7b00982
9957245 178983 14 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL470757 178983 14 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
11327107 74049 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
CHEMBL2022248 74049 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
162646017 179470 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4740846 179470 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
58319134 86552 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315553 86552 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 280 4 1 2 3.1 COc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
75511304 122452 3 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2coc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
CHEMBL3600996 122452 3 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
ChEMBL 323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2coc(-c3ccccc3)n2)cc1 10.1016/j.bmcl.2015.06.018
145990228 166904 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 436 7 1 5 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(F)(F)F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4286382 166904 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 436 7 1 5 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC(F)(F)F)cc3O2)cc1 10.1016/j.bmc.2018.10.019
54584571 62167 0 None -1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777877 62167 0 None -1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
54757517 65328 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccc(Cl)nc2)cc1 10.1021/jm2005699
CHEMBL1829149 65328 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 285 3 1 2 3.2 O=C(O)CCc1ccc(C#Cc2ccc(Cl)nc2)cc1 10.1021/jm2005699
134153148 152717 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 519 7 1 6 5.5 COc1ccc(C)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
CHEMBL3973075 152717 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assayAgonist activity at flag-tagged human GPR40 expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by FLIPR assay
ChEMBL 519 7 1 6 5.5 COc1ccc(C)c(N2CC[C@@H](Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmcl.2016.10.074
53248846 62151 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 62151 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
90644287 111952 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288345 111952 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 361 7 1 3 5.0 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)nc2)c1 10.1016/j.bmcl.2014.04.065
131986300 163625 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4203837 163625 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 528 8 1 6 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccc(OC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
57706778 80795 29 None -8 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
CHEMBL2152070 80795 29 None -8 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300133f
58218608 156682 0 None -10 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4069764 156682 0 None -10 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
145963330 162024 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 488 8 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4159848 162024 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 488 8 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
118129981 159465 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 159465 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
68194159 183059 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 183059 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
73354950 90376 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
CHEMBL2386370 90376 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 418 9 1 4 3.2 CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/ml4000673
46231548 200494 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1C 10.1016/j.bmcl.2009.10.052
CHEMBL598673 200494 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1C 10.1016/j.bmcl.2009.10.052
153272850 171892 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 376 7 2 4 4.4 N#Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4469691 171892 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 376 7 2 4 4.4 N#Cc1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
58218651 158317 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4089171 158317 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
71612681 90005 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 406 4 1 4 5.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381318 90005 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 406 4 1 4 5.0 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2F)c1)O3 10.1016/j.bmcl.2013.03.060
127033818 138745 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
CHEMBL3780334 138745 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2016.02.040
155551584 173997 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4542487 173997 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1 10.1016/j.bmcl.2019.04.050
121294455 181201 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.9 CCOC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4761155 181201 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 617 13 1 7 6.9 CCOC(CC(=O)O)c1cccc(OCC2CCN(c3cc(OC)ccc3C(=O)N(CC(C)(C)C)c3cccc(C)n3)CC2)c1 10.1021/acs.jmedchem.0c00843
58218638 157434 0 None 75 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4078852 157434 0 None 75 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
58218694 158469 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4090766 158469 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
25150016 185421 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cc(C)cc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL486139 185421 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cc(C)cc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
145971800 164497 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 424 8 1 4 4.9 CC(C)c1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4214530 164497 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 424 8 1 4 4.9 CC(C)c1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
71655293 90359 0 None 52 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
CHEMBL2386354 90359 0 None 52 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assayAgonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
ChEMBL 307 4 1 2 3.3 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml4000673
71612682 89968 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 456 4 1 4 5.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381280 89968 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 456 4 1 4 5.8 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccccc2C(F)(F)F)c1)O3 10.1016/j.bmcl.2013.03.060
71612680 90004 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 440 4 1 4 5.6 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccc(F)cc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381317 90004 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 440 4 1 4 5.6 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cccc(-c2ccc(F)cc2Cl)c1)O3 10.1016/j.bmcl.2013.03.060
57705719 164467 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 520 10 1 3 8.4 CC[C@H](CC(=O)O)c1ccc(F)c(OCc2ccc(-c3cc(OC)ccc3F)c(C3=CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4214121 164467 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 520 10 1 3 8.4 CC[C@H](CC(=O)O)c1ccc(F)c(OCc2ccc(-c3cc(OC)ccc3F)c(C3=CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
87262743 158779 0 None -4 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4094160 158779 0 None -4 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 449 6 1 4 5.6 O=C(O)C[C@@H]1C[C@H](C(F)(F)F)CN1c1ccc(Oc2ccccc2OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01559
54582149 61804 0 None 33 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
CHEMBL1773255 61804 0 None 33 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 281 6 1 3 3.2 N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm300215x
127027727 137811 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.2 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(C(F)(F)F)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759746 137811 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 501 9 1 5 6.2 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(C(F)(F)F)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
54584098 61803 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/jm300215x
CHEMBL1773254 61803 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/jm300215x
54757625 65336 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 270 3 1 2 3.5 Cc1ccsc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
CHEMBL1829156 65336 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 270 3 1 2 3.5 Cc1ccsc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm2005699
9957245 178983 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL470757 178983 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 490 22 3 5 9.0 CCCCCCCCCCCC(=O)c1c(O)cc(O)c(C(=O)CCCCCCCCCCC)c1O 10.1016/j.bmcl.2008.10.085
168279392 191138 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 421 9 2 3 5.6 CC1(C)C2CCC1(C)C(NCc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
CHEMBL5188313 191138 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in calcium efflux by Fluo-8AM dye based FLIPR assay
ChEMBL 421 9 2 3 5.6 CC1(C)C2CCC1(C)C(NCc1ccc(COc3ccc(CCC(=O)O)cc3)cc1)C2 10.1016/j.bmcl.2021.127969
142738582 184518 0 None 42 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
CHEMBL4847662 184518 0 None 42 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by cAMP-Glo assay
ChEMBL 293 4 2 1 4.5 Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 10.1021/acs.jmedchem.1c00031
118638010 167563 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4165008 167563 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
CHEMBL4300503 167563 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 480 7 1 5 5.7 COc1cc(-c2cnc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)c(F)cn1 10.1021/acsmedchemlett.8b00149
3893 2285 98 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
4642 2285 98 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
5534 2285 98 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL108766 2285 98 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
DB03017 2285 98 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
23346507 88286 1 None 30 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL234834 88286 1 None 30 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1021/ml100106c
54584571 62167 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777877 62167 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
57522038 3885 60 None -1995 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
6490 3885 60 None -1995 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
CHEMBL2058533 3885 60 None -1995 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmc.2017.10.040
145983825 165738 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 485 12 1 7 4.7 Cc1cc(OCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
CHEMBL4246335 165738 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 485 12 1 7 4.7 Cc1cc(OCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
127048842 140234 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 367 6 2 5 3.8 Cc1cccc(-c2cccc(NC(=O)c3nnc(CCC(=O)O)s3)c2)c1 10.1016/j.bmc.2016.04.065
CHEMBL3805328 140234 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium influx assayAgonist activity at human GPR40 expressed in CHO cells by calcium influx assay
ChEMBL 367 6 2 5 3.8 Cc1cccc(-c2cccc(NC(=O)c3nnc(CCC(=O)O)s3)c2)c1 10.1016/j.bmc.2016.04.065
90644302 111968 0 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288361 111968 0 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 301 8 1 4 3.2 CCOC(CC(=O)O)c1ccc(OCc2ccccc2)nc1 10.1016/j.bmcl.2014.04.065
1622278 95002 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 95002 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
90372616 142231 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884609 142231 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1 10.1021/acsmedchemlett.6b00443
145982433 166677 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1ccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)cc1 10.1016/j.ejmech.2018.09.071
CHEMBL4281988 166677 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 342 8 1 4 3.8 Cc1ccc(OCCCOc2ccc3c(c2)OCC3CC(=O)O)cc1 10.1016/j.ejmech.2018.09.071
90151763 157842 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccnc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
CHEMBL4083678 157842 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 462 6 1 6 4.3 C[C@@H]1C(C(F)(F)F)=NN(c2ccc(OC3CCN(c4cccnc4)CC3)cc2)[C@H]1CC(=O)O 10.1021/acs.jmedchem.7b00982
134141490 154582 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 527 10 1 4 6.6 Cc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3926143 154582 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 527 10 1 4 6.6 Cc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3991349 154582 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 527 10 1 4 6.6 Cc1ccc(CC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)cc1 10.1016/j.bmc.2016.09.004
53248846 62151 0 None 1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 62151 0 None 1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
57706009 80664 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 450 8 1 3 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151294 80664 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 450 8 1 3 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](C)CC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
57391960 70022 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml300133f
CHEMBL1939651 70022 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml300133f
127025488 137835 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 403 6 1 4 5.1 Cc1ccccc1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
CHEMBL3759922 137835 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 403 6 1 4 5.1 Cc1ccccc1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.ejmech.2015.12.049
142738553 162241 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4163511 162241 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 299 4 2 1 4.5 O=C(O)CCc1ccc2[nH]c(-c3ccc(Cl)cc3)cc2c1 10.1021/acsmedchemlett.7b00460
46231596 201971 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 401 4 1 4 5.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL607983 201971 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 401 4 1 4 5.0 O=C1NC(=O)C(Cc2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
90644303 111970 0 None -2 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288363 111970 0 None -2 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2cccc(C)c2)cc1 10.1016/j.bmcl.2014.04.065
137636358 155884 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4060499 155884 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
1622278 95002 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
CHEMBL254861 95002 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 H137F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 341 7 1 5 3.6 O=C(O)CCCCCN1C(=O)/C(=C\c2cccs2)SC1=S 10.1021/jm7012425
45107307 111969 4 None -3 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
CHEMBL3288362 111969 4 None -3 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 314 8 1 3 4.1 CCOC(CC(=O)O)c1ccc(OCc2ccccc2C)cc1 10.1016/j.bmcl.2014.04.065
71460255 80794 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL2152069 80794 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1021/acsmedchemlett.6b00443
71460255 80794 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL2152069 80794 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 420 9 1 3 6.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2)c1 10.1016/j.bmcl.2019.04.050
127047532 139647 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 9 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC(C)C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3797784 139647 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 9 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC(C)C)c1 10.1016/j.ejmech.2016.03.054
1050 1900 94 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
11595431 1900 94 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
CHEMBL207881 1900 94 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
145975484 163992 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 480 10 1 5 5.2 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4208237 163992 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 480 10 1 5 5.2 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
54757830 65349 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 335 3 1 2 4.3 O=C(O)CCc1ccc(C#Cc2ccnc3cc(Cl)ccc23)cc1 10.1021/jm2005699
CHEMBL1829169 65349 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 335 3 1 2 4.3 O=C(O)CCc1ccc(C#Cc2ccnc3cc(Cl)ccc23)cc1 10.1021/jm2005699
57521919 76275 0 None -23 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL2058532 76275 0 None -23 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
CHEMBL4207911 76275 0 None -23 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assayAgonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1016/j.bmc.2017.10.040
24825491 88029 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 305 6 2 2 4.5 O=C(O)CCc1ccc(NCc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234467 88029 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 305 6 2 2 4.5 O=C(O)CCc1ccc(NCc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2006.12.084
24825492 149540 0 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL394666 149540 0 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 10.1016/j.bmcl.2006.12.084
54757829 65348 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 375 5 1 2 4.7 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2Cc2ccccc2)cc1 10.1021/jm2005699
CHEMBL1829168 65348 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 375 5 1 2 4.7 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)c2Cc2ccccc2)cc1 10.1021/jm2005699
23346507 88286 1 None 30 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1016/j.bmcl.2006.12.084
CHEMBL234834 88286 1 None 30 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
ChEMBL 255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1 10.1016/j.bmcl.2006.12.084
137638995 156963 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4072885 156963 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
137642604 158515 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4091228 158515 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
16058685 172557 0 None -1 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cellsAgonist activity at mouse GPR40 expressed in HEK293 cells
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.bmcl.2008.10.085
CHEMBL448569 172557 0 None -1 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cellsAgonist activity at mouse GPR40 expressed in HEK293 cells
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.bmcl.2008.10.085
131986030 164812 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218596 164812 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 566 11 2 7 6.9 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCC(C)(C)O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
11674915 58860 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL1688486 58860 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b01357
137661294 159498 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101901 159498 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
68194743 182546 12 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
90357481 167614 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163916 167614 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301212 167614 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
162676686 183484 0 None -11 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 183484 0 None -11 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
90644296 111961 0 None 29 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288354 111961 0 None 29 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 4.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
11674915 58860 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688486 58860 1 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
57705880 111211 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL3264816 111211 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
57707025 164559 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4215239 164559 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 504 10 1 3 8.3 CC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
24857286 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
6484 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
CHEMBL1829174 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
DB12491 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2019.01.014
155512776 169662 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4437470 169662 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4Cl)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
155542122 173104 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
CHEMBL4520404 173104 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assayAgonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay
ChEMBL 462 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1 10.1016/j.bmcl.2019.01.014
145971688 163015 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4175666 163015 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 459 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCCc4ccccc43)s2)cc1 10.1016/j.ejmech.2018.04.023
24857286 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
6484 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
CHEMBL1829174 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
DB12491 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2018.10.019
90151527 157217 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
CHEMBL4076149 157217 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 493 6 1 5 5.4 Cc1cccc(F)c1N1CCC(Oc2ccc(N3N=C(C(F)(F)F)[C@@H](C)[C@@H]3CC(=O)O)cc2)CC1 10.1021/acs.jmedchem.7b00982
145947468 167672 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)CC5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4244619 167672 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)CC5)c3)ccc21 10.1016/j.bmcl.2018.07.048
CHEMBL4301987 167672 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CN(Cc4ccccc4)CC5)c3)ccc21 10.1016/j.bmcl.2018.07.048
145948093 167724 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 9 1 3 7.2 CC(C)(CC(=O)O)c1ccc(OCc2cccc(-c3cccc4c3CCN(Cc3ccccc3)C4)c2)cc1 10.1016/j.bmcl.2018.07.048
CHEMBL4241897 167724 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 9 1 3 7.2 CC(C)(CC(=O)O)c1ccc(OCc2cccc(-c3cccc4c3CCN(Cc3ccccc3)C4)c2)cc1 10.1016/j.bmcl.2018.07.048
CHEMBL4302692 167724 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assayTransactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay
ChEMBL 505 9 1 3 7.2 CC(C)(CC(=O)O)c1ccc(OCc2cccc(-c3cccc4c3CCN(Cc3ccccc3)C4)c2)cc1 10.1016/j.bmcl.2018.07.048
15659412 203948 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL6931 203948 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
145990337 166778 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 390 6 1 5 3.3 O=C(O)CC1(c2ccc(OCC3COc4ccc(Cl)cc4O3)cc2)COC1 10.1016/j.bmc.2018.10.019
CHEMBL4283988 166778 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 390 6 1 5 3.3 O=C(O)CC1(c2ccc(OCC3COc4ccc(Cl)cc4O3)cc2)COC1 10.1016/j.bmc.2018.10.019
145986689 167207 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 376 4 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2018.08.075
CHEMBL4291766 167207 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay
ChEMBL 376 4 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(C#CC(=O)O)cc3)c2)c(Cl)c1 10.1016/j.ejmech.2018.08.075
137634330 156373 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
CHEMBL4066238 156373 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 540 12 1 6 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)s1 10.1021/acs.jmedchem.6b01357
90644294 111959 0 None 13 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288352 111959 0 None 13 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1 10.1016/j.bmcl.2014.04.065
66562287 139176 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C=C(C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
CHEMBL3787463 139176 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 232 3 1 1 2.8 C=C(C)C#Cc1ccc(CCC(=O)O)c(F)c1 10.1021/acs.jmedchem.5b01962
51350272 58839 0 None 107 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1688465 58839 0 None 107 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albuminAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay in presence of 0.05 % bovine serum albumin
ChEMBL 346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
134133343 154473 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3F)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3898066 154473 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3F)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3990349 154473 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as induction of Ca2+ flux by fluo-8 dye based FLIPR assay
ChEMBL 531 10 1 4 6.4 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccccc3F)CCO4)cc2)cc1 10.1016/j.bmc.2016.09.004
118144982 170350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4447353 170350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 478 8 1 3 6.9 COc1ccc(F)c(-c2ccc3c(c2F)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
73777175 143907 0 None -17 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 357 3 1 2 4.9 O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 10.1021/acsmedchemlett.6b00360
CHEMBL3901994 143907 0 None -17 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
ChEMBL 357 3 1 2 4.9 O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 10.1021/acsmedchemlett.6b00360
71562640 86520 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 386 8 1 4 2.9 CS(=O)(=O)CCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315253 86520 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 386 8 1 4 2.9 CS(=O)(=O)CCCOc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm301470a
15659412 203948 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL6931 203948 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 266 4 3 5 2.5 CC(C)C(=O)c1c(O)cc(O)c(C(=O)C(C)C)c1O 10.1016/j.bmcl.2008.10.085
90372458 142222 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3884347 142222 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 500 7 1 3 7.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc(CCC(=O)O)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
51350273 58856 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
CHEMBL1688482 58856 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm101405t
137644843 158157 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 423 6 1 5 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)s2)c1 10.1021/acs.jmedchem.6b01357
CHEMBL4087365 158157 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
ChEMBL 423 6 1 5 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)s2)c1 10.1021/acs.jmedchem.6b01357
58173000 119126 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3427707 119126 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1016/j.bmc.2015.07.028
58218673 157523 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079930 157523 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
58218726 159136 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4097951 159136 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 5 1 3 5.3 Cc1cccc(C)c1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
71613093 89984 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381297 89984 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 570 9 1 7 5.4 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc([C@@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1 10.1016/j.bmcl.2013.03.060
145951402 162839 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 494 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(C4CCCCC4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4172853 162839 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 494 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(C4CCCCC4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
4987566 94657 2 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 333 7 2 3 4.6 O=C(O)c1cccc(NCc2cccc(OCc3ccccc3)c2)c1 10.1021/jm7012425
CHEMBL252527 94657 2 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayAgonist activity at FFAR1 expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 333 7 2 3 4.6 O=C(O)c1cccc(NCc2cccc(OCc3ccccc3)c2)c1 10.1021/jm7012425
137638317 156720 0 None -11 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 387 6 1 5 4.4 COc1cc(CCC(=O)O)ccc1-c1ccc2c(C)nn(-c3ccccn3)c2c1 10.1021/acs.jmedchem.7b00210
CHEMBL4070273 156720 0 None -11 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 387 6 1 5 4.4 COc1cc(CCC(=O)O)ccc1-c1ccc2c(C)nn(-c3ccccn3)c2c1 10.1021/acs.jmedchem.7b00210
131986250 163683 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4204776 163683 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 471 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(N4CCCCC4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58173000 119126 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1021/ml500391n
CHEMBL3427707 119126 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 7 1 3 3.8 CCO[C@@H](CC(=O)O)c1ccc(OC2Cc3ccccc3C2)cc1 10.1021/ml500391n
162675949 183296 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4797024 183296 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 614 12 1 7 6.8 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cc([C@H](CC(=O)O)C4CC4)ccn3)CC2)c1 10.1021/acs.jmedchem.0c00843
54583098 61807 0 None 70 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
CHEMBL1773258 61807 0 None 70 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 10.1021/jm300215x
58319094 86547 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 328 3 1 1 3.9 O=C(O)CCc1ccc(C#Cc2ccccc2Br)cc1 10.1021/jm301470a
CHEMBL2315548 86547 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 328 3 1 1 3.9 O=C(O)CCc1ccc(C#Cc2ccccc2Br)cc1 10.1021/jm301470a
127031001 139131 0 None 91 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.4 CC(C)=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
CHEMBL3786972 139131 0 None 91 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
ChEMBL 242 3 1 1 3.4 CC(C)=C(C)C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.5b01962
54586011 61806 0 None 14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
CHEMBL1773257 61806 0 None 14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/ml100106c
145981771 166666 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.7 O=C(O)CCc1ccc(OCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4281714 166666 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 366 6 1 4 3.7 O=C(O)CCc1ccc(OCC2COc3ccc(Cl)cc3O2)cc1F 10.1016/j.bmc.2018.10.019
561372 58825 65 None 20 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
CHEMBL1688452 58825 65 None 20 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/ml100106c
90372625 167719 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4159022 167719 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4302640 167719 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1 10.1021/acsmedchemlett.8b00149
57325841 74103 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022579 74103 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
121294461 182429 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 11 1 7 6.1 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C4(CC(=O)O)COC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4786019 182429 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 615 11 1 7 6.1 COc1ccc(C(=O)N(CC(C)(C)C)c2cccc(C)n2)c(N2CCC(COc3cccc(C4(CC(=O)O)COC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
90644288 111953 0 None -20 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288346 111953 0 None -20 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 366 7 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)s2)c1 10.1016/j.bmcl.2014.04.065
145994196 167393 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 354 9 1 4 3.8 O=C(O)COc1ccc(OCCCOc2cccc(Cl)c2)cc1F 10.1016/j.ejmech.2018.09.071
CHEMBL4295200 167393 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay
ChEMBL 354 9 1 4 3.8 O=C(O)COc1ccc(OCCCOc2cccc(Cl)c2)cc1F 10.1016/j.ejmech.2018.09.071
131986182 164619 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4216026 164619 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cc(OCCOC)ccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
54582628 62153 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777863 62153 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
44589697 191609 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 354 7 1 1 5.5 C=C/C=C/c1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1/C=C/C=C 10.1021/jm8010178
CHEMBL519548 191609 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 354 7 1 1 5.5 C=C/C=C/c1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1/C=C/C=C 10.1021/jm8010178
127033821 138814 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3781162 138814 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
57521812 76265 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 410 7 1 2 5.7 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Br)cc2)cc1 10.1021/jm300215x
CHEMBL2058523 76265 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 410 7 1 2 5.7 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Br)cc2)cc1 10.1021/jm300215x
127027728 137834 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 467 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759913 137834 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 467 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3)c3ccccc3)cc2)S1 10.1016/j.ejmech.2015.12.049
137642604 158515 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4091228 158515 0 None -41 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 370 7 1 3 5.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F 10.1016/j.bmcl.2017.01.034
131986162 164834 0 None -3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4218822 164834 0 None -3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 414 7 1 5 5.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CC4)c3c2)cc1 10.1016/j.bmcl.2017.12.022
58230598 183117 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 183117 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
148173135 171149 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 393 8 2 3 5.7 CC(C)c1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
CHEMBL4458669 171149 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assayAgonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
ChEMBL 393 8 2 3 5.7 CC(C)c1ccccc1-c1cccc(CNc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2019.06.087
137638995 156963 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
CHEMBL4072885 156963 0 None -16 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay
ChEMBL 338 6 1 2 4.6 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F 10.1016/j.bmcl.2017.01.034
127046667 139935 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccn1 10.1016/j.ejmech.2016.03.054
CHEMBL3799646 139935 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 370 7 1 5 4.1 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccn1 10.1016/j.ejmech.2016.03.054
155565379 175564 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
CHEMBL4579146 175564 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c(F)cn1 10.1016/j.bmcl.2019.04.050
25150015 185302 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm8010178
CHEMBL485935 185302 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 278 3 1 1 3.7 Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm8010178
3367 1155 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/jm2005699
46216676 1155 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/jm2005699
CHEMBL604126 1155 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/jm2005699
1050 1900 94 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
11595431 1900 94 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
CHEMBL207881 1900 94 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assayAgonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/ml100106c
168291052 191917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.4 Cc1ccc(OCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5200197 191917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 472 10 1 4 6.4 Cc1ccc(OCc2ccccc2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
54580626 62164 0 None 3 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777874 62164 0 None 3 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
131986065 163851 0 None -4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206579 163851 0 None -4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 465 7 1 6 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccnc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
46231841 202126 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 435 4 1 4 5.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2C(F)(F)F)S1 10.1016/j.bmcl.2009.10.052
CHEMBL609037 202126 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 435 4 1 4 5.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2C(F)(F)F)S1 10.1016/j.bmcl.2009.10.052
71615670 90002 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381315 90002 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 416 4 1 4 5.4 Cc1ccc(C)c(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1 10.1016/j.bmcl.2013.03.060
54582628 62153 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777863 62153 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
168289402 191309 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 408 7 1 4 5.8 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccsc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
CHEMBL5191306 191309 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 408 7 1 4 5.8 O=C(O)COc1ccc(OCc2cccc(-c3ccc4ccsc4c3)c2)cc1F 10.1016/j.bmc.2022.116615
137647107 157551 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4080336 157551 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
10266133 156166 5 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4063898 156166 5 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 4 2 0 5.6 CCCC(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
11507535 159296 1 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 3 2 0 5.4 CC(C)C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
CHEMBL4099626 159296 1 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assayAntagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
ChEMBL 288 3 2 0 5.4 CC(C)C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1021/acs.jmedchem.6b01593
58172991 122674 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 330 9 1 4 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604042 122674 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 330 9 1 4 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmc.2015.07.028
146316684 171563 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4464769 171563 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assayAgonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
58319135 86544 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 4 1 1 3.7 CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315545 86544 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 278 4 1 1 3.7 CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
25150013 186245 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2cccc(C(F)(F)F)c2)cc1 10.1021/jm8010178
CHEMBL487365 186245 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 318 3 1 1 4.1 O=C(O)CCc1ccc(C#Cc2cccc(C(F)(F)F)c2)cc1 10.1021/jm8010178
54584098 61803 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/ml100106c
CHEMBL1773254 61803 5 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 10.1021/ml100106c
127047533 139904 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 11 1 5 5.9 CCCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799443 139904 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 441 11 1 5 5.9 CCCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
137658391 159646 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
CHEMBL4103681 159646 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O 10.1021/acs.jmedchem.6b01559
25150117 186685 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2cccc(CO)c2)cc1 10.1021/jm8010178
CHEMBL488385 186685 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 280 4 2 2 2.6 O=C(O)CCc1ccc(C#Cc2cccc(CO)c2)cc1 10.1021/jm8010178
118645756 181460 7 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
CHEMBL4764485 181460 7 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulationAgonist activity at human GPR40 receptor expressed in CHOK1 cells assessed as induction of IP1 accumulation
ChEMBL 479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1 10.1016/j.bmcl.2018.01.013
131986295 163540 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4202907 163540 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCOC)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
131986294 163839 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206445 163839 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at human GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 464 7 1 5 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
90644562 111804 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
CHEMBL3287576 111804 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assayAgonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
118129979 155792 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155792 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
131986116 163822 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
CHEMBL4206318 163822 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assayAgonist activity at rat GPR40 assessed as increase in intracellular calcium flux by cell based FLIPR assay
ChEMBL 600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1 10.1016/j.bmcl.2017.12.022
51049992 145617 5 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3915620 145617 5 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assayAgonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
51049992 145617 5 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None -23 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assayAgonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
60195125 3886 8 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
9149 3886 8 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
CHEMBL2164242 3886 8 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/jm3002026
44409926 75981 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 485 7 2 4 6.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCC2)cc1 10.1016/j.bmcl.2006.01.007
CHEMBL205433 75981 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
ChEMBL 485 7 2 4 6.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc([C@H]2C[C@@H]2C(=O)NC2CCC2)cc1 10.1016/j.bmcl.2006.01.007
127045863 139978 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3799898 139978 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 403 7 1 4 5.3 Cc1noc(C)c1-c1ccc(Cl)c(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1016/j.ejmech.2016.03.054
90644293 111958 0 None 13 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
CHEMBL3288351 111958 0 None 13 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O 10.1016/j.bmcl.2014.04.065
60195038 81790 0 None 912 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 363 7 2 2 5.4 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
CHEMBL2164239 81790 0 None 912 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilizationAgonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
ChEMBL 363 7 2 2 5.4 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm3002026
142738539 162317 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Br)cc2c1 10.1021/acsmedchemlett.7b00460
CHEMBL4164625 162317 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayAgonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay
ChEMBL 343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3ccccc3Br)cc2c1 10.1021/acsmedchemlett.7b00460
118645671 180927 0 None 5 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4758060 180927 0 None 5 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 476 10 1 5 6.3 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C=C(C)C)c1 10.1016/j.bmcl.2018.01.013
162659599 181196 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4761101 181196 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 515 10 1 4 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1 10.1016/j.bmcl.2018.01.013
118645392 180107 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
CHEMBL4748392 180107 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysisAgonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis
ChEMBL 494 12 1 6 5.9 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2OCC(C)C)c1 10.1016/j.bmcl.2018.01.013
51350407 58862 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm101405t
CHEMBL1688488 58862 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
ChEMBL 360 7 1 2 5.6 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm101405t
45107323 122697 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 410 8 1 4 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(OC(F)(F)F)cccc32)cc1 10.1016/j.bmc.2015.07.028
CHEMBL3604065 122697 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 410 8 1 4 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(OC(F)(F)F)cccc32)cc1 10.1016/j.bmc.2015.07.028
57705679 163507 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(F)cc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4202429 163507 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 522 10 1 3 8.5 CC[C@H](CC(=O)O)c1cc(F)cc(OCc2ccc(-c3cc(OC)ccc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/acsmedchemlett.8b00213
57706280 164825 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 10 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
CHEMBL4218710 164825 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assayAgonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay
ChEMBL 530 10 1 3 8.7 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.8b00213
46231778 199479 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 4.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL591686 199479 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 368 4 1 5 4.1 O=C1NC(=O)C(Cc2ccc(Oc3ncc(Cl)cc3Cl)cc2)S1 10.1016/j.bmcl.2009.10.052
145992623 166856 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 352 6 1 4 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmc.2018.10.019
CHEMBL4285582 166856 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 352 6 1 4 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmc.2018.10.019
134130352 142143 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883532 142143 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1 10.1021/acsmedchemlett.6b00443
118145020 171067 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
CHEMBL4457184 171067 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting methodPositive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method
ChEMBL 461 8 1 4 6.2 COc1ccc(F)c(-c2cnc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)c1 10.1016/j.bmcl.2019.04.050
127046663 139773 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 439 10 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC2CC2)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798609 139773 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 439 10 1 5 5.5 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC2CC2)c1 10.1016/j.ejmech.2016.03.054
57705863 80663 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 436 8 1 3 6.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
CHEMBL2151293 80663 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serumAgonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum
ChEMBL 436 8 1 3 6.4 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C(C)(C)C)c1 10.1021/ml300133f
57391957 70010 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 312 8 1 3 4.0 C=CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
CHEMBL1939639 70010 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assayAgonist activity at human GPR40 expressed in CHO cells assessed as calcium flux measured for 20 secs by aequorin assay
ChEMBL 312 8 1 3 4.0 C=CC(CC(=O)O)c1ccc(OCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2011.10.118
137640781 157015 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 516 10 1 6 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Oc3ccccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
CHEMBL4073421 157015 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo-8 dye based FLIPR assay
ChEMBL 516 10 1 6 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Oc3ccccn3)CCO4)cc2)cc1 10.1016/j.ejmech.2017.01.005
57325917 74106 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022582 74106 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
54586011 61806 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
CHEMBL1773257 61806 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 324 6 1 2 4.3 O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 10.1021/jm300215x
25150012 193450 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 275 3 1 2 3.0 N#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
CHEMBL526510 193450 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 275 3 1 2 3.0 N#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1 10.1021/jm8010178
168274068 190284 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 478 10 1 4 6.8 Cc1ccc(OCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
CHEMBL5175750 190284 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay
ChEMBL 478 10 1 4 6.8 Cc1ccc(OCC2CCCCC2)cc1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2022.116615
90644295 111960 0 None -3 2 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288353 111960 0 None -3 2 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 375 7 1 3 5.3 Cc1cc(CCC(=O)O)cnc1OCc1cccc(-c2c(C)cccc2C)c1 10.1016/j.bmcl.2014.04.065
51349860 58826 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
CHEMBL1688453 58826 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assayAgonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1021/ml100106c
54757619 65331 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 286 3 1 3 2.5 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)n2)cc1 10.1021/jm2005699
CHEMBL1829151 65331 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 286 3 1 3 2.5 O=C(O)CCc1ccc(C#Cc2ccnc(Cl)n2)cc1 10.1021/jm2005699
118642379 142117 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
CHEMBL3883354 142117 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assayPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@@H](C)C(=O)O)cc4O3)cc2)c1 10.1021/acsmedchemlett.6b00443
118719720 115661 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 532 12 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(Cl)c2)c1 10.1016/j.bmc.2014.11.016
CHEMBL3353741 115661 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assayAgonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay
ChEMBL 532 12 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(Cl)c2)c1 10.1016/j.bmc.2014.11.016
90357481 167614 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4163916 167614 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
CHEMBL4301212 167614 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
ChEMBL 461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)c(F)c2)ccn1 10.1021/acsmedchemlett.8b00149
137646368 158026 0 None -3 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 358 5 1 5 3.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
CHEMBL4085695 158026 0 None -3 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assayAgonist activity at mouse GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins by FLUO-4-AM dye-based FLIPR assay
ChEMBL 358 5 1 5 3.8 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ncc12 10.1021/acs.jmedchem.7b00210
134133297 143777 0 None -117 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 372 7 1 3 4.9 Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
CHEMBL3900990 143777 0 None -117 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 372 7 1 3 4.9 Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O 10.1016/j.bmcl.2016.10.054
46231434 200603 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 297 4 1 3 3.2 O=C1NC(=O)C(Cc2ccc(Cc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
CHEMBL599270 200603 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 297 4 1 3 3.2 O=C1NC(=O)C(Cc2ccc(Cc3ccccc3)cc2)S1 10.1016/j.bmcl.2009.10.052
54582629 62154 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 62154 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
71562421 86538 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1cccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)c1 10.1021/jm301470a
CHEMBL2315539 86538 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 276 2 1 1 3.6 Cc1cccc(C#Cc2ccc([C@H]3C[C@@H]3C(=O)O)cc2)c1 10.1021/jm301470a
145985123 165907 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 513 14 1 7 5.5 Cc1cc(OCCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
CHEMBL4250135 165907 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay
ChEMBL 513 14 1 7 5.5 Cc1cc(OCCCCO[N+](=O)[O-])cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1 10.1016/j.bmc.2018.07.050
57521810 76263 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(F)cc2)cc1 10.1021/jm300215x
CHEMBL2058521 76263 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(F)cc2)cc1 10.1021/jm300215x
11265145 86532 1 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 248 2 1 1 3.2 O=C(O)/C=C/c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315533 86532 1 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 248 2 1 1 3.2 O=C(O)/C=C/c1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
145957539 162239 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
CHEMBL4163496 162239 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
ChEMBL 482 7 1 3 7.3 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3cccc(OC(F)(F)F)c3)cc1)CC2)C1CC1 10.1021/acsmedchemlett.8b00149
54580624 62150 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777860 62150 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
145954367 162563 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4168467 162563 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4[N+](=O)[O-])CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
71613095 89986 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
CHEMBL2381299 89986 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
ChEMBL 558 9 1 7 5.3 CS(=O)(=O)CCCOc1ccc(-c2cccc([C@@H]3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c(Cl)c1 10.1016/j.bmcl.2013.03.060
75204485 155994 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
CHEMBL4061819 155994 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
ChEMBL 496 8 1 5 5.0 COc1ccc(F)c(N2CC[C@H](COc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C2)c1 10.1021/acs.jmedchem.7b00982
23111754 74046 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022245 74046 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
134144214 150356 0 None -354 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 384 8 1 3 5.7 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
CHEMBL3953203 150356 0 None -354 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR40 measured after 60 mins by IP1-HTRF assayAgonist activity at human GPR40 measured after 60 mins by IP1-HTRF assay
ChEMBL 384 8 1 3 5.7 O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 10.1016/j.bmcl.2016.10.054
54582630 62156 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 62156 0 None 1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
71562637 86554 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2cccc(OC(F)(F)F)c2)cc1 10.1021/jm301470a
CHEMBL2315555 86554 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 334 4 1 2 4.0 O=C(O)CCc1ccc(C#Cc2cccc(OC(F)(F)F)c2)cc1 10.1021/jm301470a
25149901 186684 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
CHEMBL488384 186684 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
145974719 164694 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 482 10 1 5 5.4 Cc1cc(OCC(C)C)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
CHEMBL4217180 164694 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 482 10 1 5 5.4 Cc1cc(OCC(C)C)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1 10.1016/j.ejmech.2017.07.001
54585512 62161 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777871 62161 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
57521919 76275 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL2058532 76275 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1021/jm300215x
CHEMBL4207911 76275 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 10.1021/jm300215x
54757620 65332 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 282 4 1 4 1.9 COc1nccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
CHEMBL1829152 65332 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL 282 4 1 4 1.9 COc1nccc(C#Cc2ccc(CCC(=O)O)cc2)n1 10.1021/jm2005699
25149901 186684 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
CHEMBL488384 186684 1 None 61 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assayAgonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay
ChEMBL 250 3 1 1 3.1 O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 10.1021/jm8010178
46231488 199340 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cc(C)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
CHEMBL590699 199340 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
ChEMBL 327 4 1 4 4.0 Cc1cc(C)cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c1 10.1016/j.bmcl.2009.10.052
90644299 111964 0 None -5 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
CHEMBL3288357 111964 0 None -5 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1 10.1016/j.bmcl.2014.04.065
127029850 138736 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
CHEMBL3780211 138736 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx by FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2016.02.040
127047531 139719 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 10 1 5 5.5 CCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
CHEMBL3798213 139719 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assayAgonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay
ChEMBL 427 10 1 5 5.5 CCCOc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1 10.1016/j.ejmech.2016.03.054
57325840 74102 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 460 10 1 4 5.8 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022578 74102 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSAAgonist activity at human GR40 receptor expressed in CHO cells assessed as increase in intracellular calcium concentration after 90 secs by FLIPR assay in presence of 0.1% BSA
ChEMBL 460 10 1 4 5.8 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
58218655 156163 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4063889 156163 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
145957072 162272 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc(F)c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
CHEMBL4163958 162272 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assayAgonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
ChEMBL 506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc(F)c4)CC3)s2)cc1 10.1016/j.ejmech.2018.04.023
24825509 87944 0 None 29 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
CHEMBL234057 87944 0 None 29 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 10.1021/jm300215x
145967558 164830 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 398 8 1 5 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
CHEMBL4218763 164830 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
ChEMBL 398 8 1 5 3.9 O=C(O)CS(=O)(=O)c1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.ejmech.2017.07.001
853224 94573 11 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
CHEMBL251963 94573 11 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assayActivity at FFAR1 L186F mutant expressed in HEK-EM293 cells assessed as calcium influx by FLIPR assay
ChEMBL 348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1 10.1021/jm7012425
58172984 122670 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 398 9 1 4 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmc.2015.07.028
CHEMBL3604039 122670 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 398 9 1 4 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmc.2015.07.028
54581632 62148 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 388 6 2 3 4.5 O=C(O)C(Cc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1)C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777858 62148 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 388 6 2 3 4.5 O=C(O)C(Cc1ccc(Oc2ccc(C(F)(F)F)cc2Cl)cc1)C(=O)O 10.1016/j.bmcl.2011.03.114
146314522 180718 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 495 12 2 5 5.7 COc1ccc(CCC(C)(C)O)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
CHEMBL4755717 180718 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assayAgonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay
ChEMBL 495 12 2 5 5.7 COc1ccc(CCC(C)(C)O)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acs.jmedchem.0c00843
44571477 183940 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL481542 183940 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
70522117 86555 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 236 2 1 1 2.7 O=C(O)Cc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
CHEMBL2315556 86555 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
ChEMBL 236 2 1 1 2.7 O=C(O)Cc1ccc(C#Cc2ccccc2)cc1 10.1021/jm301470a
44571477 183940 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
CHEMBL481542 183940 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assayAgonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
ChEMBL 350 9 3 5 4.6 CCCCc1c(O)c(C(=O)CC(C)C)c(O)c(C(=O)CC(C)C)c1O 10.1016/j.bmcl.2008.10.085
25098573 2745 8 None -8 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm300215x
5587 2745 8 None -8 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm300215x
CHEMBL463785 2745 8 None -8 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
ChEMBL 376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 10.1021/jm300215x
58172978 122669 2 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 402 8 1 3 5.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1Cl 10.1016/j.bmc.2015.07.028
CHEMBL3604038 122669 2 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
ChEMBL 402 8 1 3 5.8 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1Cl 10.1016/j.bmc.2015.07.028
145982071 166474 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3cc(Br)ccc3O2)cc1F 10.1016/j.bmc.2018.10.019
CHEMBL4278249 166474 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
ChEMBL 410 6 1 4 3.8 O=C(O)CCc1ccc(OCC2COc3cc(Br)ccc3O2)cc1F 10.1016/j.bmc.2018.10.019
54583581 62158 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777868 62158 0 None 2 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at mouse GPR40 expressed in CHO cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
12002185 75831 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048625 75831 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSAAgonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
1050 1900 94 None 1 3 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
11595431 1900 94 None 1 3 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
CHEMBL207881 1900 94 None 1 3 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayAgonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.04.065
85970906 137776 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 389 6 1 4 4.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccccc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
CHEMBL3759467 137776 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
ChEMBL 389 6 1 4 4.8 O=C1NC(=O)C(Cc2ccc(OCc3cccc(-c4ccccc4)c3)cc2)S1 10.1016/j.ejmech.2015.12.049
44591693 184233 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 419 6 1 2 5.8 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483546 184233 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 419 6 1 2 5.8 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
44591612 184522 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 421 6 1 3 5.4 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(O[C@H]2CC[C@@H](C)CC2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL484771 184522 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 421 6 1 3 5.4 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(O[C@H]2CC[C@@H](C)CC2)cc1 10.1016/j.bmcl.2009.03.082
44591719 184776 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 408 6 1 4 5.1 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1nc2ccccc2s1 10.1016/j.bmcl.2009.03.082
CHEMBL485131 184776 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 408 6 1 4 5.1 CCC(CC)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1nc2ccccc2s1 10.1016/j.bmcl.2009.03.082
127038399 136755 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 338 6 1 5 4.1 CC(C)Nc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741045 136755 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 338 6 1 5 4.1 CC(C)Nc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
4671033 145360 9 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 339 5 1 3 4.6 Cc1ccc(S(=O)(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3913640 145360 9 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 339 5 1 3 4.6 Cc1ccc(S(=O)(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1021/acs.jmedchem.6b00685
127042700 136670 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccccc2C#N)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740222 136670 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccccc2C#N)nc(-c2ccccn2)n1 10.1039/C5MD00037H
100502467 142851 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 357 5 0 3 4.4 CN(c1ccc(Oc2ccccc2)cc1)S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3893258 142851 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 357 5 0 3 4.4 CN(c1ccc(Oc2ccccc2)cc1)S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
44591691 184209 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 349 4 1 3 4.2 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
CHEMBL483342 184209 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 349 4 1 3 4.2 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
44591613 184523 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 387 5 1 3 4.9 CCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL484772 184523 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 387 5 1 3 4.9 CCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
127040115 136654 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 401 7 0 5 4.7 Fc1ccc(OCc2cc(OCC3CCC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3740072 136654 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 401 7 0 5 4.7 Fc1ccc(OCc2cc(OCC3CCC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127042382 136574 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 5 0 5 3.3 COc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739442 136574 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 5 0 5 3.3 COc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042380 136639 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)cc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739963 136639 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)cc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
674995 143002 14 None -3 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 343 5 1 3 4.4 O=S(=O)(Nc1ccc(Oc2ccccc2)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3894632 143002 14 None -3 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 343 5 1 3 4.4 O=S(=O)(Nc1ccc(Oc2ccccc2)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b00685
44591692 184232 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 405 5 1 2 5.4 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483545 184232 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 405 5 1 2 5.4 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
44591651 184702 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 373 4 1 3 4.5 CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485025 184702 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 373 4 1 3 4.5 CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
126961699 136678 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3740291 136678 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
127042378 136898 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)ccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3742333 136898 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2c(F)ccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127041066 136904 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 5 0 5 3.3 CN(C)c1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3742371 136904 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 5 0 5 3.3 CN(C)c1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
134134846 144237 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 337 3 0 3 4.2 O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3904654 144237 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 337 3 0 3 4.2 O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
127040434 136721 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccccc1OCc1cc(C)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740758 136721 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccccc1OCc1cc(C)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040748 136729 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1cccc(OCc2cc(C)nc(-c3ccccn3)n2)c1 10.1039/C5MD00037H
CHEMBL3740835 136729 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1cccc(OCc2cc(C)nc(-c3ccccn3)n2)c1 10.1039/C5MD00037H
134147328 150047 0 None -3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 394 4 0 4 4.4 N#CCc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3950610 150047 0 None -3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 394 4 0 4 4.4 N#CCc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
44591628 184687 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2cc(C)cc(C)c2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485006 184687 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2cc(C)cc(C)c2)cc1 10.1016/j.bmcl.2009.03.082
44244518 184909 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 5 1 3 4.8 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
CHEMBL485328 184909 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 5 1 3 4.8 CC[C@H](C)CN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cc2ccccc2o1 10.1016/j.bmcl.2009.03.082
25272661 184783 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 339 5 1 3 3.5 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485146 184783 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 339 5 1 3 3.5 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1016/j.bmcl.2009.03.082
44591690 184276 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 343 4 1 2 4.1 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483937 184276 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 343 4 1 2 4.1 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.082
67134965 151004 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 4 0 3 4.1 O=S1(=O)c2ccccc2CN1c1cc(F)cc(OCc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3958418 151004 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 4 0 3 4.1 O=S1(=O)c2ccccc2CN1c1cc(F)cc(OCc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
127038400 136874 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 400 5 0 5 4.4 CC1(C)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3742135 136874 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 400 5 0 5 4.4 CC1(C)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
5332902 136600 4 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 288 4 1 4 3.9 Cc1cc(N/N=C/c2ccccc2)nc(-c2ccccc2)n1 10.1039/C5MD00037H
CHEMBL3739652 136600 4 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 288 4 1 4 3.9 Cc1cc(N/N=C/c2ccccc2)nc(-c2ccccc2)n1 10.1039/C5MD00037H
127040096 136610 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739712 136610 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040433 136790 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccc(Cl)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741358 136790 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccc(Cl)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042383 136857 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 325 6 0 5 3.7 CCOc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741974 136857 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 325 6 0 5 3.7 CCOc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042701 136747 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2cccc(C#N)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740984 136747 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2cccc(C#N)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
134154953 151274 0 None -7 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3960369 151274 0 None -7 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
805130 95036 13 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 348 6 1 4 4.3 O=C(NCc1cccc(Oc2ccccc2)c1)c1ccc([N+](=O)[O-])cc1 10.1021/jm7012425
CHEMBL255074 95036 13 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 348 6 1 4 4.3 O=C(NCc1cccc(Oc2ccccc2)c1)c1ccc([N+](=O)[O-])cc1 10.1021/jm7012425
134138099 147820 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3932897 147820 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
44591630 191482 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 470 6 1 4 5.7 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL519358 191482 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 470 6 1 4 5.7 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.03.082
44591629 184688 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C)c(C)c2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485007 184688 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 429 6 1 3 5.9 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Oc2ccc(C)c(C)c2)cc1 10.1016/j.bmcl.2009.03.082
127040388 136754 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccccc2Cl)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741030 136754 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2ccccc2Cl)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040116 136795 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 403 7 0 6 3.6 Fc1ccc(OCc2cc(OCC3COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741385 136795 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 403 7 0 6 3.6 Fc1ccc(OCc2cc(OCC3COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127040723 136847 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 388 5 1 6 2.7 OC1CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3741899 136847 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 388 5 1 6 2.7 OC1CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
127042702 136828 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccc(C#N)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741704 136828 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 302 4 0 5 3.3 Cc1cc(COc2ccc(C#N)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
134141650 146697 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3923955 146697 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 10.1021/acs.jmedchem.6b00685
134145778 149345 0 None -13 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 355 3 0 3 4.3 O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3945213 149345 0 None -13 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 355 3 0 3 4.3 O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 10.1021/acs.jmedchem.6b00685
127040118 136587 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 442 8 0 7 3.8 N#CCC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
CHEMBL3739522 136587 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 442 8 0 7 3.8 N#CCC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
127039708 136661 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2cccc(Cl)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740168 136661 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 311 4 0 4 4.1 Cc1cc(COc2cccc(Cl)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040059 136679 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccccc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740298 136679 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccccc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042381 136697 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740515 136697 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042379 136738 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740906 136738 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)c(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127038708 136763 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741109 136763 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)cc2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040094 136777 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2cccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741230 136777 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2cccc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
44591652 191593 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 413 6 1 3 5.3 O=C(O)[C@@H]1c2ccccc2C(=O)N(CC2CC2)[C@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL519525 191593 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 413 6 1 3 5.3 O=C(O)[C@@H]1c2ccccc2C(=O)N(CC2CC2)[C@H]1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
134153067 152254 0 None -16 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 10.1021/acs.jmedchem.6b00685
CHEMBL3969073 152254 0 None -16 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 369 3 0 3 4.6 Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 10.1021/acs.jmedchem.6b00685
127038401 136782 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 414 5 0 6 3.5 Fc1ccc(OCc2cc(N3CC4(CCO4)C3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741297 136782 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 414 5 0 6 3.5 Fc1ccc(OCc2cc(N3CC4(CCO4)C3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127040095 136813 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741570 136813 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 313 4 0 4 3.7 Cc1cc(COc2ccc(F)c(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127039385 136815 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 433 8 0 7 3.3 COC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
CHEMBL3741582 136815 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 433 8 0 7 3.3 COC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
127040097 136851 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)cc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741919 136851 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2cc(F)cc(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
2233248 168861 9 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 334 5 1 4 4.6 O=C(Nc1ccccc1)c1cccc(Oc2ccc([N+](=O)[O-])cc2)c1 10.1021/jm7012425
CHEMBL438164 168861 9 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assayAntagonist activity at FFAR1 expressed in HEK-EM293 cells assessed as inhibition calcium influx by FLIPR assay
ChEMBL 334 5 1 4 4.6 O=C(Nc1ccccc1)c1cccc(Oc2ccc([N+](=O)[O-])cc2)c1 10.1021/jm7012425
134152545 153475 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3979588 153475 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 380 3 0 4 4.2 N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 10.1021/acs.jmedchem.6b00685
127041988 136832 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741735 136832 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
58137077 136611 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 348 5 0 6 3.0 c1ccc(OCc2cc(N3CCOCC3)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
CHEMBL3739715 136611 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 348 5 0 6 3.0 c1ccc(OCc2cc(N3CCOCC3)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
127040093 136682 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccc(F)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740314 136682 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2ccc(F)cc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127042713 136845 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 6 1 5 3.7 CCNc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3741858 136845 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 324 6 1 5 3.7 CCNc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127038402 136789 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 478 7 0 7 3.4 CC1(CS(C)(=O)=O)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3741353 136789 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 478 7 0 7 3.4 CC1(CS(C)(=O)=O)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
127038403 136788 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 415 6 0 5 4.5 Fc1ccc(OCc2cc(OCC(F)(F)F)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741349 136788 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 415 6 0 5 4.5 Fc1ccc(OCc2cc(OCC(F)(F)F)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
127040117 136703 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 417 7 0 6 4.0 CC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
CHEMBL3740598 136703 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 417 7 0 6 4.0 CC1(COc2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)COC1 10.1039/C5MD00037H
127040432 136698 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 277 4 0 4 3.4 Cc1cc(COc2ccccc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740555 136698 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 277 4 0 4 3.4 Cc1cc(COc2ccccc2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127039748 136724 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3740771 136724 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 295 4 0 4 3.6 Cc1cc(COc2cccc(F)c2)nc(-c2ccccn2)n1 10.1039/C5MD00037H
127040749 136581 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccc(OCc2cc(C)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
CHEMBL3739500 136581 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysisAntagonist activity against human GPR40 expressed in HEK293s FLPIN cells assessed as elaidic acid stimulated IP1 release after 2 hrs by TR-FRET analysis
ChEMBL 307 5 0 5 3.4 COc1ccc(OCc2cc(C)nc(-c3ccccn3)n2)cc1 10.1039/C5MD00037H
2843133 147645 51 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 307 6 1 2 4.0 CCCCc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b00685
CHEMBL3931570 147645 51 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assayAntagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay
ChEMBL 307 6 1 2 4.0 CCCCc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b00685
44591689 184275 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 4 1 2 4.8 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
CHEMBL483936 184275 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 377 4 1 2 4.8 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.03.082
44591627 184920 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 415 7 1 3 5.0 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
CHEMBL485335 184920 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assayAntagonist activity at human GPR40 expressed HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay
ChEMBL 415 7 1 3 5.0 CCCN1C(=O)c2ccccc2[C@@H](C(=O)O)[C@@H]1c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2009.03.082
5280933 178218 64 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
Drug Central 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O None
CHEMBL464982 178218 64 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assayAgonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay
Drug Central 278 13 1 1 5.7 CCCCC/C=C\C/C=C\C/C=C\CCCCC(=O)O None
1049 363 75 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
4618 363 75 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
5280934 363 75 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
CHEMBL8739 363 75 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
DB00132 363 75 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assayAgonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay
Drug Central 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O None
1056 3369 116 None 15 10 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
2405 3369 116 None 15 10 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
77999 3369 116 None 15 10 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
CHEMBL121 3369 116 None 15 10 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
DB00412 3369 116 None 15 10 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C None
1052 2319 85 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
3323 2319 85 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
5280450 2319 85 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
CHEMBL267476 2319 85 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
DB14104 2319 85 None -5 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O None
1054 2915 85 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
3400 2915 85 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
445639 2915 85 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
CHEMBL8659 2915 85 None 1 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O None
1051 1454 63 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
4289 1454 63 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
445580 1454 63 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
57417355 1454 63 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
CHEMBL367149 1454 63 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
DB03756 1454 63 None -14 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O None
3893 2285 98 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
4642 2285 98 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
5534 2285 98 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
CHEMBL108766 2285 98 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
DB03017 2285 98 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assayAgonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay
Drug Central 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O None
10043 3592 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
24749700 3592 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
CHEMBL4297635 3592 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
DB15447 3592 0 None -2 2 Human 3.0 pEC50 = 3.0 Functional
In a β-arrestin 2 recruitment assay measured by BRET.In a β-arrestin 2 recruitment assay measured by BRET.
Guide to Pharmacology 206 6 1 1 3.0 CCCCCc1cccc(c1)CC(=O)O 29454750
1055 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
1055 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
1055 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
135369651 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
135369651 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
135369651 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
985 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
985 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
985 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
CHEMBL82293 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
CHEMBL82293 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
CHEMBL82293 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
DB03796 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12496284
DB03796 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12565875
DB03796 2992 105 None -2884 2 Human 4.6 pEC50 = 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 14 1 1 5.6 CCCCCCCCCCCCCCCC(=O)O 12629551
1054 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
1054 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
1054 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
3400 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
3400 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
3400 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
445639 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
445639 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
445639 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
CHEMBL8659 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12496284
CHEMBL8659 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12565875
CHEMBL8659 2915 85 None 1 5 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 12629551
11005 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
11005 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
11005 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
2806 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
2806 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
2806 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
CHEMBL111077 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
CHEMBL111077 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
CHEMBL111077 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
DB08231 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12496284
DB08231 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12565875
DB08231 2692 107 None -2 3 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 228 12 1 1 4.8 CCCCCCCCCCCCCC(=O)O 12629551
1052 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
1052 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
1052 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
3323 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
3323 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
3323 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
5280450 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
5280450 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
5280450 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
CHEMBL267476 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
CHEMBL267476 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
CHEMBL267476 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
DB14104 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12496284
DB14104 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12565875
DB14104 2319 85 None -5 4 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O 12629551
1049 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
1049 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
1049 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
4618 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
4618 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
4618 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
5280934 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
5280934 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
5280934 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
CHEMBL8739 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
CHEMBL8739 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
CHEMBL8739 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
DB00132 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12496284
DB00132 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12565875
DB00132 363 75 None 1 3 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O 12629551
1051 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
1051 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
4289 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
4289 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
445580 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
445580 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
57417355 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
57417355 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
CHEMBL367149 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
CHEMBL367149 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
DB03756 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12496284
DB03756 1454 63 None -14 2 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 14 1 1 6.5 CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O 12629551
3367 1155 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 18477808
46216676 1155 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 18477808
CHEMBL604126 1155 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 18477808
24857286 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
24857286 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
24857286 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
24857286 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
6484 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
6484 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
6484 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
6484 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
CHEMBL1829174 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
CHEMBL1829174 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
CHEMBL1829174 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
CHEMBL1829174 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
DB12491 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 21752941
DB12491 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 24900210
DB12491 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25043059
DB12491 1622 72 None -3 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 25787200
1050 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 16702987
11595431 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 16702987
CHEMBL207881 1900 94 None -1 3 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 16702987
25150014 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 18947221
3952 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 18947221
CHEMBL449588 3883 55 None 44 2 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 18947221
10668 1951 16 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 31971610
139600331 1951 16 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 31971610
CHEMBL5169614 1951 16 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 7 1 3 4.8 OC(=O)COc1ccc(cc1F)OCc1cccc(c1)c1ccccc1C 31971610
60195125 3886 8 None 4 3 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 22724451
9149 3886 8 None 4 3 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 22724451
CHEMBL2164242 3886 8 None 4 3 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 22724451
6483 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 23687558
66553168 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 23687558
CHEMBL2386353 3884 54 None 13 4 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 23687558
46854655 395 47 None -8 3 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 22859723
6485 395 47 None -8 3 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 22859723
CHEMBL1829173 395 47 None -8 3 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 22859723
1056 3369 116 None 15 10 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
2405 3369 116 None 15 10 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
77999 3369 116 None 15 10 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
CHEMBL121 3369 116 None 15 10 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
DB00412 3369 116 None 15 10 Human 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 12565875
1053 2480 0 None - 1 Human 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 15 2 2 5.9 OC(=O)CC(CCCCCCCCCCC(CC(=O)O)(C)C)(C)C 12565875
121871 2480 0 None - 1 Human 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 15 2 2 5.9 OC(=O)CC(CCCCCCCCCCC(CC(=O)O)(C)C)(C)C 12565875
CHEMBL63829 2480 0 None - 1 Human 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 15 2 2 5.9 OC(=O)CC(CCCCCCCCCCC(CC(=O)O)(C)C)(C)C 12565875
1057 1892 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 16702987
1057 1892 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 17200419
11692123 1892 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 16702987
11692123 1892 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 17200419
CHEMBL4303679 1892 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 16702987
CHEMBL4303679 1892 0 None - 1 Human 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 0 9 4.6 CCOc1ncc(cn1)Cc1cn(c2ccc(cc2)C(=O)OCC)c(nc1=O)SCc1ccc(cc1)F 17200419


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 Vendors

 Reference
ligand		 Fold
selectivity		 Tested
GPCRs		 Species

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

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
162673875 182984 0 None - 1 Mouse 9.4 pEC50 = 9.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182984 0 None - 1 Mouse 9.4 pEC50 = 9.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
52936292 182108 27 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
67087100 182596 0 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182596 0 None - 1 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182984 0 None - 1 Rat 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182984 0 None - 1 Rat 9.3 pEC50 = 9.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
67087041 182369 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 182369 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087100 182596 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182596 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087095 183373 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 183373 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194465 183304 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 183304 0 None - 1 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
134139282 146490 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(F)(F)F)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3922381 146490 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(F)(F)F)c2)cc1 10.1021/acsmedchemlett.6b00331
162668378 182505 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 182505 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
162674654 183453 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 183453 0 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
67087095 183373 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 183373 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145617 5 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087246 182875 5 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None - 1 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087041 182369 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 182369 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
52936292 182108 27 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
71257551 150591 24 None - 1 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3955132 150591 24 None - 1 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
162674654 183453 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 183453 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
162668378 182505 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 182505 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
68194465 183304 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 183304 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162668378 182505 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 182505 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
68194743 182546 12 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162674998 183389 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 183389 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183583 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183583 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
45254027 90303 10 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.2c00160
CHEMBL2385460 90303 10 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/acsmedchemlett.2c00160
67087246 182875 5 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
162674998 183389 0 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 183389 0 None - 1 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
162664735 182084 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 182084 0 None - 1 Mouse 8.9 pEC50 = 8.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
134136015 144205 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 475 12 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3904378 144205 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 475 12 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
46854655 395 47 None - 1 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None - 1 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None - 1 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
67087095 183373 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 183373 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194743 182546 12 None - 1 Rat 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None - 1 Rat 8.8 pEC50 = 8.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182984 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182984 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1622 72 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
6484 1622 72 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
CHEMBL1829174 1622 72 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
DB12491 1622 72 None 10 2 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
134134433 143231 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 510 12 1 5 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccncc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3896509 143231 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 510 12 1 5 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccncc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
134150797 151983 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 459 11 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3966739 151983 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 459 11 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
134137203 142837 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 523 12 1 5 5.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3893141 142837 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 523 12 1 5 5.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)C3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
162664735 182084 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 182084 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
68194159 183059 0 None - 1 Rat 7.0 pEC50 = 7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 183059 0 None - 1 Rat 7.0 pEC50 = 7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
67087160 182342 0 None - 1 Human 7.0 pEC50 = 7 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 182342 0 None - 1 Human 7.0 pEC50 = 7 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5271504 193685 0 None - 0 Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 544 13 1 7 5.0 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](OCCCOC)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5285139 194278 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.4 Cc1cc(OCc2nc(N)nc(NCCc3cc(Cl)ccc3Cl)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
11961321 111797 4 None - 0 Human 5.0 pEC50 = 5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111797 4 None - 0 Human 5.0 pEC50 = 5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
127033514 138778 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 381 6 1 5 4.6 Cc1nc(-c2ccccc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3780725 138778 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 381 6 1 5 4.6 Cc1nc(-c2ccccc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
46854655 395 47 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
6485 395 47 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
CHEMBL1829173 395 47 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml400501x
156010524 177114 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4cccc(C)c4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633625 177114 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4cccc(C)c4)cn3c2)cc1 10.1016/j.bmc.2020.115574
57705838 111242 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 508 10 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](F)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL3265139 111242 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 508 10 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](F)C(C)(C)C)c1 10.1021/ml4005123
58379987 90307 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 547 7 1 4 7.6 COc1cc(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml300427u
CHEMBL2385464 90307 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 547 7 1 4 7.6 COc1cc(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml300427u
127033821 138814 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3781162 138814 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
90655860 111247 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265144 111247 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 518 10 1 5 7.1 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
91809187 147122 13 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 147122 13 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
67087160 182342 0 None - 1 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 182342 0 None - 1 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182812 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182812 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
46854655 395 47 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
67087246 182875 5 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
46941175 61810 26 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL1773261 61810 26 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
58230598 183117 0 None - 1 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 183117 0 None - 1 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL5266348 193475 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 564 11 1 7 5.8 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](Oc5cccc(OC)c5)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1016/j.bmc.2023.117273
CHEMBL5267060 193507 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 473 7 1 6 4.7 COc1cc(N2CC[C@@H](Oc3ccc(N4CC[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
132606863 157821 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cellsPositive allosteric modulation of human GPR40 expressed in HEK293 cells
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 10.1016/j.bmc.2023.117273
CHEMBL4083365 157821 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cellsPositive allosteric modulation of human GPR40 expressed in HEK293 cells
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 10.1016/j.bmc.2023.117273
CHEMBL5290549 194499 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 436 8 2 7 3.3 Cc1cc(OCc2nc(N)nc(NCCc3ccccc3F)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5290651 194504 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 432 8 2 7 3.4 Cc1cc(OCc2nc(N)nc(NCCc3ccccc3C)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5277986 193959 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 438 6 2 7 4.2 Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3C)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
CHEMBL5281518 194112 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 409 5 2 8 3.8 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4cccc(Cl)c4)n3)ccc12 10.1021/acsmedchemlett.2c00160
155530111 171491 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4463798 171491 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
127036748 137515 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754173 137515 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
127029850 138736 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3780211 138736 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
57707214 111244 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 534 12 1 4 8.2 CCO[C@@H](c1cc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)ccc1-c1cc(OC)ccc1F)C(C)(C)C 10.1021/ml4005123
CHEMBL3265141 111244 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 534 12 1 4 8.2 CCO[C@@H](c1cc(COc2cccc([C@@H](CC(=O)O)C3CC3)c2)ccc1-c1cc(OC)ccc1F)C(C)(C)C 10.1021/ml4005123
1056 3369 116 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
2405 3369 116 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
77999 3369 116 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
CHEMBL121 3369 116 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
DB00412 3369 116 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1016/j.bmcl.2014.07.043
134138359 147619 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 419 10 2 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CNCc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3931296 147619 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 419 10 2 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CNCc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
15604310 111799 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287571 111799 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1 10.1021/ml400501x
134155821 150925 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 463 12 2 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCO)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3957744 150925 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 463 12 2 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCO)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
24857286 1622 72 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None 10 2 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
57705806 111212 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 515 10 1 4 7.6 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3264817 111212 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 515 10 1 4 7.6 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c(F)cn1 10.1021/ml4005123
162666840 182452 0 None - 1 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 182452 0 None - 1 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
132578495 182884 2 None - 1 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182884 2 None - 1 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
59132613 137260 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 483 8 1 4 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1nccs1 10.1016/j.bmcl.2015.11.050
CHEMBL3752026 137260 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 483 8 1 4 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1nccs1 10.1016/j.bmcl.2015.11.050
CHEMBL5284294 194247 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 556 11 1 8 5.0 COc1cc(N2CC[C@@H](Oc3ccc(N4C[C@H](OCCCC#N)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
CHEMBL5285235 194285 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 507 8 1 7 4.1 COc1cc(N2CC[C@@H](Oc3ccc(N4C[C@H](F)[C@@H](OC)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
CHEMBL5269688 193603 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.1 Cc1cc(OCc2nc(N)nc(NCCc3cccc(C(F)(F)F)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5278791 193994 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.1 Cc1cc(OCc2nc(N)nc(NCCc3ccccc3C(F)(F)F)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5288405 194421 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 448 9 2 8 3.1 COc1cccc(CCNc2nc(N)nc(COc3cc(C)cc(N4CCCC4=O)c3)n2)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5092999 215398 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
IPOne assayIPOne assay
ChEMBL None None None COCCCS(=O)(=O)c1cc(C)c(-c2ccc(F)c3c2CC[C@H]3Oc2ccc3c(c2)OC[C@H]3CC(=O)O)c(C)c1 10.6019/CHEMBL5058643
156021111 178050 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4647211 178050 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
59590781 111250 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265147 111250 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 8 1 4 7.4 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL5289774 194478 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 375 5 2 8 3.2 Cc1ccc(Nc2nc(N)nc(COc3ccc4ccc(=O)oc4c3)n2)cc1 10.1021/acsmedchemlett.2c00160
46854655 395 47 None - 1 Human 7.9 pEC50 = 7.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
6485 395 47 None - 1 Human 7.9 pEC50 = 7.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
CHEMBL1829173 395 47 None - 1 Human 7.9 pEC50 = 7.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
58758896 137550 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 480 8 1 4 6.3 Cn1ccnc1C(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754486 137550 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 480 8 1 4 6.3 Cn1ccnc1C(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL5276368 193894 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 510 7 1 5 5.5 COc1ccc(F)c(N2CC[C@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C[C@@H]2C)c1 10.1016/j.bmc.2023.117273
90176463 114259 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
CHEMBL3330549 114259 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
CHEMBL5285406 194295 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 417 5 2 9 3.2 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc5c(c4)COC5)n3)ccc12 10.1021/acsmedchemlett.2c00160
155523655 170901 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 357 7 1 5 3.8 Cc1nc(-c2ccccc2)oc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4454699 170901 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 357 7 1 5 3.8 Cc1nc(-c2ccccc2)oc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
134465785 176109 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4591657 176109 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
73356502 90311 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 486 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H]4C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385471 90311 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 486 8 1 3 7.5 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H]4C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
91809187 147122 13 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 147122 13 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL5285988 194323 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of mouse GPR40Positive allosteric modulation of mouse GPR40
ChEMBL 561 12 1 8 4.8 COCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
60195125 3886 8 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
9149 3886 8 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL2164242 3886 8 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL5290885 194515 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 423 5 2 8 4.2 Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
134134768 144325 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 516 11 1 5 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCN(C)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3905435 144325 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 516 11 1 5 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCN(C)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL5265829 193454 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 484 8 1 5 5.6 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4CC(C)(C)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
130253300 159109 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cellsPositive allosteric modulation of human GPR40 expressed in HEK293 cells
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1 10.1016/j.bmc.2023.117273
CHEMBL4097617 159109 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cellsPositive allosteric modulation of human GPR40 expressed in HEK293 cells
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1 10.1016/j.bmc.2023.117273
CHEMBL5273939 193785 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 466 8 2 7 4.1 Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)c(C)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
162644059 181822 0 None - 1 Rat 4.9 pEC50 = 4.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None - 1 Rat 4.9 pEC50 = 4.9 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
57706451 111246 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H](OC)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL3265143 111246 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H](OC)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL5278350 193975 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 442 6 2 7 4.0 Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3F)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
71816761 90308 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H]3[C@@H](C(=O)O)[C@@H]3C4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385466 90308 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H]3[C@@H](C(=O)O)[C@@H]3C4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
57706220 111243 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/ml4005123
CHEMBL3265140 111243 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 11 1 4 7.8 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@H](OC)C(C)(C)C)c1 10.1021/ml4005123
155563228 175304 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 441 7 1 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4573403 175304 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 441 7 1 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
118129974 157192 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 157192 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
90655861 111248 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265145 111248 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 506 10 1 5 7.1 CC[C@H](CC(=O)O)c1ccnc(OCc2ccc(-c3cc(OC)ncc3F)c([C@@H]3CCCC3(C)C)c2)c1 10.1021/ml4005123
58380381 90313 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385473 90313 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL5288340 194415 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 482 9 2 8 3.9 COC(CNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1)c1cccc(Cl)c1 10.1021/acsmedchemlett.2c00160
156017497 177854 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cccc(C)c4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4644239 177854 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cccc(C)c4)nc3c2)cc1 10.1016/j.bmc.2020.115574
46854655 395 47 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
6485 395 47 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL1829173 395 47 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
127029851 138860 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL3781779 138860 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
155547595 173663 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1ccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4534812 173663 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1ccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)cc1 10.1016/j.ejmech.2018.12.069
156013146 177465 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4OCC)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639050 177465 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4OCC)cn3c2)cc1 10.1016/j.bmc.2020.115574
162667620 182555 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 182555 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
134137248 143095 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 473 12 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3895442 143095 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 473 12 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC3CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
134138706 147896 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 551 11 1 6 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCS(=O)(=O)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3933446 147896 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 551 11 1 6 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCS(=O)(=O)CC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL5266881 193498 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 458 6 2 7 4.5 Cc1ccc(Nc2nc(N)nc(COc3cc(Cl)cc(N4CCCC4=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
CHEMBL5273250 193752 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 437 6 2 8 4.4 CCc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
58230552 182217 0 None - 1 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None - 1 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
57706778 80795 29 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2152070 80795 29 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL5282952 194176 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 530 13 1 7 4.7 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](OCCCOC)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1016/j.bmc.2023.117273
CHEMBL5268182 193548 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 454 8 2 7 3.4 Cc1cc(OCc2nc(N)nc(NCCc3cc(F)ccc3F)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5278391 193977 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.4 Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)c(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
57706778 80795 29 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
CHEMBL2152070 80795 29 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml4005123
86288852 111252 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265149 111252 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 522 11 1 6 6.6 COc1cc(-c2ccc(COc3cc([C@@H](CC(=O)O)C4CC4)ccn3)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
118151370 159101 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 159101 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
68194237 182204 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 182204 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182812 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182812 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
168298569 192677 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 389 5 2 8 3.5 Cc1cccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5219055 192677 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 389 5 2 8 3.5 Cc1cccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5284985 194272 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 389 5 2 8 3.5 Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1 10.1021/acsmedchemlett.2c00160
68194159 183059 0 None - 1 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 183059 0 None - 1 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
67087160 182342 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 182342 0 None - 1 Rat 7.8 pEC50 = 7.8 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5281753 194122 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of mouse GPR40Positive allosteric modulation of mouse GPR40
ChEMBL 558 13 1 7 5.2 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](OCCCOC)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
6483 3884 54 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
66553168 3884 54 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL2386353 3884 54 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
68265494 90310 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385470 90310 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL5275737 193867 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 486 9 1 6 4.6 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](OC)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5277523 193935 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 577 13 1 9 4.3 COCCOCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
CHEMBL5287383 194380 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 524 8 1 5 5.8 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5281423 194109 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 442 6 2 7 4.0 Cc1ccc(Nc2nc(N)nc(COc3cc(F)cc(N4CCCC4=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
CHEMBL5287642 194386 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 454 7 2 8 3.9 COc1cc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5285988 194323 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 561 12 1 8 4.8 COCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
CHEMBL5266810 193492 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 393 5 2 8 3.3 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(F)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
155525700 171038 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4456869 171038 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 391 7 1 5 4.4 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
46941175 61810 26 None - 1 Mouse 7.7 pEC50 = 7.7 Binding
Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretionActivation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
CHEMBL1773261 61810 26 None - 1 Mouse 7.7 pEC50 = 7.7 Binding
Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretionActivation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/ml100106c
75204006 114258 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330548 114258 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
68676271 137312 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccncc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752557 137312 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccncc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
127035472 137374 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 482 8 1 3 7.6 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccs1 10.1016/j.bmcl.2015.11.050
CHEMBL3753088 137374 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 482 8 1 3 7.6 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccs1 10.1016/j.bmcl.2015.11.050
CHEMBL5278354 193976 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 531 10 1 7 5.1 CCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
CHEMBL5282559 194157 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 559 12 1 7 5.9 CCCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
162649435 180038 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 288 6 1 2 3.7 Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4747554 180038 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 288 6 1 2 3.7 Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
67087173 182458 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 182458 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145617 5 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
134140466 146633 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3923431 146633 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 501 11 1 4 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
68194476 182885 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182885 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
162676686 183484 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 183484 0 None - 1 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183583 0 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183583 0 None - 1 Rat 8.7 pEC50 = 8.7 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134129919 142405 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 515 12 1 5 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3889768 142405 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 515 12 1 5 7.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
46854655 395 47 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acsmedchemlett.6b00331
6485 395 47 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acsmedchemlett.6b00331
CHEMBL1829173 395 47 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acsmedchemlett.6b00331
67087100 182596 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182596 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5268316 193557 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 438 6 2 7 4.2 Cc1cc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
90176463 114259 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
CHEMBL3330549 114259 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O 10.1021/ml5002757
134137874 152979 0 None - 0 Rat 4.7 pEC50 = 4.7 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152979 0 None - 0 Rat 4.7 pEC50 = 4.7 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152979 0 None - 0 Rat 4.7 pEC50 = 4.7 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL5283269 194194 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 502 9 2 8 4.0 Cc1cc(OCc2nc(N)nc(NCCc3ccccc3OC(F)(F)F)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5274344 193808 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 492 6 2 7 4.9 Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3C(F)(F)F)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
CHEMBL5269158 193591 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 454 7 2 8 3.9 COc1ccc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc1N1CCCC1=O 10.1021/acsmedchemlett.2c00160
162656082 180700 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 299 6 1 3 3.3 N#Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4755578 180700 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 299 6 1 3 3.3 N#Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL5288493 194428 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 403 5 2 8 3.8 Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1C 10.1021/acsmedchemlett.2c00160
75204360 157615 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
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 10.1016/j.bmc.2023.117273
CHEMBL4081072 157615 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
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 10.1016/j.bmc.2023.117273
132606863 157821 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
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 10.1016/j.bmc.2023.117273
CHEMBL4083365 157821 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
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 10.1016/j.bmc.2023.117273
127037633 137564 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754659 137564 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
58379893 90304 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385461 90304 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@H]2CCCC2(C)C)c1 10.1021/ml300427u
71816808 90312 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@]4(C)C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385472 90312 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@]4(C)C[C@H]4C(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
118129979 155792 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155792 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
6483 3884 54 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3884 54 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3884 54 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL5266488 193481 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 575 13 1 8 5.1 CCOCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
CHEMBL5275101 193836 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 500 9 1 6 5.0 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@](C)(OC)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
15603739 137569 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754682 137569 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL5275388 193849 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 415 5 2 8 3.7 Cc1ccc(Nc2nc(N)nc(COc3ccc4c5c(c(=O)oc4c3)CCC5)n2)cc1 10.1021/acsmedchemlett.2c00160
CHEMBL5278703 193988 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 438 6 2 7 4.3 Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCCC4=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
57705939 111245 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 532 10 1 4 7.9 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2OCCCC2(C)C)c1 10.1021/ml4005123
CHEMBL3265142 111245 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 532 10 1 4 7.9 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2OCCCC2(C)C)c1 10.1021/ml4005123
46854655 395 47 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmc.2016.09.004
6485 395 47 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmc.2016.09.004
CHEMBL1829173 395 47 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmc.2016.09.004
68194127 183193 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 183193 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5283315 194197 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 532 9 1 5 6.4 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](c5ccccc5)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
127035636 137273 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 490 9 1 6 4.7 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3S(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752168 137273 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 490 9 1 6 4.7 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3S(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2015.11.050
127036959 137417 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753362 137417 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
156017123 177741 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4OCC)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4642543 177741 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4OCC)nc3c2)cc1 10.1016/j.bmc.2020.115574
51049992 145617 5 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmc.2016.09.004
CHEMBL3915620 145617 5 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at FFA1 receptor (unknown origin)Agonist activity at FFA1 receptor (unknown origin)
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1016/j.bmc.2016.09.004
59590895 111253 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265150 111253 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 521 9 1 5 6.9 COc1cc(-c2ccc(COc3ccc4c(c3)[C@@](C)(CC(=O)O)CC4)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
67072752 86527 0 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL2315528 86527 0 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL5268389 193561 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 423 5 2 8 4.2 Cc1cc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)ccc1Cl 10.1021/acsmedchemlett.2c00160
127036959 137417 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753362 137417 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1C 10.1016/j.bmcl.2015.11.050
CHEMBL5274396 193812 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 599 11 1 7 6.1 COc1cc(N2CC[C@@H](Oc3ccc(N4C[C@H](OCCCC(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
CHEMBL5289929 194483 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 458 6 2 7 4.5 Cc1ccc(Nc2nc(N)nc(COc3ccc(Cl)c(N4CCCC4=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
155561358 175652 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1cccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4581313 175652 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 387 7 1 5 4.6 Cc1cccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)c1 10.1016/j.ejmech.2018.12.069
90655863 111251 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265148 111251 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 7 1 5 6.5 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
67087173 182458 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 182458 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
57393692 70025 11 None - 0 Human 7.6 pEC50 = 7.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL1939654 70025 11 None - 0 Human 7.6 pEC50 = 7.6 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 438 7 1 2 6.5 CC#CC(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
58380220 111254 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265151 111254 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 520 8 1 6 5.9 COc1cc(-c2ccc(COc3cc4c(cn3)CC[C@]43C[C@H]3C(=O)O)cc2[C@H](OC)C(C)(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL5281304 194107 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 522 10 1 6 5.2 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](OC(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5274496 193819 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 524 7 1 5 5.6 COc1ccc(F)c(N2C[C@@H](C)[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5267671 193533 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 446 8 2 7 3.7 Cc1cc(OCc2nc(N)nc(NCCc3c(C)cccc3C)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5287009 194369 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 418 8 2 7 3.1 Cc1cc(OCc2nc(N)nc(NCCc3ccccc3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
155569735 176674 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 371 7 1 4 4.9 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4535460 176674 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 371 7 1 4 4.9 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4598257 176674 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 371 7 1 4 4.9 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
145965707 164201 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4210871 164201 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
162676686 183484 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 183484 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
6483 3884 54 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3884 54 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3884 54 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albuminAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL5272492 193725 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 403 6 2 8 3.8 CCc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
24857286 1622 72 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
6484 1622 72 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
CHEMBL1829174 1622 72 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
DB12491 1622 72 None -10 2 Rat 4.6 pEC50 = 4.6 Binding
Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISAAgonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.6b00331
1050 1900 94 None 1 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
11595431 1900 94 None 1 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
CHEMBL207881 1900 94 None 1 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
90655862 111249 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3265146 111249 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 492 9 1 5 6.7 COc1cc(-c2ccc(COc3cc([C@H](C)CC(=O)O)ccn3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
156635003 180934 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 394 3 2 3 3.9 Nc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
CHEMBL4758125 180934 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 394 3 2 3 3.9 Nc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
11961321 111797 4 None - 0 Crab-eating macaque 7.5 pEC50 = 7.5 Binding
Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111797 4 None - 0 Crab-eating macaque 7.5 pEC50 = 7.5 Binding
Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837Agonist activity at cynomolgus monkey GPR40 in presence of 0.01% human serum albumin relative to AMG 837
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL5283236 194191 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 491 7 1 6 4.7 COc1cc(N2CC[C@@H](Oc3ccc(N4C[C@H](F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
134139990 146326 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)=O)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3921143 146326 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)=O)c2)cc1 10.1021/acsmedchemlett.6b00331
75204006 114258 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330548 114258 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL5282578 194160 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 552 9 1 5 6.4 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](C(C)C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5279836 194038 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 417 7 2 8 4.1 CCCc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
127035669 137315 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752601 137315 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
71257551 150591 24 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3955132 150591 24 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
162664735 182084 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 182084 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5075693 214388 3 None - 1 Human 8.5 pEC50 = 8.5 Binding
IPOne assayIPOne assay
ChEMBL None None None Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Oc1ccc2c(c1)OC[C@H]2CC(=O)O 10.6019/CHEMBL5058643
46854655 395 47 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
51357276 182005 0 None - 1 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None - 1 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087041 182369 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 182369 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162674654 183453 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 183453 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
134465794 171076 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
CHEMBL4457303 171076 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assayAgonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
ChEMBL 458 9 1 3 6.5 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@H](C4CC4)[C@@](C)(F)C(=O)O)c3)CC2)c1 10.1021/acsmedchemlett.8b00444
68194237 182204 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 182204 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194449 182812 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182812 0 None - 1 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
68194465 183304 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 183304 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
118129999 157765 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157765 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL5277813 193950 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 541 7 1 6 5.5 COc1cc(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
90159227 158065 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 514 7 1 4 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1016/j.bmc.2023.117273
CHEMBL4086198 158065 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 514 7 1 4 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(C(F)(F)F)[C@@H](C)[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1016/j.bmc.2023.117273
CHEMBL5275546 193859 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 454 8 2 7 3.4 Cc1cc(OCc2nc(N)nc(NCCc3c(F)cccc3F)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5278836 193997 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 452 8 2 7 3.8 Cc1cc(OCc2nc(N)nc(NCCc3cccc(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5280494 194068 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 450 8 2 7 3.6 Cc1cc(OCc2nc(N)nc(NCCc3cc(C)ccc3F)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5282108 194143 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.4 Cc1cc(OCc2nc(N)nc(NCCc3cccc(Cl)c3Cl)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
90655859 111213 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cncc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
CHEMBL3264818 111213 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cncc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
127036829 137305 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752487 137305 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
118129981 159465 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 159465 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
162645828 179661 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 352 6 1 2 4.2 O=C(O)CCc1ccc(COc2cc(F)ccc2Br)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4743323 179661 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 352 6 1 2 4.2 O=C(O)CCc1ccc(COc2cc(F)ccc2Br)cc1 10.1016/j.bmcl.2020.127650
162652317 180319 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 304 7 1 3 3.4 COc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4751137 180319 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 304 7 1 3 3.4 COc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 10.1016/j.bmcl.2020.127650
CHEMBL5284113 194242 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 575 12 1 8 5.1 COCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)C1(C)C 10.1016/j.bmc.2023.117273
156013152 177476 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639182 177476 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
1050 1900 94 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.07.043
11595431 1900 94 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.07.043
CHEMBL207881 1900 94 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationAgonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2014.07.043
CHEMBL5289099 194458 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 425 6 2 8 4.1 Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C(F)F)cc(=O)oc4c3)n2)cc1 10.1021/acsmedchemlett.2c00160
CHEMBL5286632 194351 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 492 6 2 7 4.9 Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)cc(C(F)(F)F)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
58230552 182217 0 None - 1 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None - 1 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
132606864 157744 0 None - 1 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157744 0 None - 1 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL5284884 194267 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 544 9 2 7 5.8 Cc1cc(OCc2nc(N)nc(NCCc3cccc(S(F)(F)(F)(F)F)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
6483 3884 54 None - 1 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
66553168 3884 54 None - 1 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL2386353 3884 54 None - 1 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/ml4000673
CHEMBL5267399 193525 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 409 5 2 8 3.8 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(Cl)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
9823501 100205 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 4 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL288341 100205 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 4 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4445519 100205 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 421 7 1 4 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
11961321 111797 4 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287569 111797 4 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1021/ml400501x
15603842 111798 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
CHEMBL3287570 111798 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1 10.1021/ml400501x
11961321 111797 4 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111797 4 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
132606863 157821 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4083365 157821 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assayAgonist activity at GPR40 in mouse STC1 cells assessed as induction of GLP-1 secretion measured after 1 hr by HTRF assay
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
68674201 137287 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 476 8 1 2 7.6 O=C(O)CC(c1ccccc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752303 137287 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 476 8 1 2 7.6 O=C(O)CC(c1ccccc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
127035471 137489 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1ccccn1 10.1016/j.bmcl.2015.11.050
CHEMBL3753980 137489 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1ccccn1 10.1016/j.bmcl.2015.11.050
CHEMBL5281020 194094 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 442 6 2 7 4.0 Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3F)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
57522038 3885 60 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmcl.2020.127650
6490 3885 60 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmcl.2020.127650
CHEMBL2058533 3885 60 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 364 7 1 2 5.4 OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C 10.1016/j.bmcl.2020.127650
58230552 182217 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL5287358 194379 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 448 9 2 8 3.1 COc1ccccc1CCNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1 10.1021/acsmedchemlett.2c00160
67361692 90296 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 540 7 1 3 8.4 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385303 90296 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 540 7 1 3 8.4 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
24857286 1622 72 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None -10 2 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
90644561 111796 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 418 7 1 2 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3C)c2)cc1 10.1021/ml400501x
CHEMBL3287568 111796 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 418 7 1 2 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3C)c2)cc1 10.1021/ml400501x
24897670 111802 23 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
CHEMBL3287574 111802 23 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ccon2)cc1 10.1021/ml400501x
162667620 182555 0 None - 1 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 182555 0 None - 1 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
127036828 137435 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753533 137435 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
76900387 157543 6 None - 0 Human 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
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 10.1016/j.bmc.2023.117273
CHEMBL4080226 157543 6 None - 0 Human 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulationPositive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as cAMP accumulation
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 10.1016/j.bmc.2023.117273
90158812 114257 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
CHEMBL3330547 114257 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
57706032 111241 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 460 10 1 3 7.6 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265138 111241 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 460 10 1 3 7.6 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)c3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
145965467 164164 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4210415 164164 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 403 7 1 6 3.6 Cc1nc(-c2ccccc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL5275951 193877 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 524 7 1 5 5.8 COc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)C(C)(C)C2)c1 10.1016/j.bmc.2023.117273
90655858 111240 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)n3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
CHEMBL3265137 111240 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 461 10 1 4 7.0 CCC[C@H](CC(=O)O)c1cccc(OCc2ccc(-c3cccc(OC)n3)c(C(C)(C)C)c2)c1 10.1021/ml4005123
155512244 169627 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 373 7 1 5 4.3 Cc1nc(-c2ccccc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
CHEMBL4436948 169627 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 373 7 1 5 4.3 Cc1nc(-c2ccccc2)sc1COc1ccc(OCC(=O)O)c(F)c1 10.1016/j.ejmech.2018.12.069
70901463 90309 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385467 90309 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 512 7 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@]3(CC4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
134136203 142969 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 433 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(C)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3894356 142969 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 433 10 1 4 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(C)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
162644059 181822 0 None - 1 Mouse 5.4 pEC50 = 5.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None - 1 Mouse 5.4 pEC50 = 5.4 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
156020437 178146 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4648853 178146 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4C)cn3c2)cc1 10.1016/j.bmc.2020.115574
67072752 86527 0 None - 1 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse FFA1Agonist activity at mouse FFA1
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
CHEMBL2315528 86527 0 None - 1 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse FFA1Agonist activity at mouse FFA1
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/jm301470a
89671280 146686 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmc.2017.03.001
CHEMBL3923877 146686 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
ChEMBL 406 5 3 3 4.1 CC#C[C@@H](CC(=O)O)c1ccc(NC(=O)C(=O)Nc2cccc(C(C)(C)C)c2)cc1 10.1016/j.bmc.2017.03.001
68194476 182885 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182885 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
134140675 146777 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 509 12 1 4 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccccc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3924534 146777 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 509 12 1 4 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccccc3)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
162676686 183484 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 183484 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
67087173 182458 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 182458 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
134147518 150115 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 487 11 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3951157 150115 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 487 11 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
59132740 137368 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccnc1 10.1016/j.bmcl.2015.11.050
CHEMBL3753057 137368 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysisPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis
ChEMBL 477 8 1 3 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccnc1 10.1016/j.bmcl.2015.11.050
CHEMBL5266730 193488 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.4 Cc1cc(OCc2nc(N)nc(NCCc3cc(Cl)cc(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
15602772 111801 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
CHEMBL3287573 111801 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 503 8 1 8 4.8 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nnnn2C)cc1 10.1021/ml400501x
127035638 137467 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753790 137467 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL5290988 194516 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation of human GPR40 expressed in HEK293 cellsPositive allosteric modulation of human GPR40 expressed in HEK293 cells
ChEMBL 428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@H]4CC(=O)O)cc3)CC2)c1 10.1016/j.bmc.2023.117273
156010854 177117 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C5CCCCC5)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633642 177117 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C5CCCCC5)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL5283217 194189 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 449 6 2 8 3.7 Cc1ccc(Nc2nc(N)nc(COc3cc(C#N)cc(N4CCCC4=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
162666840 182452 0 None - 1 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 182452 0 None - 1 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
127036828 137435 0 None - 0 Human 4.4 pEC50 = 4.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753533 137435 0 None - 0 Human 4.4 pEC50 = 4.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 444 8 1 4 5.7 Cc1ccc(F)cc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
127035667 137284 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752274 137284 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
127037608 137397 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753265 137397 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL5268183 193549 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 538 9 1 5 6.1 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](CC)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5280786 194081 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 566 10 1 5 6.8 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](CC(C)C)C2)c1 10.1016/j.bmc.2023.117273
127036747 137567 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754670 137567 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1ccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL5285104 194277 0 None - 0 Human 4.4 pEC50 = 4.4 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 486 8 2 7 4.4 Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)cc3Cl)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
118129979 155792 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155792 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
24857286 1622 72 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
6484 1622 72 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
CHEMBL1829174 1622 72 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
DB12491 1622 72 None 10 2 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.ejmech.2018.12.069
CHEMBL5268798 193576 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 534 10 1 6 5.8 CCOc1ccc(F)c(N2CCC(Oc3ccc(N4C[C@H](Oc5ccccc5)C[C@@H]4CC(=O)O)cc3)CC2)c1 10.1016/j.bmc.2023.117273
156016183 177666 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4641652 177666 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL5276740 193911 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 417 6 2 8 4.3 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C(C)C)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
156013404 177457 3 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4638956 177457 3 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 440 8 1 5 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
1050 1900 94 None 1 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.0c01002
11595431 1900 94 None 1 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.0c01002
CHEMBL207881 1900 94 None 1 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.0c01002
127035668 137337 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752807 137337 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL5283236 194191 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of mouse GPR40Positive allosteric modulation of mouse GPR40
ChEMBL 491 7 1 6 4.7 COc1cc(N2CC[C@@H](Oc3ccc(N4C[C@H](F)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c(Cl)cn1 10.1016/j.bmc.2023.117273
CHEMBL5273852 193780 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 478 8 2 7 4.3 Cc1cc(OCc2nc(N)nc(NCC3(c4cccc(Cl)c4)CC3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
837245 10597 46 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 315 3 1 2 3.8 Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
CHEMBL1170012 10597 46 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 315 3 1 2 3.8 Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
CHEMBL5285988 194323 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 561 12 1 8 4.8 COCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
156019672 177988 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(CC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4646212 177988 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(CC)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
52936292 182108 27 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
51357276 182005 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162667620 182555 0 None - 1 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 182555 0 None - 1 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL5271268 193675 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at FFAR1 (unknown origin) incubated for 16 hrs by Promoter-luciferase assayAgonist activity at FFAR1 (unknown origin) incubated for 16 hrs by Promoter-luciferase assay
ChEMBL 470 9 1 5 5.3 CC#CC(CC(=O)O)c1ccc(OCc2cccc(CN3CCc4oc(C5CC5)nc4C3)c2)cc1 10.1016/j.ejmech.2018.04.061
44223813 90316 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.8 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H](CC(=O)O)CC4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385476 90316 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 500 8 1 3 7.8 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@@H](CC(=O)O)CC4)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL5266523 193483 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 484 10 2 8 3.7 Cc1cc(OCc2nc(N)nc(NCCc3cccc(OC(F)F)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5267225 193511 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 436 8 2 7 3.3 Cc1cc(OCc2nc(N)nc(NCCc3cccc(F)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
156013456 177473 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639121 177473 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 7 1 4 5.8 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4C)nc3c2)cc1 10.1016/j.bmc.2020.115574
156019224 177969 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4645989 177969 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL5281753 194122 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 558 13 1 7 5.2 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](OCCCOC)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
67359903 90314 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385474 90314 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 526 7 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)CC[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
68194159 183059 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 183059 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
156012263 177292 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4636540 177292 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
24857286 1622 72 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
6484 1622 72 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
CHEMBL1829174 1622 72 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
DB12491 1622 72 None 10 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmc.2020.115574
3367 1155 1 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
46216676 1155 1 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
CHEMBL604126 1155 1 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
58230598 183117 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 183117 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
132578495 182884 2 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182884 2 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5283683 194223 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 482 9 2 8 3.8 COc1ccc(Cl)cc1CCNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1 10.1021/acsmedchemlett.2c00160
561372 58825 65 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL1688452 58825 65 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
156014759 177250 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(F)(F)F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4635975 177250 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(F)(F)F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
156011495 177352 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C5CCCCC5)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4637557 177352 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 492 8 1 4 7.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C5CCCCC5)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
51357276 182005 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
90158812 114257 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
CHEMBL3330547 114257 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 335 5 1 5 3.7 Cc1ccccc1Oc1ccc(N2N=C(C#N)CC2CC(=O)O)cc1 10.1021/ml5002757
127035667 137284 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752274 137284 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 446 8 1 4 5.9 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
118129998 157321 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 157321 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
162673626 183191 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 350 3 2 3 3.7 Nc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
CHEMBL4795755 183191 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 350 3 2 3 3.7 Nc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)cc1C(F)(F)F 10.1016/j.bmcl.2020.127650
90644562 111804 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
CHEMBL3287576 111804 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2cnco2)cc1 10.1021/ml400501x
68194237 182204 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 182204 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
127035669 137315 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752601 137315 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 440 8 1 4 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL5269274 193594 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 500 9 1 6 4.8 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](OC)[C@@H](C)[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5289252 194461 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 510 7 1 5 5.4 COc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c1 10.1016/j.bmc.2023.117273
156013517 177508 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4639658 177508 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
127037633 137564 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754659 137564 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 444 8 1 4 5.7 Cc1cc(F)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
155569722 176256 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 353 7 1 4 4.7 Cc1nc(-c2ccccc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4528449 176256 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 353 7 1 4 4.7 Cc1nc(-c2ccccc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL4594952 176256 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 353 7 1 4 4.7 Cc1nc(-c2ccccc2)sc1COc1ccc(CCC(=O)O)cc1 10.1016/j.ejmech.2018.12.069
156021563 178023 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells incubated for 1 hrs by calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells incubated for 1 hrs by calcium flux assay
ChEMBL 534 12 1 6 6.2 COc1ccc(F)c(-c2ncc(COc3ccc([C@@H](CC(=O)O)C4CC4)cc3)nc2OCCC(F)(F)F)c1 10.1016/j.ejmech.2018.04.061
CHEMBL4646784 178023 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells incubated for 1 hrs by calcium flux assayAgonist activity at human GPR40 expressed in HEK293 cells incubated for 1 hrs by calcium flux assay
ChEMBL 534 12 1 6 6.2 COc1ccc(F)c(-c2ncc(COc3ccc([C@@H](CC(=O)O)C4CC4)cc3)nc2OCCC(F)(F)F)c1 10.1016/j.ejmech.2018.04.061
73891117 114261 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330550 114261 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
132578495 182884 2 None - 1 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182884 2 None - 1 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
46854655 395 47 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300427u
6485 395 47 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300427u
CHEMBL1829173 395 47 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/ml300427u
CHEMBL5286544 194348 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 457 5 2 8 4.8 Cc1c(Cl)cc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
162644059 181822 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL5268800 193577 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 452 8 2 7 3.8 Cc1cc(OCc2nc(N)nc(NCCc3ccccc3Cl)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5283726 194225 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 466 8 2 7 4.3 Cc1cc(OCc2nc(N)nc(NCC(C)c3cccc(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
15603739 137569 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754682 137569 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1c(Cl)cccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
67072752 86527 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL2315528 86527 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL5271725 193692 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 478 8 2 7 4.3 Cc1cc(OCc2nc(N)nc(NC3(Cc4cccc(Cl)c4)CC3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
127036748 137515 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3754173 137515 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2015.11.050
156019823 177937 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(C)C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4645557 177937 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 452 8 1 4 6.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(C)C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
156016011 177605 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4640818 177605 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
68194476 182885 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182885 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
137633536 156293 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
Agonist activity at mouse FFA1 receptorAgonist activity at mouse FFA1 receptor
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
CHEMBL4065397 156293 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
Agonist activity at mouse FFA1 receptorAgonist activity at mouse FFA1 receptor
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
156010092 177105 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633473 177105 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL5290818 194510 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 545 11 1 7 5.5 CCCCO[C@H]1CN(c2ccc(O[C@@H]3CCN(c4cc(OC)ncc4Cl)C[C@H]3C)cc2)[C@@H](CC(=O)O)[C@@H]1C 10.1016/j.bmc.2023.117273
156019930 177960 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cc(F)ccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4645938 177960 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cc(F)ccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
11961321 111797 4 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Agonist activity at rat GPR40 in presence of 0.01% human serum albuminAgonist activity at rat GPR40 in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3287569 111797 4 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Agonist activity at rat GPR40 in presence of 0.01% human serum albuminAgonist activity at rat GPR40 in presence of 0.01% human serum albumin
ChEMBL 460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
73891117 114261 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
CHEMBL3330550 114261 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Modulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assayModulation activity at human GPR40 expressed in HEK293 cells by IP-1 detection based HTRF assay
ChEMBL 522 8 1 4 7.1 COc1ccc(F)c(-c2ccc(Cc3ccc(N4N=C(c5ccccc5)C(C)C4CC(=O)O)cc3)c(C)c2)c1 10.1021/ml5002757
23083113 177450 6 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 306 6 1 2 4.4 O=C(O)CCc1ccc(OCc2cccc3ccccc23)cc1 10.1016/j.bmc.2019.115263
CHEMBL4638816 177450 6 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 306 6 1 2 4.4 O=C(O)CCc1ccc(OCc2cccc3ccccc23)cc1 10.1016/j.bmc.2019.115263
15603947 111800 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 502 8 1 7 5.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncnn2C)cc1 10.1021/ml400501x
CHEMBL3287572 111800 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 502 8 1 7 5.5 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncnn2C)cc1 10.1021/ml400501x
8852666 192680 26 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1021/acsmedchemlett.2c00160
CHEMBL5219102 192680 26 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1021/acsmedchemlett.2c00160
127035668 137337 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3752807 137337 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 440 9 1 4 5.8 CCc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
118129999 157765 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157765 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
25150014 3883 55 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
3952 3883 55 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
CHEMBL449588 3883 55 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
156017576 177837 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(CC)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4644067 177837 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 438 8 1 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(CC)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
156021586 178078 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(F)(F)F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4647663 178078 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 478 7 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(C(F)(F)F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
162674533 183463 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 372 3 2 3 4.4 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
CHEMBL4799103 183463 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assayAgonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay
ChEMBL 372 3 2 3 4.4 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2020.127650
57706227 111210 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 10 1 4 7.7 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3264815 111210 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 517 10 1 4 7.7 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
155565451 175593 11 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL4579901 175593 11 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OC[C@H]2CC(=O)O 10.1016/j.ejmech.2018.12.069
118129981 159465 0 None - 1 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 159465 0 None - 1 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
162666840 182452 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 182452 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
118129998 157321 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 157321 0 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at human PK-tagged GPR40 expressed in HEK293 cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
15604434 111803 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncco2)cc1 10.1021/ml400501x
CHEMBL3287575 111803 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 488 8 1 6 6.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2ncco2)cc1 10.1021/ml400501x
127036829 137305 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3752487 137305 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 480 8 1 4 6.6 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(Cl)cc3Cl)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL5268534 193567 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 510 7 1 5 5.4 COc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](C)C2)c1 10.1016/j.bmc.2023.117273
67072752 86527 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
CHEMBL2315528 86527 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assayAgonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/ml4000673
127035637 137253 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 437 8 1 5 5.1 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3C#N)c2)cc1 10.1016/j.bmcl.2015.11.050
CHEMBL3751968 137253 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 437 8 1 5 5.1 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3C#N)c2)cc1 10.1016/j.bmcl.2015.11.050
134139119 145984 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 511 12 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)CC)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3918387 145984 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 511 12 1 5 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)CC)c2)cc1 10.1021/acsmedchemlett.6b00331
71257551 150591 24 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3955132 150591 24 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.6b00892
68194127 183193 0 None - 1 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 183193 0 None - 1 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1622 72 None 10 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.2c00160
6484 1622 72 None 10 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.2c00160
CHEMBL1829174 1622 72 None 10 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.2c00160
DB12491 1622 72 None 10 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at FFAR1 (unknown origin)Agonist activity at FFAR1 (unknown origin)
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acsmedchemlett.2c00160
134142245 145498 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 503 11 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCOCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3914686 145498 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 503 11 1 5 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCOCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
134142149 145466 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 519 11 1 5 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCSCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3914418 145466 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 519 11 1 5 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCSCC3)c2)cc1 10.1021/acsmedchemlett.6b00331
68194743 182546 12 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL5267168 193509 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 415 6 2 8 4.1 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C5CC5)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
CHEMBL5283407 194204 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 425 5 2 8 4.3 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc5ccccc5c4)n3)ccc12 10.1021/acsmedchemlett.2c00160
CHEMBL5279649 194031 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 432 8 2 7 3.4 Cc1cccc(CCNc2nc(N)nc(COc3cc(C)cc(N4CCCC4=O)c3)n2)c1 10.1021/acsmedchemlett.2c00160
CHEMBL5289306 194462 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 466 8 2 7 4.1 Cc1cc(OCc2nc(N)nc(NCCc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
156016727 177716 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4642297 177716 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL5280836 194085 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR40 expressed in HEK293 cells incubated for 18 to 24 hrs by HTRF assayAgonist activity at human GPR40 expressed in HEK293 cells incubated for 18 to 24 hrs by HTRF assay
ChEMBL 541 7 2 8 3.9 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)[C@H](N)C2)c(Cl)cn1 10.1016/j.ejmech.2018.04.061
156016929 177723 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Modulation of GPR40 (unknown origin)Modulation of GPR40 (unknown origin)
ChEMBL 540 7 1 7 5.3 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)C(C)C2)c(Cl)cn1 10.1016/j.bmc.2019.115263
CHEMBL4642324 177723 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Modulation of GPR40 (unknown origin)Modulation of GPR40 (unknown origin)
ChEMBL 540 7 1 7 5.3 COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)C(C)C2)c(Cl)cn1 10.1016/j.bmc.2019.115263
CHEMBL5285725 194309 0 None - 0 Human 4.2 pEC50 = 4.2 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 446 8 2 7 3.7 Cc1cc(OCc2nc(N)nc(NCCc3ccc(C)cc3C)n2)cc(N2CCCC2=O)c1 10.1021/acsmedchemlett.2c00160
15603946 111656 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
CHEMBL3286409 111656 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
ChEMBL 501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1 10.1021/ml400501x
58230598 183117 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 183117 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL5267340 193519 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 600 10 1 5 7.0 CCOc1ccc(F)c(N2CC[C@@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@H](Cc3ccccc3)C2)c1 10.1016/j.bmc.2023.117273
CHEMBL5286962 194364 0 None - 0 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 438 6 2 7 4.2 Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3C)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
23136411 58830 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2019.115263
CHEMBL1688457 58830 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2019.115263
127035639 137553 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1cccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3754524 137553 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 442 9 1 5 5.3 COc1cccc(-c2cccc(COc3ccc([C@H](CC(=O)O)c4nccn4C)cc3)c2)c1 10.1016/j.bmcl.2015.11.050
57705880 111211 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml4005123
CHEMBL3264816 111211 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml4005123
71575419 89970 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
CHEMBL2381282 89970 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3 10.1016/j.bmcl.2013.03.060
8852666 192680 26 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of GPR40 (unknown origin)Positive allosteric modulation of GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
CHEMBL5219102 192680 26 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of GPR40 (unknown origin)Positive allosteric modulation of GPR40 (unknown origin)
ChEMBL 389 5 2 8 3.5 Cc1ccccc1Nc1nc(N)nc(COc2ccc3c(C)cc(=O)oc3c2)n1 10.1016/j.ejmech.2022.114645
CHEMBL5278642 193986 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 443 5 2 8 4.5 Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(Cl)c(Cl)c4)n3)ccc12 10.1021/acsmedchemlett.2c00160
CHEMBL5268155 193547 0 None - 0 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 407 6 2 8 3.2 Cc1cc(=O)oc2cc(OCc3nc(N)nc(NCc4ccc(F)cc4)n3)ccc12 10.1021/acsmedchemlett.2c00160
156011880 177328 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4637214 177328 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 428 7 1 4 5.3 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4)nc3c2)cc1 10.1016/j.bmc.2020.115574
127034370 138839 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
CHEMBL3781477 138839 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 399 6 1 5 4.8 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O 10.1016/j.ejmech.2018.12.069
57705648 90315 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 474 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385475 90315 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 474 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
156016232 177770 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4642960 177770 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccc(F)cc4F)nc3c2)cc1 10.1016/j.bmc.2020.115574
3893 2285 98 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
4642 2285 98 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
5534 2285 98 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL108766 2285 98 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
DB03017 2285 98 None - 1 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 200 10 1 1 4.0 CCCCCCCCCCCC(=O)O 10.1021/acs.jmedchem.6b00202
156009878 177122 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 281 6 1 3 3.2 N#Cc1ccccc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmc.2019.115263
CHEMBL4633698 177122 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 281 6 1 3 3.2 N#Cc1ccccc1COc1ccc(CCC(=O)O)cc1 10.1016/j.bmc.2019.115263
162676881 183583 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183583 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1622 72 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None - 2 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
134143418 145331 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 477 13 1 5 5.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCOC)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3913383 145331 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 477 13 1 5 5.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCOC)Cc3ccsc3)c2)cc1 10.1021/acsmedchemlett.6b00331
134137874 152979 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3930086 152979 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
CHEMBL3975239 152979 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assayAgonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
ChEMBL 461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1 10.1021/acsmedchemlett.6b00331
51049992 145617 5 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
46854655 395 47 None - 1 Human 7.1 pEC50 = 7.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
6485 395 47 None - 1 Human 7.1 pEC50 = 7.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
CHEMBL1829173 395 47 None - 1 Human 7.1 pEC50 = 7.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
45254027 90303 10 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385460 90303 10 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 514 7 1 3 7.7 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL5278718 193990 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 424 6 2 7 3.9 Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
58380284 90301 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(C4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385459 90301 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 498 7 1 3 7.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(C4)C[C@H]3C(=O)O)cc2C2=CCCC2(C)C)c1 10.1021/ml300427u
156021515 178136 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4648621 178136 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 446 7 1 4 5.4 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(F)cc4F)cn3c2)cc1 10.1016/j.bmc.2020.115574
68194127 183193 0 None - 1 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 183193 0 None - 1 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57706902 111208 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 490 10 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2CC(C)(C)C)c1 10.1021/ml4005123
CHEMBL3264813 111208 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 490 10 1 3 7.6 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2CC(C)(C)C)c1 10.1021/ml4005123
46854655 395 47 None - 1 Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
6485 395 47 None - 1 Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
CHEMBL1829173 395 47 None - 1 Human 5.1 pEC50 = 5.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1016/j.bmcl.2015.11.050
127037608 137397 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
CHEMBL3753265 137397 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 426 8 1 4 5.6 Cc1ccccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1 10.1016/j.bmcl.2015.11.050
162674998 183389 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 183389 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1622 72 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
6484 1622 72 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL1829174 1622 72 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
DB12491 1622 72 None 10 2 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assayAgonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
58380255 90305 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 528 7 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385462 90305 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 528 7 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
57707110 111209 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 535 10 1 4 7.9 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
CHEMBL3264814 111209 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albuminAgonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin
ChEMBL 535 10 1 4 7.9 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3F)cc2[C@@H]2CCCC2(C)C)c(F)cn1 10.1021/ml4005123
24857286 1622 72 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
6484 1622 72 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
CHEMBL1829174 1622 72 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
DB12491 1622 72 None -10 2 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretionAgonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1016/j.bmcl.2013.03.060
127033818 138745 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
CHEMBL3780334 138745 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay
ChEMBL 395 6 1 5 5.0 Cc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1 10.1016/j.ejmech.2018.12.069
118129974 157192 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 157192 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
127036960 137387 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753188 137387 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albuminPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
CHEMBL5274923 193828 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysisAgonist activity at N-terminal FLAG tagged human FFAR1 transfected in African green monkey COS-7 cells assessed as accumulation of inositol phosphate incubated for 90 mins by TopCount NXT counter based analysis
ChEMBL 460 6 2 8 3.3 Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCS4(=O)=O)c3)n2)cc1Cl 10.1021/acsmedchemlett.2c00160
156009978 177096 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
CHEMBL4633252 177096 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
ChEMBL 410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4)cn3c2)cc1 10.1016/j.bmc.2020.115574
58379717 90306 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 546 7 1 3 8.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
CHEMBL2385463 90306 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assayAgonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay
ChEMBL 546 7 1 3 8.2 COc1ccc(F)c(-c2ccc(COc3ccc4c(c3F)[C@]3(CCC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1 10.1021/ml300427u
118151370 159101 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 159101 0 None - 1 Rat 7.0 pEC50 = 7.0 Binding
Agonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assayAgonist activity at rat PK-tagged GPR40 expressed in human U2OS cells assessed as EA-tagged beta-arrestin recruitment after 90 mins in presence of 1 % heat inactivated FBS by beta-galactosidase reporter gene assay
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL5274742 193824 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human GPR40 by calcium based FLIPR analysisPositive allosteric modulation of human GPR40 by calcium based FLIPR analysis
ChEMBL 524 7 1 5 5.6 COc1ccc(F)c(N2C[C@@H](C)[C@H](Oc3ccc(N4C[C@H](C(F)(F)F)C[C@@H]4CC(=O)O)cc3)[C@@H](C)C2)c1 10.1016/j.bmc.2023.117273
127036960 137387 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
CHEMBL3753188 137387 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serumPartial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
ChEMBL 474 8 1 4 6.5 Cc1cc(Cl)ccc1-c1cc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)ccc1C 10.1016/j.bmcl.2015.11.050
54580627 62165 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777875 62165 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
53248846 62151 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777861 62151 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 414 7 1 3 5.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1 10.1016/j.bmcl.2011.03.114
54582629 62154 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777864 62154 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
54584572 62168 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777878 62168 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
53248848 62166 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777876 62166 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
127040096 136610 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
CHEMBL3739712 136610 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 331 4 0 4 3.8 Cc1cc(COc2ccc(F)c(F)c2F)nc(-c2ccccn2)n1 10.1039/C5MD00037H
54586485 62155 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777865 62155 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
54586484 62152 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777862 62152 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 339 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
54583582 62162 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777872 62162 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1 10.1016/j.bmcl.2011.03.114
54584571 62167 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777877 62167 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 455 6 1 5 4.8 CC#C[C@H](c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)[C@H]1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
54583581 62158 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777868 62158 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1 10.1016/j.bmcl.2011.03.114
54582630 62156 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777866 62156 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1 10.1016/j.bmcl.2011.03.114
127041988 136832 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
CHEMBL3741735 136832 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 421 7 0 6 3.7 Fc1ccc(OCc2cc(OCC3(F)COC3)nc(-c3ccccn3)n2)c(F)c1F 10.1039/C5MD00037H
54580625 62163 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777873 62163 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1 10.1016/j.bmcl.2011.03.114
54581633 62159 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777869 62159 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1 10.1016/j.bmcl.2011.03.114
54580626 62164 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
CHEMBL1777874 62164 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 394 4 1 2 5.5 CC#C[C@]1(c2ccc(Oc3ccc(C(F)(F)F)cc3Cl)cc2)C[C@@H]1C(=O)O 10.1016/j.bmcl.2011.03.114
54582628 62153 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777863 62153 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 383 5 1 3 4.7 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)cc2Br)cc1 10.1016/j.bmcl.2011.03.114
54580624 62150 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777860 62150 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1 10.1016/j.bmcl.2011.03.114
54586486 62160 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777870 62160 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 320 5 1 2 4.3 CC#CC(CC(=O)O)c1ccc(O[C@@H]2CCc3ccccc32)cc1 10.1016/j.bmcl.2011.03.114
54582631 62157 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
CHEMBL1777867 62157 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2011.03.114
54585512 62161 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
CHEMBL1777871 62161 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 335 5 1 4 3.0 CC#CC(c1ccc(OCc2ccccc2)cc1)C1OC(=O)NC1=O 10.1016/j.bmcl.2011.03.114
53248847 62145 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
CHEMBL1777855 62145 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GPR40 expressed in CHO cells by SPA based binding assayInhibition of human GPR40 expressed in CHO cells by SPA based binding assay
ChEMBL 432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F 10.1016/j.bmcl.2011.03.114
126961699 136678 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
CHEMBL3740291 136678 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonist activity against rat GPR40Antagonist activity against rat GPR40
ChEMBL 411 5 0 6 3.9 CC1(C#N)CN(c2cc(COc3ccc(F)c(F)c3F)nc(-c3ccccn3)n2)C1 10.1039/C5MD00037H
16661950 137664 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 415 10 1 6 4.2 CCOC(=O)CCCCCOc1ccc2cc(CC3SC(=O)NC3=O)ccc2c1 10.1016/j.ejmech.2015.12.049
CHEMBL3758511 137664 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 415 10 1 6 4.2 CCOC(=O)CCCCCOc1ccc2cc(CC3SC(=O)NC3=O)ccc2c1 10.1016/j.ejmech.2015.12.049
16058685 172557 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.ejmech.2015.12.049
CHEMBL448569 172557 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Modulation of FFAR1 (unknown origin)Modulation of FFAR1 (unknown origin)
ChEMBL 229 7 1 3 3.1 CCCCCCCCC1SC(=O)NC1=O 10.1016/j.ejmech.2015.12.049
46854655 395 47 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
24857286 1622 72 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
6484 1622 72 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
CHEMBL1829174 1622 72 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
DB12491 1622 72 None 10 2 Human 7.9 pKd = 7.9 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.0c00843
52936292 182108 27 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
67087246 182875 5 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None - 1 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145617 5 None - 1 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None - 1 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194743 182546 12 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
162644059 181822 0 None - 1 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None - 1 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
127051856 140725 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL3817889 140725 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 preincubated for 5 mins followed by TUG-905 addition measured after 15 mins by kinetic BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
24857286 1622 72 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None 10 2 Human 8.4 pKd = 8.4 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
57706778 80795 29 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
CHEMBL2152070 80795 29 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysisBinding affinity to human GPR40 expressed in CHO cells by LC-MS analysis
ChEMBL 514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1 10.1021/acs.jmedchem.0c00843
58230552 182217 0 None - 1 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None - 1 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
127051856 140725 0 None - 1 Human 8.1 pKd = 8.1 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL3817889 140725 0 None - 1 Human 8.1 pKd = 8.1 Binding
Binding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayBinding affinity to N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/acs.jmedchem.6b00202
51357276 182005 0 None - 1 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None - 1 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assayDisplacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162668378 182505 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787010 182505 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 559 8 1 3 7.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.6b00892
162673875 182984 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4793371 182984 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1 10.1021/acs.jmedchem.6b00892
67087095 183373 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797858 183373 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
162674654 183453 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798993 183453 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1 10.1021/acs.jmedchem.6b00892
67085761 157023 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4073525 157023 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57413290 75824 0 None 2 2 Rat 8.0 pKi = 8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048617 75824 0 None 2 2 Rat 8.0 pKi = 8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
23111682 74100 0 None -5 2 Rat 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022576 74100 0 None -5 2 Rat 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
68194159 183059 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4794233 183059 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1 10.1021/acs.jmedchem.6b00892
23083015 75818 0 None -19 2 Rat 5.0 pKi = 5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
CHEMBL2048611 75818 0 None -19 2 Rat 5.0 pKi = 5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
118129998 157321 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4077366 157321 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
57414677 75623 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047164 75623 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
51357276 182005 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4780641 182005 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11271473 74470 0 None -2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022584 74470 0 None -2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2027975 74470 0 None -2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
57414402 75612 0 None -4 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047152 75612 0 None -4 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857375 75628 0 None -5 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047169 75628 0 None -5 2 Rat 7.0 pKi = 7.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111781 74048 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022247 74048 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23111781 74048 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022247 74048 0 None -6 2 Rat 6.0 pKi = 6.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
57414543 75621 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
CHEMBL2047162 75621 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
24857376 75629 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047170 75629 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57413373 75825 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048618 75825 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
57413375 77217 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2048620 77217 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2079468 77217 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
57414679 75625 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
CHEMBL2047166 75625 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
57413287 75819 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
CHEMBL2048612 75819 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
68194449 182812 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4790921 182812 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57325674 74050 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022249 74050 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 372 6 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CC3CC(=O)O)c1 10.1021/jm2012968
58218673 157523 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4079930 157523 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 413 5 1 3 5.7 Cc1c(Cl)cccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
162667620 182555 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4787628 182555 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
23111693 74056 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
CHEMBL2022255 74056 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
23111766 74059 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022258 74059 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
68194127 183193 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4795763 183193 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
58218740 156443 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4067052 156443 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1 10.1021/acs.jmedchem.6b01559
58218551 159045 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4096887 159045 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
561372 58825 65 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL1688452 58825 65 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 256 6 1 2 3.3 O=C(O)CCc1ccc(OCc2ccccc2)cc1 10.1021/acs.jmedchem.6b00202
67087173 182458 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4786335 182458 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 522 8 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
24857286 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
6484 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
CHEMBL1829174 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
DB12491 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
24857286 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
6484 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
CHEMBL1829174 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
DB12491 1622 72 None -10 2 Rat 6.9 pKi = 6.9 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
91809187 147122 13 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3927519 147122 13 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
57414676 75622 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047163 75622 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
11190525 75823 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048616 75823 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11226058 75828 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048622 75828 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
57413289 75822 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048615 75822 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11203294 75829 3 None -2 5 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048623 75829 3 None -2 5 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
162676686 183484 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4799453 183484 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 523 8 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CC(=O)c3ccccc3O4)cc2)cc1 10.1021/acs.jmedchem.6b00892
11203294 75829 3 None -2 5 Human 7.8 pKi = 7.8 Binding
FFAR1 binding assayFFAR1 binding assay
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 75829 3 None -2 5 Human 7.8 pKi = 7.8 Binding
FFAR1 binding assayFFAR1 binding assay
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
23111693 74056 0 None -12 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
CHEMBL2022255 74056 0 None -12 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 418 7 1 4 5.5 COc1ccc(COc2ccc3c(c2)OCC3CC(=O)O)cc1-c1c(C)cccc1C 10.1021/jm2012968
23111689 74058 0 None -27 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022257 74058 0 None -27 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
71457285 82655 27 None -4 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2179472 82655 27 None -4 2 Rat 5.8 pKi = 5.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
23111781 74048 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022247 74048 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23111694 74057 0 None -24 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
CHEMBL2022256 74057 0 None -24 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
57414405 75615 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047155 75615 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
24857285 75617 0 None -7 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047157 75617 0 None -7 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414539 75618 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047158 75618 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57414540 75620 0 None -5 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047160 75620 0 None -5 2 Rat 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111781 74048 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022247 74048 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 388 6 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/ml1000855
23111682 74100 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022576 74100 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
23642299 75627 1 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047168 75627 1 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
12002202 75832 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048626 75832 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
23157282 77218 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048628 77218 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2079469 77218 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
58218694 158469 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4090766 158469 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 327 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2C[C@@H](F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
137653896 158543 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
CHEMBL4091552 158543 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 326 6 1 4 3.4 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cn1 10.1021/acs.jmedchem.6b01559
24857375 75628 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047169 75628 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 558 11 1 6 6.0 Cc1cc(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
11398822 75830 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048624 75830 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
12002201 75833 1 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048627 75833 1 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
57414676 75622 0 None -12 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047163 75622 0 None -12 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
46854655 395 47 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
6485 395 47 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
CHEMBL1829173 395 47 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00892
162664735 182084 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4781604 182084 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1 10.1021/acs.jmedchem.6b00892
67087100 182596 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4788206 182596 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 576 8 1 4 6.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(C(F)(F)F)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11236925 75826 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048619 75826 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
12002185 75831 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048625 75831 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
68194476 182885 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792075 182885 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1 10.1021/acs.jmedchem.6b00892
23111734 74101 0 None -7 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022577 74101 0 None -7 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
23642299 75627 1 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047168 75627 1 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 542 11 1 6 5.5 Cc1cc(OCCCS(C)(=O)=O)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
58230598 183117 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
CHEMBL4794904 183117 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl 10.1021/acs.jmedchem.6b00892
67072752 86527 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
CHEMBL2315528 86527 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 10.1021/acs.jmedchem.6b00202
57414401 75611 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047151 75611 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
11489259 75827 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048621 75827 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
23111668 74044 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022243 74044 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
57414404 75614 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047154 75614 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
23111668 74044 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022243 74044 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
57325916 74105 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022581 74105 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 488 11 1 4 6.5 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
1050 1900 94 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
11595431 1900 94 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
CHEMBL207881 1900 94 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1021/acs.jmedchem.6b00202
57414403 75613 0 None -8 2 Rat 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047153 75613 0 None -8 2 Rat 5.7 pKi = 5.7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
57414267 75609 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047149 75609 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57413290 75824 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048617 75824 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL5075693 214388 3 None - 1 Human 7.6 pKi = 7.6 Binding
FFAR1 biochemical assayFFAR1 biochemical assay
ChEMBL None None None Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Oc1ccc2c(c1)OC[C@H]2CC(=O)O 10.6019/CHEMBL5058643
137649008 157144 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2CCC[C@@]2(C)CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4075190 157144 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.4 Cc1ccccc1Cc1ccc(N2CCC[C@@]2(C)CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
24857285 75617 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047157 75617 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 566 9 2 7 4.8 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414267 75609 0 None -10 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047149 75609 0 None -10 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
23111754 74046 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022245 74046 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/jm2012968
23111754 74046 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022245 74046 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 414 6 1 2 6.8 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCCC3CC(=O)O)c1 10.1021/ml1000855
57414402 75612 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047152 75612 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57413288 75821 0 None -4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048614 75821 0 None -4 2 Human 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
71257551 150591 24 None - 1 Human 7.6 pKi = 7.6 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3955132 150591 24 None - 1 Human 7.6 pKi = 7.6 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1 10.1021/acs.jmedchem.7b01411
11674915 58860 1 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL1688486 58860 1 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11327107 74049 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
CHEMBL2022248 74049 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/jm2012968
57325841 74103 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022579 74103 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 11 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CC(CC(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
57414403 75613 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047153 75613 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
57414680 75626 0 None -8 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047167 75626 0 None -8 2 Rat 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
11327107 74049 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
CHEMBL2022248 74049 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 402 5 1 3 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)OCCC(C(=O)O)C3)c1 10.1021/ml1000855
24857286 1622 72 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
6484 1622 72 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL1829174 1622 72 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
DB12491 1622 72 None 10 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
57325842 74104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022580 74104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1 10.1021/jm2012968
57414268 75610 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047150 75610 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
67087160 182342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4784555 182342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
23111666 74054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
CHEMBL2022253 74054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4csc5ccccc45)c3)ccc21 10.1021/jm2012968
67087041 182369 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4785057 182369 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
68194465 183304 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4797124 183304 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
23083189 75817 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
CHEMBL2048610 75817 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
57414538 75616 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047156 75616 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
23111734 74101 0 None -7 2 Rat 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2022577 74101 0 None -7 2 Rat 6.5 pKi = 6.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
57414540 75620 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047160 75620 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414680 75626 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047167 75626 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 554 8 1 6 5.6 Cc1cc(OC2CCS(=O)(=O)CC2)c(F)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
137638269 156874 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4071899 156874 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
58218640 158920 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4095599 158920 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
132578495 182884 2 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4792027 182884 2 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
118129999 157765 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4082711 157765 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 453 8 1 5 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C(C)C)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
51350138 58847 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
CHEMBL1688473 58847 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
23111734 74101 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022577 74101 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
23111734 74101 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2022577 74101 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
51350138 58847 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL1688473 58847 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
51350138 58847 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
CHEMBL1688473 58847 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
57414679 75625 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
CHEMBL2047166 75625 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 552 11 1 6 5.9 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OCCCS(C)(=O)=O 10.1021/jm300170m
58218651 158317 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4089171 158317 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 5 1 3 5.0 Cc1ccccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
118129979 155792 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4059614 155792 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 436 7 1 6 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(C#N)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
23111766 74059 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022258 74059 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 402 6 1 3 5.8 Cc1cc(C)c(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
57414405 75615 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047155 75615 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
51350138 58847 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL1688473 58847 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
58218607 155938 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4061093 155938 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57414543 75621 0 None -30 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
CHEMBL2047162 75621 0 None -30 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 529 9 1 6 7.2 Cc1nc(C)c(COc2cc(C)c(-c3cccc(COc4ccc5c(c4)OC[C@H]5CC(=O)O)c3)c(C)c2)s1 10.1021/jm300170m
118129981 159465 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101472 159465 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 513 11 2 7 5.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCC(C)(C)O)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
57414539 75618 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047158 75618 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
71457285 82655 27 None 4 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2179472 82655 27 None 4 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/ml1000855
23111704 74045 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022244 74045 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
23111704 74045 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022244 74045 0 None -63 2 Rat 5.4 pKi = 5.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
24857286 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
6484 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
CHEMBL1829174 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
DB12491 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/jm300170m
24857286 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
6484 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
CHEMBL1829174 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
DB12491 1622 72 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/ml1000855
51031010 156629 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4069191 156629 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 409 6 1 4 5.0 COc1ccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c(C)c1 10.1021/acs.jmedchem.6b01559
57325917 74106 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022582 74106 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
162674998 183389 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4798023 183389 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1 10.1021/acs.jmedchem.6b00892
162676881 183583 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4800563 183583 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1 10.1021/acs.jmedchem.6b00892
11226058 75828 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048622 75828 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 514 12 1 5 5.5 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
60195125 3886 8 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
9149 3886 8 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
CHEMBL2164242 3886 8 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00202
57413373 75825 0 None 2 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048618 75825 0 None 2 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 12 1 4 6.1 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
12002185 75831 0 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048625 75831 0 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 513 12 2 5 5.6 CCS(=O)(=O)CCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
12002201 75833 1 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048627 75833 1 None 4 2 Rat 8.4 pKi = 8.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 555 10 3 6 5.1 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
67087246 182875 5 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4791842 182875 5 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
51049992 145617 5 None - 1 Human 8.3 pKi = 8.3 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL3915620 145617 5 None - 1 Human 8.3 pKi = 8.3 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.7b01411
51049992 145617 5 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL3915620 145617 5 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1 10.1021/acs.jmedchem.6b00892
52936292 182108 27 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4782004 182108 27 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57414678 75624 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
CHEMBL2047165 75624 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
57414678 75624 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
CHEMBL2047165 75624 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 564 8 1 6 6.1 Cc1c(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c(C)c1OC1CCS(=O)(=O)CC1 10.1021/jm300170m
23111791 74053 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022252 74053 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
46854655 395 47 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
6485 395 47 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL1829173 395 47 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O 10.1021/acs.jmedchem.6b00202
162666840 182452 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4786299 182452 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
11271473 74470 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022584 74470 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2027975 74470 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 475 11 2 5 5.9 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
58218638 157434 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4078852 157434 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 311 5 1 3 4.2 Cc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
132606864 157744 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4082395 157744 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 501 7 1 3 6.6 COc1ccc(F)c(-c2ccc(Cc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c(C)c2)c1 10.1021/acs.jmedchem.6b01559
11674915 58860 1 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL1688486 58860 1 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
23082877 75820 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
CHEMBL2048613 75820 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
23111791 74053 0 None -11 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022252 74053 0 None -11 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 424 6 1 3 6.3 Cc1ccc2ccccc2c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm2012968
137636358 155884 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
CHEMBL4060499 155884 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 517 8 1 4 6.8 COc1ccc(F)c(Cc2cccc(Oc3ccc(N4C[C@@H](C(F)(F)F)C[C@H]4CC(=O)O)cc3)c2C)c1 10.1021/acs.jmedchem.6b01559
12002202 75832 0 None 3 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048626 75832 0 None 3 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 525 9 2 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
57413289 75822 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048615 75822 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
46941175 61810 26 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
CHEMBL1773261 61810 26 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 10.1021/acs.jmedchem.6b00202
57414538 75616 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047156 75616 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@@H]3CC(=O)O)c1 10.1021/jm300170m
23111668 74044 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022243 74044 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/jm2012968
23083015 75818 0 None 19 2 Human 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
CHEMBL2048611 75818 0 None 19 2 Human 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(-c2c(C)cccc2C)cc1COc1ccc(CCC(=O)O)cc1 10.1021/jm2016123
23111668 74044 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022243 74044 0 None -2 2 Rat 6.3 pKi = 6.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 386 6 1 2 6.1 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCC3CC(=O)O)c1 10.1021/ml1000855
51350138 58847 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
CHEMBL1688473 58847 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2012968
51350138 58847 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
CHEMBL1688473 58847 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/ml1000855
57414677 75623 0 None -5 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047164 75623 0 None -5 2 Rat 7.3 pKi = 7.3 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111689 74058 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022257 74058 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 388 6 1 3 5.5 Cc1ccc(-c2cccc(COc3ccc4c(c3)OCC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
23111671 74055 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
CHEMBL2022254 74055 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21 10.1021/jm2012968
23083189 75817 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
CHEMBL2048610 75817 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 374 7 1 2 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1C 10.1021/jm2016123
23111704 74045 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
CHEMBL2022244 74045 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/jm2012968
24857376 75629 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047170 75629 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 592 11 1 6 6.6 Cc1c(Cl)c(OCCCS(C)(=O)=O)c(Cl)c(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
23111704 74045 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
CHEMBL2022244 74045 0 None 63 2 Human 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA
ChEMBL 400 6 1 2 6.4 Cc1cccc(C)c1-c1cccc(COc2ccc3c(c2)CCCC3CC(=O)O)c1 10.1021/ml1000855
68194237 182204 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4783033 182204 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57413288 75821 0 None 4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048614 75821 0 None 4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1 10.1021/jm2016123
23157282 77218 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2048628 77218 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
CHEMBL2079469 77218 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 465 12 2 4 6.2 CCOCCOc1cc(C)c(-c2cccc(CNc3ccc(CCC(=O)O)c(F)c3)c2)c(C)c1 10.1021/jm2016123
11203294 75829 3 None 2 5 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048623 75829 3 None 2 5 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
11190525 75823 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
CHEMBL2048616 75823 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 10.1021/jm2016123
11236925 75826 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048619 75826 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 478 9 1 4 6.3 Cc1cc(OC2CCOCC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
57413375 77217 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2048620 77217 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
CHEMBL2079468 77217 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 485 9 1 4 7.2 Cc1cccc(Oc2cc(C)c(-c3cccc(COc4ccc(CCC(=O)O)c(F)c4)c3)c(C)c2)n1 10.1021/jm2016123
23111694 74057 0 None 24 2 Human 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
CHEMBL2022256 74057 0 None 24 2 Human 8.2 pKi = 8.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1 10.1021/jm2012968
58218709 158416 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
CHEMBL4090240 158416 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C 10.1021/acs.jmedchem.6b01559
118151370 159101 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4097527 159101 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
118129974 157192 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4075819 157192 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 575 12 1 8 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cc(OCCCS(C)(=O)=O)cc4C)nn3c2)cc1 10.1021/acs.jmedchem.7b01411
25150014 3883 55 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
3952 3883 55 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
CHEMBL449588 3883 55 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.1021/acs.jmedchem.6b00202
58218542 156764 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4070703 156764 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 297 5 1 3 3.9 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2)cc1 10.1021/acs.jmedchem.6b01559
57414542 77214 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047161 77214 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2079433 77214 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57325917 74106 0 None 5 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
CHEMBL2022582 74106 0 None 5 2 Rat 7.2 pKi = 7.2 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cells after 90 mins by scintillation counting in presence of 0.2% BSA
ChEMBL 476 11 1 5 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)COC4CC(=O)O)c2)c(C)c1 10.1021/jm2012968
58230552 182217 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
CHEMBL4783190 182217 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F 10.1021/acs.jmedchem.6b00892
3367 1155 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
46216676 1155 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
CHEMBL604126 1155 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F 10.1021/acs.jmedchem.6b00202
24857286 1622 72 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
6484 1622 72 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
CHEMBL1829174 1622 72 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
DB12491 1622 72 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C 10.1021/acs.jmedchem.6b00892
58218608 156682 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4069764 156682 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 377 5 1 2 4.8 Cc1ccccc1Cc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1 10.1021/acs.jmedchem.6b01559
57414268 75610 0 None -26 2 Rat 5.1 pKi = 5.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
CHEMBL2047150 75610 0 None -26 2 Rat 5.1 pKi = 5.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@@H]4CC(=O)O)c2)c(C)c1 10.1021/jm300170m
162644059 181822 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
CHEMBL4778264 181822 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1 10.1021/acs.jmedchem.6b00892
137661294 159498 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
CHEMBL4101901 159498 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation countingCompetitive displacement of [3H]-TAK-875 from full length human recombinant GPR40 expressed in HEK293 cell membranes after 2 hrs by scintillation counting
ChEMBL 485 7 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(N3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.7b01411
11398822 75830 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048624 75830 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 556 10 2 6 5.0 Cc1cc(OCC2(O)CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
68194743 182546 12 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
CHEMBL4787498 182546 12 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting methodDisplacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
ChEMBL 499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1 10.1021/acs.jmedchem.6b00892
57414542 77214 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047161 77214 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2079433 77214 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1 10.1021/jm300170m
57414404 75614 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047154 75614 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 536 8 1 6 5.5 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
57414401 75611 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
CHEMBL2047151 75611 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
ChEMBL 488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1 10.1021/jm300170m
6483 3884 54 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
66553168 3884 54 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
CHEMBL2386353 3884 54 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assayDisplacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay
ChEMBL 307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O 10.1021/acs.jmedchem.6b00202
23082877 75820 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
CHEMBL2048613 75820 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 390 8 1 3 5.6 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1-c1c(C)cccc1C 10.1021/jm2016123
58218630 159653 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
CHEMBL4103729 159653 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 379 6 1 3 5.0 O=C(O)C[C@@H]1CCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1 10.1021/acs.jmedchem.6b01559
11489259 75827 0 None 2 2 Rat 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
CHEMBL2048621 75827 0 None 2 2 Rat 8.0 pKi = 8.0 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 519 12 1 4 6.1 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.1021/jm2016123
58218655 156163 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
CHEMBL4063889 156163 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting methodBinding affinity to human GPR40 expressed in HEK293 cell membranes after 1 hr by radioligand displacement based scintillation counting method
ChEMBL 341 6 1 4 3.9 CO[C@H]1C[C@@H](CC(=O)O)N(c2ccc(Oc3ccccc3C)cc2)C1 10.1021/acs.jmedchem.6b01559
57413287 75819 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
CHEMBL2048612 75819 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSADisplacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
ChEMBL 408 8 1 3 5.7 COc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)cccc2C)c1 10.1021/jm2016123
137076846 1113 0 None - 1 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 16 3 9 4.7 OC(=O)CCc1ccc(cc1F)OCc1cccc(c1)c1ccc(cc1C)OCCOCCNc1ccc(c2=NCN=c12)N(O)[O] 27074625
9148 1113 0 None - 1 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 16 3 9 4.7 OC(=O)CCc1ccc(cc1F)OCc1cccc(c1)c1ccc(cc1C)OCCOCCNc1ccc(c2=NCN=c12)N(O)[O] 27074625