Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
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ligand		 Fold
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GPCRs		 Species

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

 Assay
Description		 Source

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weight		 Rot
Bonds		 H don

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 DOI
164616580 192106 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 192106 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 187031 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 187031 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 180746 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 180746 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 178254 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 178254 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 191788 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 191788 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 177857 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 177857 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 156038 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 156038 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 180746 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 180746 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 177857 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 177857 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 8405 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 8405 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 8405 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 8405 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 191385 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 191385 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 153466 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 153466 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 178254 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 178254 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 192090 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 192090 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 191299 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 191299 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 174388 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 174388 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 174388 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 118031 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 118031 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 188889 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 188889 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 192928 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 192928 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 191976 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 191976 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 174388 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 174388 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 174388 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 174431 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 174431 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 174431 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 182890 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 182890 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 190085 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 190085 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 165882 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 165882 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 180447 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 180447 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 174368 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 174368 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 174368 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 149030 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 149030 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 152397 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 152397 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 174432 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 174432 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 174432 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 174368 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 174368 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 174368 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 118578 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 118578 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 7183 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 7183 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 7183 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 189666 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 189666 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 174344 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 174344 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 174344 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 174523 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 174523 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 174523 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 118026 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 118026 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 148948 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 148948 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 148948 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 148948 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 148948 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 148948 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 189286 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 189286 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 174500 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 174500 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 174500 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 173416 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 173416 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 196330 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 196330 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 157246 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 157246 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 170404 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 170404 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 7939 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 7939 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 7939 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 209345 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 209345 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 118744 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 118744 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 80834 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 80834 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 188985 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 188985 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 170763 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 170763 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 153942 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 153942 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 159760 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 159760 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 159760 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 147183 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 147183 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 170663 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 170663 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 171284 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 171284 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 7183 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 7183 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 7183 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 8683 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 8683 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 8683 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 129455 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 129455 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 186365 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 186365 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 186736 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 186736 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 162694 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 162694 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 173821 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 173821 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 68938 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 68938 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 81827 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 81827 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 82737 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 82737 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 94601 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 94601 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 93322 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 93322 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 93333 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 93333 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 187400 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 187400 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 65604 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 65604 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 65604 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 164822 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 164822 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 207865 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 207865 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 148915 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 148915 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 168886 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 168886 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 146604 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 146604 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 180616 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 180616 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 171552 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 171552 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 164822 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 164822 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 130750 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 130750 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 171768 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 171768 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 173218 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 173218 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 198702 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 198702 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 174314 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 174314 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 174314 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 68921 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 68921 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 159024 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 159024 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 174431 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 174431 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 174431 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 96756 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 96756 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 130748 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 130748 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 83039 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 83039 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 83039 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 169860 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 169860 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 147094 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 147094 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 147019 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 147019 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 171558 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 171558 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 191961 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 191961 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 129233 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 129233 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 72119 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 72119 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 68584 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 68584 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 68932 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 68932 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 170984 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 170984 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 130133 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 130133 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 207178 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 207178 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 207893 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 207893 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 169573 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 169573 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 130756 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 130756 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 83050 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 83050 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 199458 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 199458 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 178413 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 178413 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 72102 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 72102 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 186906 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 186906 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 170414 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 170414 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 118577 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 118577 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 153902 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 153902 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 188266 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 188266 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 189285 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 189285 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 189150 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 189150 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 190364 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 190364 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 188985 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 188985 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 125911 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 125911 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 169463 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 169463 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 181724 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 181724 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 146471 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 146471 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 96753 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 96753 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 87572 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 87572 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 182181 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 182181 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 159760 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 159760 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 159760 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 197047 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 197047 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 170379 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 170379 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 76798 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 76798 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 165294 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 165294 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 164602 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 164602 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 165197 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 165197 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 163781 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 163781 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 166564 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 166564 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 173538 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 173538 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 130749 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 130749 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 65605 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 65605 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 87573 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 87573 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 76785 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 76785 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 162719 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 162719 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 166237 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 166237 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 163983 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 163983 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 118738 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 118738 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 173639 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 173639 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 162603 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 162603 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 164566 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 164566 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 172687 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 172687 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 7151 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 7151 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 7151 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 7151 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 7151 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 96748 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 96748 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 129242 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 129242 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 167804 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 167804 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 167804 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 72113 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 72113 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 82700 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 82700 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 153588 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 153588 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 207345 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 207345 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 68921 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 68921 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 169549 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 169549 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 129243 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 129243 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 171122 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 171122 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 168424 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 168424 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 169406 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 169406 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 68939 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 68939 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 146557 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 146557 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 168965 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 168965 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 147764 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 147764 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 167901 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 167901 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 167901 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 83043 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 83043 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 95063 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 95063 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 9067 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 9067 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 9067 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 9067 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 9067 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 114292 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 114292 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 130135 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 130135 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 144524 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 144524 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 166236 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 166236 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 161217 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 161217 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 161217 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 163973 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 163973 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 174134 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 174134 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 171129 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 171129 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 145592 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 145592 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 164350 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 164350 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 163074 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 163074 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 207276 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 207276 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 153902 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 153902 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 147067 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 147067 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 170603 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 170603 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 129448 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 129448 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 129459 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 129459 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 129473 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 129473 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 129474 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 129474 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 146835 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 146835 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 189863 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 189863 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 82598 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 82598 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 188786 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 188786 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 189974 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 189974 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 188889 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 188889 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 171576 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 171576 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 83917 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 83917 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 186251 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 186251 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 81556 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 81556 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 68586 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 68586 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 147637 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 147637 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 65613 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 65613 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 65633 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 65633 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 170563 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 170563 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 176878 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 176878 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 177405 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 177405 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 206974 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 206974 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 76789 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 76789 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 129472 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 129472 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 118742 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 118742 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 186903 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 186903 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 187920 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 187920 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 163804 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 163804 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 165701 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 165701 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 173306 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 173306 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 72121 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 72121 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 65632 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 65632 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 96762 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 96762 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 129244 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 129244 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 87439 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 87439 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 87450 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 87450 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 8683 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 8683 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 8683 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 76790 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 76790 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 76799 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 76799 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 165890 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 165890 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 166210 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 166210 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 174372 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 174372 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 174372 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 169463 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 169463 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 169764 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 169764 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 207386 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 207386 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 122313 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 122313 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 130136 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 130136 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 167997 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 167997 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 167997 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 149011 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 149011 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 96765 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 96765 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 101778 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 101778 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 148905 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 148905 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 148923 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 148923 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 93317 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 93317 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 170690 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 170690 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 145640 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 145640 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 94098 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 94098 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 207095 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 207095 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 68942 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 68942 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 68939 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 68939 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 68931 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 68931 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 96768 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 96768 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 170510 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 170510 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 68585 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 68585 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 147121 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 147121 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 148961 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 148961 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 155054 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 155054 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 186108 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 186108 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 163074 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 163074 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 164609 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 164609 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 166236 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 166236 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 68575 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 68575 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 129281 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 129281 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 167764 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 167764 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 167764 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 68926 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 68926 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 174368 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 174368 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 174368 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 148900 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 148900 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 176354 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 176354 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 161230 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 161230 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 161230 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 167872 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 167872 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 167872 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 171071 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 171071 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 171567 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 171567 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 147061 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 147061 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 191299 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 191299 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 7183 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 7183 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 7183 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 7183 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 7183 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 7183 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 87572 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 87572 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 82394 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 82394 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 170717 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 170717 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 170895 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 170895 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 129412 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 129412 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 129464 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 129464 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 129469 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 129469 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 129475 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 129475 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 8683 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 8683 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 8683 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 154450 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 154450 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 82601 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 82601 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 7183 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 7183 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 7183 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 174495 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 174495 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 174495 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 83917 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 83917 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 96747 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 96747 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 68944 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 68944 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 118736 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 118736 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 173199 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 173199 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 189123 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 189123 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 118737 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 118737 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 118745 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 118745 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 87572 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 87572 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 87572 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 87572 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 161216 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 161216 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 161216 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 165477 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 165477 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 166060 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 166060 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 166195 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 166195 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 163079 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 163079 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 164821 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 164821 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 169547 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 169547 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 87448 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 87448 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 129290 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 129290 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 164609 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 164609 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 72098 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 72098 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 96780 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 96780 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 130170 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 130170 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 169275 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 169275 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 169904 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 169904 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 168817 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 168817 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 171398 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 171398 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 152397 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 152397 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 72122 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 72122 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 65606 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 65606 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 163693 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 163693 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 208978 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 208978 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 130131 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 130131 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 130132 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 130132 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 155355 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 155355 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 171365 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 171365 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 173491 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 173491 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 68922 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 68922 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 68944 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 68944 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 155355 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 155355 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 145556 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 145556 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 148948 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 148948 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 148948 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 169689 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 169689 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 93314 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 93314 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 93319 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 93319 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 171323 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 171323 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 148948 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 148948 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 148948 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 207284 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 207284 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 148923 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 148923 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 157018 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 157018 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 8405 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 8405 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 8405 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 8405 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 192659 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 192659 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 82395 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 82395 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 118745 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 118745 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 82600 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 82600 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 189336 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 189336 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 188603 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 188603 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 189377 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 189377 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 169270 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 169270 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 170717 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 170717 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 171196 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 171196 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 171231 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 171231 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 148936 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 148936 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 8405 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 8405 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 8405 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 8405 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 147183 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 147183 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 65623 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 65623 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 68586 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 68586 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 88497 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 88497 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 81778 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 81778 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 171631 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 171631 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 189520 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 189520 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 162719 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 162719 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 80881 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 80881 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 189898 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 189898 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 130137 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 130137 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 164109 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 164109 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 118736 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 118736 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 166427 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 166427 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 68931 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 68931 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 207283 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 207283 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 97142 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 97142 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 171025 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 171025 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 166532 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 166532 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 146818 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 146818 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 207657 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 207657 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 169016 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 169016 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 93313 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 93313 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 97140 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 97140 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 83200 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 83200 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 145798 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 145798 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 97148 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 97148 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 96764 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 96764 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 197810 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 197810 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 101435 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 101435 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 157855 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 157855 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 174368 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 174368 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 174368 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 149030 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 149030 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 129468 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 129468 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 130107 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 130107 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 10658 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 10658 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 10658 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 173857 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 173857 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 165513 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 165513 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 170954 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 170954 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 130134 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 130134 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 167962 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 167962 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 167962 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 163130 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 163130 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 68933 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 68933 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 68935 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 68935 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 171231 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 171231 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 171576 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 171576 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 82599 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 82599 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 82607 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 82607 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 7183 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 7183 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 7183 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 182164 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 182164 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 170290 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 170290 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 189759 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 189759 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 182988 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 182988 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 146650 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 146650 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 178003 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 178003 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 87572 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 87572 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 189770 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 189770 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 163224 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 163224 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 164530 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 164530 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 165826 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 165826 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 163203 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 163203 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 165534 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 165534 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 173515 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 173515 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 198692 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 198692 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 129446 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 129446 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 163804 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 163804 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 163922 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 163922 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 182427 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 182427 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 93323 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 93323 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 101410 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 101410 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 157372 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 157372 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 147045 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 147045 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 170365 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 170365 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 122440 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 122440 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 197052 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 197052 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 170735 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 170735 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 149011 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 149011 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 65603 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 65603 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 193165 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 193165 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 162766 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 162766 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 169302 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 169302 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 182461 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 182461 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 68933 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 68933 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 171799 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 171799 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 170368 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 170368 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 68934 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 68934 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 160057 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 160057 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 162766 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 162766 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 166383 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 166383 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 166532 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 166532 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 8405 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 8405 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 8405 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 8405 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 82386 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 82386 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 82404 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 82404 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 82405 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 82405 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 170662 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 170662 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 177973 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 177973 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 118435 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 118435 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 164102 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 164102 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 96751 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 96751 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 171558 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 171558 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 118734 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 118734 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 148943 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 148943 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 180778 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 180778 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 192012 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 192012 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 65615 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 65615 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 97145 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 97145 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 129230 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 129230 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 87572 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 87572 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 87572 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 87572 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 87572 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 87572 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 178644 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 178644 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 187197 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 187197 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 8405 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 8405 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 8405 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 8405 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 129234 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 129234 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 129443 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 129443 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 162255 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 162255 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 93326 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 93326 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 148915 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 148915 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 176901 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 176901 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 166383 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 166383 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 208463 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 208463 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 147011 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 147011 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 169522 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 169522 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 68577 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 68577 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 94765 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 94765 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 144468 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 144468 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 144555 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 144555 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 101433 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 101433 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 161905 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 161905 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 7183 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 7183 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 7183 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 170921 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 170921 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 147034 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 147034 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 148905 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 148905 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 82397 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 82397 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 82399 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 82399 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 82400 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 82400 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 82406 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 82406 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 188136 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 188136 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 190331 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 190331 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 188865 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 188865 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 189150 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 189150 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 189840 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 189840 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 190170 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 190170 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 188241 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 188241 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 88496 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 88496 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 88569 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 88569 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 65620 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 65620 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 65621 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 65621 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 171378 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 171378 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 199012 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 199012 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 165560 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 165560 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 173981 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 173981 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 163410 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 163410 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 65641 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 65641 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 80824 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 80824 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 129440 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 129440 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 163977 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 163977 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 166237 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 166237 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 68930 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 68930 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 169639 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 169639 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 156321 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 156321 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 83530 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 83530 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 171224 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 171224 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 72120 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 72120 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 7939 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 7939 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 7939 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 147076 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 147076 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 168192 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 168192 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 176922 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 176922 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 8683 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 8683 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 8683 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 169147 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 169147 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 146976 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 146976 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 82389 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 82389 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 82398 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 82398 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 82402 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 82402 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 171494 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 171494 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 207584 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 207584 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 118743 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 118743 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 189336 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 189336 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 170688 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 170688 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 65636 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 65636 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 188266 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 188266 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 148905 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 148905 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 97137 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 97137 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 97146 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 97146 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 171955 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 171955 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 68586 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 68586 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 68586 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 68586 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 68586 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 68586 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 76796 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 76796 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 189283 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 189283 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 163548 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 163548 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 80832 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 80832 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 188998 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 188998 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 101350 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 101350 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 65619 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 65619 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 198408 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 198408 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 169133 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 169133 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 169523 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 169523 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 9101 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 9101 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 9101 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 9101 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 9101 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 173848 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 173848 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 163608 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 163608 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 10660 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 10660 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 10660 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 94721 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 94721 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 145929 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 145929 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 150033 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 150033 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 150033 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 150033 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 170521 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 170521 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 93292 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 93292 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 72118 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 72118 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 68581 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 68581 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 65604 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 65604 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 65604 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 173301 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 173301 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 147505 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 147505 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 168845 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 168845 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 207728 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 207728 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 129293 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 129293 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 144407 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 144407 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 65637 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 65637 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 8734 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 8734 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 8734 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 186355 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 186355 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 118028 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 118028 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 82403 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 82403 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 83991 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 83991 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 83991 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 170299 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 170299 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 125912 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 125912 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 129453 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 129453 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 189656 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 189656 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 170299 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 170299 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 170638 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 170638 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 170662 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 170662 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 169243 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 169243 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 96772 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 96772 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 176510 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 176510 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 93304 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 93304 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 93304 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 93304 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 129476 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 129476 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 164259 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 164259 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 166497 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 166497 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 189233 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 189233 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 118746 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 118746 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 96752 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 96752 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 93305 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 93305 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 170982 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 170982 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 87438 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 87438 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 87445 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 87445 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 163655 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 163655 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 165701 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 165701 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 101811 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 101811 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 9523 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 9523 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 9523 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 163379 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 163379 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 164497 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 164497 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 65604 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 65604 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 65604 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 146437 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 146437 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 164150 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 164150 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 94721 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 94721 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 170592 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 170592 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 171251 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 171251 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 97149 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 97149 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 10660 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 10660 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 10660 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 144606 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 144606 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 163836 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 163836 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 179679 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 179679 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 170931 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 170931 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 182890 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 182890 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 68581 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 68581 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 93311 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 93311 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 193465 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 193465 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 145864 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 145864 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 193465 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 193465 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 193465 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 193465 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 193465 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 193465 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 94807 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 94807 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 156631 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 156631 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 163508 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 163508 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 163608 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 163608 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 163836 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 163836 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 193116 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 193116 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 178254 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 178254 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 171542 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 171542 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 164546 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 164546 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 186647 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 186647 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 188241 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 188241 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 170895 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 170895 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 178096 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 178096 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 190154 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 190154 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 179582 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 179582 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 190170 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 190170 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 148948 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 148948 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 148948 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 192762 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 192762 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 147794 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 147794 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 186836 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 186836 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 174368 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 174368 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 174368 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 148900 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 148900 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 174314 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 174314 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 174314 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 189974 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 189974 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 190085 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 190085 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 65634 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 65634 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 93304 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 93304 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 145787 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 145787 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 170763 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 170763 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 171265 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 171265 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 118748 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 118748 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 118748 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 118748 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 129479 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 129479 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 118748 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 118748 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 180447 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 180447 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 169270 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 169270 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 82597 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 82597 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 189286 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 189286 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 170632 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 170632 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 171265 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 171265 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 145787 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 145787 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 192540 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 192540 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 177156 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 177156 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 173905 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 173905 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 188441 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 188441 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 159360 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 159360 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 163125 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 163125 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 161317 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 161317 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 161317 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 166359 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 166359 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 207123 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 207123 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 169647 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 169647 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 65603 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 65603 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 148007 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 148007 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 83561 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 83561 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 83044 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 83044 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 93294 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 93294 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 83561 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 83561 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 96767 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 96767 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 167810 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 167810 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 167810 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 206973 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 206973 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 145865 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 145865 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 173449 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 173449 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 207385 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 207385 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 129478 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 129478 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 80830 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 80830 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 190154 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 190154 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 170464 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 170464 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 171204 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 171204 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 187007 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 187007 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 88495 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 88495 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 129236 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 129236 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 171514 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 171514 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 164659 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 164659 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 165571 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 165571 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 129445 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 129445 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 164396 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 164396 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 173348 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 173348 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 173760 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 173760 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 174078 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 174078 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 164602 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 164602 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 118731 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 118731 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 87449 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 87449 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 87570 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 87570 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 197312 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 197312 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 129462 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 129462 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 162696 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 162696 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 158030 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 158030 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 173935 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 173935 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 164000 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 164000 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 118741 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 118741 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 196543 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 196543 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 144491 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 144491 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 169476 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 169476 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 173802 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 173802 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 129282 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 129282 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 171398 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 171398 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 171053 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 171053 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 171345 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 171345 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 168271 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 168271 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 97138 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 97138 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 68572 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 68572 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 146446 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 146446 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 180435 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 180435 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 170733 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 170733 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 163508 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 163508 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 208459 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 208459 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 94766 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 94766 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 93328 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 93328 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 96750 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 96750 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 170060 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 170060 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 118030 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 118030 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 82392 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 82392 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 80825 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 80825 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 179582 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 179582 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 65636 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 65636 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 189666 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 189666 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 148936 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 148936 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 97144 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 97144 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 180545 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 180545 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 146547 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 146547 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 196797 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 196797 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 176335 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 176335 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 177828 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 177828 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 163357 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 163357 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 163655 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 163655 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 164506 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 164506 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 180746 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 180746 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 87444 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 87444 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 92541 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 92541 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 8683 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 8683 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 8683 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 157881 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 157881 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 172675 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 172675 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 207094 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 207094 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 93330 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 93330 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 8683 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 8683 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 8683 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 68942 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 68942 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 173674 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 173674 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 178662 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 178662 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 161906 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 161906 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 206198 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 206198 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 93310 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 93310 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 170434 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 170434 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 80822 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 80822 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 129456 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 129456 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 82603 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 82603 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 82609 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 82609 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 189123 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 189123 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 189765 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 189765 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 169270 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 169270 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 7183 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 7183 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 7183 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 169096 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 169096 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 149011 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 149011 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 88568 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 88568 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 186888 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 186888 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 118747 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 118747 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 87434 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 87434 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 87437 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 87437 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 162944 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 162944 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 169315 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 169315 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 144514 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 144514 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 162889 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 162889 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 191252 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 191252 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 152397 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 152397 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 170327 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 170327 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 170655 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 170655 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 208119 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 208119 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 167759 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 167759 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 167759 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 207891 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 207891 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 173616 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 173616 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 208906 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 208906 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 173993 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 173993 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 171615 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 171615 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 156321 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 156321 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 129283 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 129283 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 170533 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 170533 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 171528 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 171528 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 82388 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 82388 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 80833 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 80833 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 190364 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 190364 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 171494 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 171494 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 174495 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 174495 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 174495 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 181970 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 181970 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 146516 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 146516 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 146769 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 146769 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 146769 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 65614 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 65614 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 182214 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 182214 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 207682 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 207682 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 76800 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 76800 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 164379 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 164379 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 168270 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 168270 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 164525 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 164525 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 162855 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 162855 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 164525 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 164525 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 165428 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 165428 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 174314 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 174314 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 174314 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 170777 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 170777 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 172209 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 172209 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 68941 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 68941 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 178096 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 178096 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 68576 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 68576 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 101812 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 101812 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 174495 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 174495 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 174495 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 68930 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 68930 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 148948 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 148948 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 148948 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 148948 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 148948 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 148948 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 68925 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 68925 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 68942 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 68942 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 170406 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 170406 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 76802 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 76802 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 82605 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 82605 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 82606 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 82606 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 169617 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 169617 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 82606 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 82606 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 149011 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 149011 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 146815 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 146815 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 88495 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 88495 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 146509 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 146509 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 189740 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 189740 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 163055 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 163055 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 118740 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 118740 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 118739 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 118739 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 159494 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 159494 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 158978 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 158978 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 94256 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 94256 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 94766 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 94766 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 170940 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 170940 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 72111 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 72111 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 97139 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 97139 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 148943 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 148943 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 171512 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 171512 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 163226 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 163226 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 167993 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 167993 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 167993 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 169243 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 169243 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 171240 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 171240 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 129284 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 129284 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 207585 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 207585 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 189859 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 189859 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 88495 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 88495 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 83995 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 83995 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 83995 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 171400 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 171400 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 65606 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 65606 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 65628 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 65628 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 21684 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 21684 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 21684 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 198071 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 198071 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 76791 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 76791 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 167859 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 167859 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 167859 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 162855 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 162855 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 163535 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 163535 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 173448 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 173448 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 125914 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 125914 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 164932 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 164932 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 164986 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 164986 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 165165 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 165165 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 162924 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 162924 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 207800 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 207800 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 93307 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 93307 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 65615 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 65615 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 129285 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 129285 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 68942 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 68942 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 129286 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 129286 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 170626 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 170626 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 65615 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 65615 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 8405 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 8405 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 8405 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 8405 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 129444 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 129444 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 80822 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 80822 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 80825 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 80825 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 171966 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 171966 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 8405 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 8405 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 8405 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 8405 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 196888 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 196888 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 82390 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 82390 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 189096 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 189096 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 165917 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 165917 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 65629 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 65629 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 65631 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 65631 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 76797 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 76797 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 163033 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 163033 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 170412 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 170412 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 173505 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 173505 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 170574 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 170574 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 72109 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 72109 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 173804 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 173804 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 171604 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 171604 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 80821 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 80821 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 80877 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 80877 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 80878 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 80878 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 169240 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 169240 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 180447 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 180447 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 186836 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 186836 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 8683 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 8683 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 8683 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 171626 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 171626 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 8683 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 8683 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 8683 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 174513 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 174513 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 174513 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 161246 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 161246 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 161246 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 164995 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 164995 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 174108 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 174108 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 189665 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 189665 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 96758 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 96758 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 68940 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 68940 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 165163 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 165163 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 174038 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 174038 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 173991 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 173991 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 170554 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 170554 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 83564 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 83564 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 7151 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 7151 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 7151 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 7151 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 7151 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 169804 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 169804 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 82401 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 82401 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 170638 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 170638 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 125908 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 125908 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 125908 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 125908 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 186909 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 186909 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 82610 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 82610 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 80835 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 80835 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 148920 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 148920 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 180839 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 180839 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 82387 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 82387 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 82393 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 82393 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 164786 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 164786 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 118437 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 118437 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 172691 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 172691 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 72115 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 72115 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 153041 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 153041 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 149044 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 149044 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 157372 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 157372 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 176354 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 176354 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 182345 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 182345 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 177857 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 177857 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 148948 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 148948 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 148948 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 148948 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 148948 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 148948 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 118029 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 118029 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 118730 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 118730 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 87572 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 87572 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 189239 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 189239 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 118581 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 118581 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 125911 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 125911 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 125911 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 125911 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 118734 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 118734 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 118580 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 118580 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 125902 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 125902 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 125902 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 125902 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 177131 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 177131 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 65624 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 65624 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 65625 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 65625 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 65635 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 65635 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 80878 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 80878 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 170836 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 170836 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 129452 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 129452 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 65623 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 65623 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 170434 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 170434 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 148898 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 148898 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 96770 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 96770 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 96754 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 96754 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 65602 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 65602 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 65627 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 65627 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 129237 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 129237 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 182980 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 182980 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 129287 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 129287 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 7151 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 7151 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 7151 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 7151 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 7151 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 169540 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 169540 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 166014 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 166014 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 174456 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 174456 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 174456 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 171025 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 171025 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 129291 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 129291 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 150066 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 150066 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 83608 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 83608 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 173370 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 173370 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 169741 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 169741 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 68921 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 68921 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 162715 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 162715 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 173952 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 173952 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 209223 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 209223 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 173171 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 173171 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 169189 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 169189 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 93316 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 93316 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 171466 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 171466 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 125904 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 125904 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 125904 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 125904 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 68936 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 68936 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 8405 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 8405 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 8405 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 8405 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 83994 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 83994 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 83994 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 169617 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 169617 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 187422 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 187422 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 8405 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 8405 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 8405 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 8405 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 65603 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 65603 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 171094 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 171094 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 166014 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 166014 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 166060 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 166060 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 118735 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 118735 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 129447 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 129447 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 149002 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 149002 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 72123 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 72123 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 82700 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 82700 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 7151 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 7151 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 7151 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 7151 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 7151 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 209177 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 209177 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 150040 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 150040 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 65622 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 65622 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 10657 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 10657 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 10657 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 118732 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 118732 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 82604 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 82604 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 190234 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 190234 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 170933 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 170933 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 171360 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 171360 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 186647 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 186647 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 10657 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 10657 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 10657 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 146769 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 146769 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 146769 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 8405 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 8405 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 8405 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 8405 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 65618 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 65618 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 165565 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 165565 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 118744 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 118744 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 101779 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 101779 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 172079 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 172079 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 76786 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 76786 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 129463 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 129463 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 165903 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 165903 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 163880 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 163880 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 83496 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 83496 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 197655 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 197655 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 178010 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 178010 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 171076 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 171076 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 174432 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 174432 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 174432 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 174517 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 174517 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 174517 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 80821 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 80821 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 80836 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 80836 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 171604 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 171604 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 97143 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 97143 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 146714 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 146714 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 8405 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 8405 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 8405 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 8405 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 125913 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 125913 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 165098 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 165098 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 170945 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 170945 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 68574 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 68574 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 182164 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 182164 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 207849 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 207849 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 170783 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 170783 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 167879 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 167879 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 167879 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 158226 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 158226 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 93325 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 93325 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 65607 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 65607 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 188219 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 188219 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 177973 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 177973 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 96749 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 96749 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 68586 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 68586 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 65623 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 65623 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 145505 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 145505 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 197839 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 197839 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 166434 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 166434 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 173342 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 173342 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 164259 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 164259 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 87573 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 87573 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 173785 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 173785 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 93312 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 93312 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 172518 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 172518 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 148897 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 148897 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 68921 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 68921 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 65626 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 65626 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 118749 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 118749 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 129461 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 129461 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 118749 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 118749 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 174388 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 174388 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 174388 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 149011 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 149011 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 93308 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 93308 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 97141 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 97141 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 96776 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 96776 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 65639 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 65639 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 65640 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 65640 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 172525 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 172525 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 166195 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 166195 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 170783 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 170783 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 193468 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 193468 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 146988 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 146988 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 83047 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 83047 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 181724 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 181724 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 144448 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 144448 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 160942 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 160942 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 174025 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 174025 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 129480 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 129480 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 174432 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 174432 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 174432 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 148905 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 148905 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 180448 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 180448 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 170862 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 170862 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 82759 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 82759 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 96755 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 96755 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 178787 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 178787 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 197232 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 197232 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 125903 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 125903 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 76626 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 76626 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 125903 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 125903 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 165903 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 165903 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 162914 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 162914 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 163684 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 163684 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 189665 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 189665 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 65604 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 65604 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 65604 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 101350 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 101350 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 159153 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 159153 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 162723 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 162723 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 173291 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 173291 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 170658 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 170658 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 97151 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 97151 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 68573 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 68573 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 171319 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 171319 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 147071 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 147071 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 170688 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 170688 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 188441 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 188441 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 8405 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 8405 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 8405 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 8405 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 145797 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 145797 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 146769 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 146769 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 146769 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 169321 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 169321 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 118033 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 118033 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 87445 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 87445 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 118437 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 118437 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 118437 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 118437 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 166262 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 166262 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 68937 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 68937 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 97154 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 97154 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 192211 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 192211 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 192211 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 192211 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 173799 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 173799 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 162842 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 162842 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 65611 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 65611 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 188241 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 188241 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 118730 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 118730 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 93296 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 93296 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 97147 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 97147 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 174513 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 174513 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 174513 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 80825 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 80825 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 8405 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 8405 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 8405 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 8405 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 177360 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 177360 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 96777 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 96777 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 146665 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 146665 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 150529 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 150529 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 173421 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 173421 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 129441 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 129441 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 165892 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 165892 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 87571 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 87571 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 174344 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 174344 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 174344 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 174523 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 174523 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 174523 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 165914 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 165914 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 173234 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 173234 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 167961 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 167961 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 167961 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 174129 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 174129 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 182063 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 182063 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 145962 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 145962 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 122314 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 122314 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 72110 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 72110 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 82391 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 82391 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 171204 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 171204 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 169240 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 169240 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 80831 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 80831 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 188998 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 188998 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 170404 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 170404 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 96771 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 96771 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 171993 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 171993 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 94803 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 94803 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 93300 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 93300 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 82366 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 82366 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 197092 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 197092 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 198187 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 198187 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 165312 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 165312 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 169320 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 169320 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 87572 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 87572 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 87572 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 87572 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 163811 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 163811 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 68935 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 68935 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 178314 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 178314 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 94764 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 94764 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 173245 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 173245 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 83655 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 83655 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 94808 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 94808 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 94809 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 94809 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 162842 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 162842 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 165914 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 165914 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 198453 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 198453 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 170414 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 170414 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 170594 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 170594 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 170321 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 170321 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 171593 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 171593 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 182890 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 182890 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 189765 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 189765 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 189593 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 189593 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 174500 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 174500 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 174500 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 147979 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 147979 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 82602 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 82602 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 189759 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 189759 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 182063 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 182063 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 189377 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 189377 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 191824 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 191824 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 178064 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 178064 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 147794 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 147794 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 190234 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 190234 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 179582 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 179582 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 65608 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 65608 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 176304 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 176304 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 82594 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 82594 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 93295 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 93295 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 72126 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 72126 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 198452 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 198452 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 180458 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 180458 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 129288 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 129288 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 87436 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 87436 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 174320 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 174320 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 174320 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 148897 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 148897 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 162955 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 162955 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 207866 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 207866 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 173223 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 173223 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 169096 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 169096 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 148898 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 148898 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 83051 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 83051 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 72100 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 72100 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 68932 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 68932 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 7183 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 7183 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 7183 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 178632 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 178632 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 169241 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 169241 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 8405 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 8405 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 8405 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 8405 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 176777 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 176777 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 161291 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 161291 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 161291 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 165052 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 165052 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 188161 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 188161 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 144493 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 144493 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 171164 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 171164 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 148920 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 148920 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 93318 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 93318 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 145776 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 145776 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 94766 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 94766 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 168969 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 168969 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 151159 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 151159 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 68928 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 68928 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 169702 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 169702 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 169240 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 169240 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 72128 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 72128 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 87446 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 87446 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 118735 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 118735 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 198440 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 198440 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 152420 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 152420 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 93298 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 93298 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 171058 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 171058 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 145767 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 145767 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 173423 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 173423 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 72097 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 72097 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 207894 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 207894 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 148915 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 148915 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 148898 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 148898 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 130757 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 130757 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 180783 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 180783 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 72127 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 72127 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 164304 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 164304 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 101350 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 101350 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 147007 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 147007 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 173427 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 173427 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 168256 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 168256 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 68927 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 68927 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 68586 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 68586 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 187977 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 187977 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 164065 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 164065 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 189233 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 189233 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 163535 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 163535 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 149218 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 149218 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 93327 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 93327 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 68578 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 68578 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 83045 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 83045 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 169055 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 169055 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 207815 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 207815 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 65610 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 65610 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 181082 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 181082 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 146769 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 146769 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 146769 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 10657 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 10657 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 10657 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 10657 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 10657 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 10657 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 10660 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 10660 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 10660 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 170978 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 170978 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 198454 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 198454 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 163583 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 163583 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 165324 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 165324 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 165453 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 165453 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 166440 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 166440 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 166434 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 166434 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 162668 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 162668 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 161259 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 161259 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 161259 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 68927 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 68927 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 68578 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 68578 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 171002 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 171002 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 65601 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 65601 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 129289 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 129289 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 169320 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 169320 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 173776 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 173776 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 10657 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 10657 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 10657 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 189285 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 189285 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 96759 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 96759 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 93306 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 93306 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 171504 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 171504 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 145588 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 145588 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 177493 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 177493 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 166581 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 166581 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 174500 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 174500 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 174500 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 184999 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 184999 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 93299 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 93299 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 147046 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 147046 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 65612 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 65612 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 184238 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 184238 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 171360 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 171360 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 169617 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 169617 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 68936 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 68936 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 8683 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 8683 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 8683 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 8683 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 8683 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 8683 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 145922 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 145922 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 207093 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 207093 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 207316 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 207316 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 129235 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 129235 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 72117 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 72117 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 68584 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 68584 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 8683 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 8683 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 8683 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 81247 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 81247 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 81247 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 68928 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 68928 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 187708 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 187708 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 145619 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 145619 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 84065 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 84065 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 87571 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 87571 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 196903 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 196903 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 197765 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 197765 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 207316 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 207316 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 164547 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 164547 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 145923 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 145923 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 65613 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 65613 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 80826 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 80826 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 129466 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 129466 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 118746 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 118746 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 130746 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 130746 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 198918 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 198918 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 163091 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 163091 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 164525 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 164525 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 80824 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 80824 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 177848 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 177848 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 146783 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 146783 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 125910 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 125910 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 125910 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 125910 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 189593 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 189593 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 174314 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 174314 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 174314 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 149011 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 149011 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 125772 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 125772 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 125772 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 125772 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 174218 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 174218 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 65623 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 65623 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 65623 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 65623 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 65623 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 65623 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 10658 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 10658 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 10658 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 174523 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 174523 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 174523 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 8683 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 8683 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 8683 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 8683 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 8683 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 8683 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 165346 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 165346 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 169215 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 169215 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 173776 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 173776 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 154045 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 154045 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 8683 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 8683 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 8683 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 65615 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 65615 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 129238 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 129238 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 162665 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 162665 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 164830 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 164830 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 165197 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 165197 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 207316 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 207316 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 52756 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 52756 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 93575 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 93575 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 148905 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 148905 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 10659 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 10659 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 10659 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 159864 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 159864 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 168645 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 168645 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 145909 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 145909 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 171480 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 171480 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 173881 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 173881 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 146538 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 146538 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 168111 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 168111 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 207346 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 207346 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 68938 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 68938 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 170448 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 170448 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 81783 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 81783 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 182149 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 182149 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 178133 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 178133 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 65601 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 65601 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 163979 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 163979 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 80882 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 80882 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 8405 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 8405 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 8405 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 8405 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 83041 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 83041 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 191939 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 191939 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 72114 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 72114 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 145854 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 145854 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 169522 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 169522 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 68928 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 68928 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 118732 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 118732 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 170877 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 170877 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 96769 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 96769 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 65617 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 65617 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 198304 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 198304 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 166396 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 166396 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 174162 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 174162 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 7151 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 7151 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 7151 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 7151 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 7151 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 192106 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 192106 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 174523 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 174523 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 174523 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 83038 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 83038 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 93320 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 93320 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 72116 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 72116 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 68580 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 68580 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 10659 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 10659 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 10659 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 8405 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 8405 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 8405 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 8405 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 129457 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 129457 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 68930 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 68930 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 164530 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 164530 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 146596 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 146596 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 145588 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 145588 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 171812 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 171812 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 68583 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 68583 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 84356 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 84356 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 65630 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 65630 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 163517 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 163517 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 207575 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 207575 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 169716 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 169716 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 149011 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 149011 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 174495 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 174495 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 174495 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 179836 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 179836 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 170320 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 170320 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 171196 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 171196 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 169765 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 169765 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 176901 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 176901 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 164602 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 164602 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 130746 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 130746 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 168820 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 168820 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 96746 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 96746 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 9101 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 9101 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 9101 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 9101 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 9101 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 129239 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 129239 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 197582 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 197582 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 199196 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 199196 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 80823 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 80823 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 9101 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 9101 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 9101 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 9101 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 9101 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 118733 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 118733 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 174481 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 174481 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 174481 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 159502 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 159502 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 168817 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 168817 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 149044 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 149044 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 178010 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 178010 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 207315 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 207315 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 209226 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 209226 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 188241 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 188241 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 177995 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 177995 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 65601 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 65601 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 170370 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 170370 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 170536 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 170536 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 68577 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 68577 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 9101 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 9101 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 9101 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 9101 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 9101 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 161299 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 161299 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 161299 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 163410 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 163410 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 188786 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 188786 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 96757 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 96757 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 207892 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 207892 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 148897 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 148897 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 96766 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 96766 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 96774 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 96774 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 129231 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 129231 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 129467 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 129467 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 163545 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 163545 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 129471 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 129471 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 164215 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 164215 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 65615 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 65615 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 82323 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 82323 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 179402 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 179402 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 65607 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 65607 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 166285 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 166285 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 169134 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 169134 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 8405 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 8405 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 8405 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 8405 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 171081 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 171081 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 65607 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 65607 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 163500 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 163500 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 80829 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 80829 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 93293 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 93293 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 129229 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 129229 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 76801 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 76801 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 148923 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 148923 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 182292 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 182292 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 193469 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 193469 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 145676 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 145676 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 76788 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 76788 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 163136 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 163136 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 129442 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 129442 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 147064 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 147064 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 147069 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 147069 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 173764 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 173764 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 176593 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 176593 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 180569 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 180569 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 165109 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 165109 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 178033 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 178033 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 68928 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 68928 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 183115 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 183115 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 118027 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 118027 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 121040 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 121040 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 10658 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 10658 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 10658 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 170836 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 170836 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 65623 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 65623 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 65623 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 65623 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 178344 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 178344 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 189327 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 189327 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 10658 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 10658 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 10658 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 125901 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 125901 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 125901 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 125901 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 189656 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 189656 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 65616 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 65616 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 118032 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 118032 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 65636 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 65636 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 174344 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 174344 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 174344 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 178344 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 178344 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 148009 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 148009 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 7183 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 7183 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 7183 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 177995 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 177995 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 162948 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 162948 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 105501 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 105501 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 83037 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 83037 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 83048 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 83048 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 72103 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 72103 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 72099 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 72099 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 105501 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 105501 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 130757 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 130757 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 189239 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 189239 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 148915 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 148915 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 145635 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 145635 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 172258 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 172258 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 96778 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 96778 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 129240 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 129240 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 198677 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 198677 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 168916 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 168916 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 173230 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 173230 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 167803 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 167803 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 167803 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 164101 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 164101 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 163627 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 163627 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 144449 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 144449 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 97150 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 97150 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 72101 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 72101 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 113948 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 113948 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 125907 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 125907 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 125907 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 125907 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 186439 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 186439 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 122442 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 122442 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 122442 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 122442 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 122442 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 122442 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 76794 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 76794 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 166511 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 166511 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 76795 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 76795 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 163709 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 163709 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 165019 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 165019 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 197023 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 197023 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 170984 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 170984 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 207313 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 207313 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 125909 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 125909 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 125909 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 125909 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 129458 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 129458 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 65607 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 65607 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 171371 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 171371 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 96707 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 96707 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 165746 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 165746 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 157228 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 157228 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 83039 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 83039 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 83039 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 83046 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 83046 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 149601 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 149601 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 68571 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 68571 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 154798 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 154798 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 76793 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 76793 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 178033 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 178033 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 187007 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 187007 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 8683 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 8683 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 8683 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 145534 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 145534 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 164650 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 164650 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 173644 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 173644 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 162603 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 162603 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 169020 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 169020 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 206011 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 206011 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 199461 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 199461 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 10659 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 10659 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 10659 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 166227 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 166227 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 129465 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 129465 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 118733 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 118733 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 118741 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 118741 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 190265 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 190265 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 96775 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 96775 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 130747 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 130747 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 87435 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 87435 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 198036 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 198036 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 178235 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 178235 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 164707 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 164707 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 113948 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 113948 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 174431 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 174431 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 174431 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 170896 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 170896 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 81264 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 81264 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 96773 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 96773 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 72106 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 72106 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 101779 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 101779 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 146993 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 146993 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 182374 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 182374 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 170933 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 170933 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 163463 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 163463 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 96760 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 96760 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 82348 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 82348 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 197429 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 197429 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 187633 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 187633 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 76792 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 76792 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 149458 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 149458 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 171071 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 171071 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 65606 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 65606 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 6854 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 6854 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 6854 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 150153 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 150153 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 188603 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 188603 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 145517 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 145517 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 129241 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 129241 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 87442 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 87442 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 163851 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 163851 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 166038 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 166038 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 199249 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 199249 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 8683 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 8683 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 8683 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 192106 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 192106 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 68923 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 68923 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 172283 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 172283 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 207726 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 207726 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 208458 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 208458 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 125905 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 125905 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 125905 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 125905 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 80827 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 80827 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 146366 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 146366 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 170968 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 170968 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 68567 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 68567 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 130747 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 130747 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 181545 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 181545 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 87443 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 87443 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 173612 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 173612 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 163224 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 163224 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 170656 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 170656 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 170620 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 170620 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 148905 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 148905 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 129460 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 129460 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 148936 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 148936 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 188865 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 188865 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 129470 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 129470 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 187422 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 187422 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 118576 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 118576 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 65623 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 65623 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 148936 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 148936 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 171989 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 171989 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 178050 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 178050 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 162727 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 162727 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 164324 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 164324 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 185764 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 185764 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 80826 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 80826 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 186251 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 186251 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 93329 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 93329 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 129232 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 129232 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 173685 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 173685 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 68943 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 68943 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 72104 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 72104 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 159498 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 159498 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 68927 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 68927 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 118731 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 118731 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 170406 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 170406 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 87572 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 87572 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 163463 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 163463 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 168805 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 168805 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 166246 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 166246 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 189840 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 189840 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 97153 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 97153 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 207275 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 207275 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 178673 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 178673 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 165098 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 165098 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 96782 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 96782 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 145525 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 145525 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 180778 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 180778 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 187982 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 187982 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 164215 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 164215 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 165250 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 165250 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 192202 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 192202 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 171278 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 171278 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 97136 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 97136 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 96745 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 96745 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 96781 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 96781 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 171248 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 171248 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 165560 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 165560 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 68580 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 68580 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 144591 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 144591 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 68579 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 68579 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 72112 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 72112 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 185764 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 185764 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 197919 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 197919 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 191299 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 191299 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 174344 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 174344 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 174344 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 9067 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 9067 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 9067 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 9067 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 9067 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 95063 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 95063 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 68943 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 68943 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 10659 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 10659 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 10659 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 172519 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 172519 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 147014 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 147014 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 118747 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 118747 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 101779 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 101779 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 149011 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 149011 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 173458 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 173458 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 164623 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 164623 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 161363 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 161363 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 161363 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 68927 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 68927 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 87441 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 87441 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 76799 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 76799 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 144615 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 144615 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 169022 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 169022 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 208752 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 208752 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 118749 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 118749 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 162665 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 162665 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 101779 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 101779 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 118748 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 118748 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 87571 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 87571 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 87571 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 87571 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 146427 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 146427 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 8683 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 8683 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 8683 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 170773 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 170773 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 72125 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 72125 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 83052 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 83052 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 83052 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 94806 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 94806 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 156321 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 156321 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 72124 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 72124 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 95063 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 95063 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 163744 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 163744 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 165296 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 165296 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 179338 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 179338 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 171593 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 171593 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 65636 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 65636 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 166279 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 166279 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 189327 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 189327 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 174395 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 174395 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 174395 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 190265 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 190265 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 118740 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 118740 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 65636 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 65636 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 117990 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 117990 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 171340 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 171340 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 8405 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 8405 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 8405 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 8405 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 176443 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 176443 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 179885 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 179885 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 169796 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 169796 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 8405 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 8405 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 8405 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 8405 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 163998 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 163998 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 174453 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 174453 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 174453 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 174505 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 174505 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 174505 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 210729 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 210729 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 173559 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 173559 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 173988 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 173988 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 163154 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 163154 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 118738 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 118738 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 145956 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 145956 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 65615 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 65615 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 161254 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 161254 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 161254 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 177131 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 177131 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 150687 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 150687 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 93297 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 93297 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 210729 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 210729 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 149002 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 149002 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 65632 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 65632 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 164938 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 164938 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 125906 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 125906 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 164304 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 164304 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 165917 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 165917 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 96761 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 96761 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 169620 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 169620 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 101434 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 101434 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 163501 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 163501 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 170464 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 170464 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 125906 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 125906 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 190077 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 190077 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 68583 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 68583 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 93324 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 93324 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 145911 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 145911 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 68582 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 68582 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 173447 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 173447 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 65601 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 65601 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 174500 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 174500 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 174500 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 80880 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 80880 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 189210 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 189210 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 118732 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 118732 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 174174 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 174174 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 171400 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 171400 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 68929 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 68929 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 198390 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 198390 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 145594 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 145594 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 83042 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 83042 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 144614 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 144614 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 165296 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 165296 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 171615 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 171615 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 189898 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 189898 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 177930 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 177930 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 163744 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 163744 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 146715 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 146715 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 182345 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 182345 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 192083 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 192083 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 7939 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 7939 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 7939 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 8683 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 8683 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 8683 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 198698 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 198698 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 68940 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 68940 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 170632 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 170632 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 208907 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 208907 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 96779 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 96779 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 68929 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 68929 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 198090 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 198090 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 164332 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 164332 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 162947 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 162947 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 166077 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 166077 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 129454 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 129454 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 178344 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 178344 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 93321 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 93321 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 193026 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 193026 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 68579 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 68579 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 146684 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 146684 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 166427 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 166427 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 193466 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 193466 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 188241 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 188241 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 170321 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 170321 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 170620 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 170620 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 118583 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 118583 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 162573 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 162573 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 170603 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 170603 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 152397 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 152397 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 152397 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 152397 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 10660 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 10660 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 10660 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 82758 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 82758 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 146758 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 146758 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 118737 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 118737 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 88567 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 88567 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 169098 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 169098 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 187708 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 187708 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 187977 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 187977 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 186888 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 186888 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 65638 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 65638 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 129477 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 129477 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 170288 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 170288 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 171606 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 171606 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 206260 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 206260 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 173637 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 173637 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 148923 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 148923 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 177848 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 177848 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 146553 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 146553 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 87440 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 87440 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 76787 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 76787 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 163796 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 163796 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 80883 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 80883 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 68582 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 68582 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 200231 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 200231 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 197065 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 197065 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 118739 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 118739 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 65602 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 65602 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 72107 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 72107 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 148897 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 148897 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 122441 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 122441 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 174395 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 174395 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 174395 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 164807 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 164807 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 150557 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 150557 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 207384 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 207384 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 68930 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 68930 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 93315 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 93315 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 172688 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 172688 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 83040 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 83040 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 93309 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 93309 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 169020 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 169020 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 68926 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 68926 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 169344 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 169344 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 96763 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 96763 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 162775 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 162775 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 80823 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 80823 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 157137 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 157137 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 68932 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 68932 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 93331 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 93331 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 193465 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 193465 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 171475 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 171475 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 68937 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 68937 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 83052 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 83052 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 83052 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 72108 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 72108 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 193465 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 193465 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 206121 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 206121 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 118743 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 118743 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 145516 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 145516 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 146499 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 146499 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 80879 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 80879 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 162944 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 162944 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 169053 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 169053 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 94721 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 94721 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 171611 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 171611 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 101350 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 101350 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 129450 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 129450 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 68924 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 68924 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 187499 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 187499 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 190721 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 190721 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 93332 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 93332 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 190721 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 190721 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 9523 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 9523 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 9523 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 129449 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 129449 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 173255 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 173255 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 68934 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 68934 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 82608 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 82608 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 8683 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 8683 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 8683 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 144556 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 144556 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 191014 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 191014 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 191303 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 191303 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 191557 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 191557 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 143535 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 143535 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 152140 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 152140 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 143450 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 143450 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 149631 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 149631 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 190990 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 190990 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 191304 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 191304 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 143434 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 143434 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 143354 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 143354 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 143419 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 143419 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 149782 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 149782 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 191013 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 191013 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 191483 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 191483 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 143458 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 143458 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 143678 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 143678 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 143684 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 143684 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 151017 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 151017 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 143501 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 143501 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 143509 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 143509 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 156828 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 156828 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 191468 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 191468 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 191690 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 191690 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 191564 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 191564 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 191057 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 191057 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 157785 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 157785 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 143654 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 143654 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 143380 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 143380 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 143390 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 143390 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 143570 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 143570 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 143637 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 143637 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 143527 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 143527 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 158055 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 158055 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 101813 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 101813 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 154600 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 154600 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 198263 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 198263 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 191469 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 191469 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 143534 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 143534 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 143575 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 143575 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 143627 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 143627 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 143608 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 143608 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 153477 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 153477 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 156126 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 156126 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 143367 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 143367 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 143441 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 143441 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 143459 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 143459 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 143477 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 143477 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 143518 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 143518 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 143543 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 143543 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 143557 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 143557 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 198374 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 198374 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 159035 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 159035 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 143562 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 143562 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 143593 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 143593 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 143595 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 143595 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 143631 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 143631 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 175642 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 175642 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 160256 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 160256 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 143612 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 143612 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 143391 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 143391 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 143462 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 143462 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 143625 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 143625 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 143569 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 143569 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 143568 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 143568 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 143483 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 143483 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 143478 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 143478 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 143504 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 143504 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 143361 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 143361 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 154425 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 154425 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 191056 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 191056 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 191701 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 191701 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 184999 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 184999 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 7151 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 7151 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 7151 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 7151 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 7151 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 10144 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 10144 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 10144 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 10144 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 10144 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 9101 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 9101 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 9101 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 9101 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 9101 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 9691 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 9691 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 9691 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 9691 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 9067 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 9067 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 9067 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 9067 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 9067 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 10366 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 10366 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 10366 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 10366 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9768 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9691 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9471 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 9101 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 7151 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 8237 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 7939 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 7939 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 7939 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8683 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 8683 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 8683 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 10657 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 10657 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 10657 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 8734 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 8734 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 8734 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 10660 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 10660 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 10660 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 10658 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 10658 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 10658 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 7183 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 7183 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 7183 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 10144 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 10144 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 10144 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 10144 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 10144 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 9260 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 9260 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 9260 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 8675 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 8675 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 8675 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 8675 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 8675 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 8675 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 Assay information 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 189765 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 189765 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 188889 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 188889 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 189377 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 189377 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 189765 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 189765 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 189150 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 189150 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 189377 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 189377 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 190154 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 190154 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 190085 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 190085 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 153270 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 153270 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 189286 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 189286 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 190234 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 190234 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 190154 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 190154 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 152397 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 152397 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 189656 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 189656 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 189150 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 189150 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 188889 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 188889 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 157372 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 157372 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 190234 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 190234 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 189286 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 189286 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 190085 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 190085 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 189286 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 189286 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 189327 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 189327 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 190170 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 190170 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 190364 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 190364 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 97080 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 97080 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 189656 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 189656 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 190170 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 190170 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 188865 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 188865 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 150985 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 150985 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 7183 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 7183 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 7183 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 190154 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 190154 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 189327 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 189327 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 189765 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 189765 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 8405 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 8405 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 8405 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 8405 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 150011 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 150011 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 158764 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 158764 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 149617 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 149617 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 188865 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 188865 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 189840 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 189840 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 189123 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 189123 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 200466 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 201059 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 118576 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 118576 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 145558 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 145558 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 7183 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 7183 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 7183 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 183895 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 183895 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 118021 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 118021 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 97084 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 97084 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 145594 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 145594 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 118026 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 118026 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 153902 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 153902 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 189123 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 189123 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 189593 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 189593 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 7183 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 7183 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 7183 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 189656 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 189656 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 68586 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 68586 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 189898 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 189898 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 200256 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 200288 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 164602 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 164602 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 201280 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 201285 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 200740 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 200893 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 178272 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 178272 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 144295 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 144295 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 145516 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 145516 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 118023 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 118023 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 10144 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 10144 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 10144 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 10144 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 10144 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 154399 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 154399 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 118578 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 118578 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 157706 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 157706 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 8405 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 8405 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 8405 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 8405 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 117991 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 117991 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 189233 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 189233 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 189665 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 189665 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 144040 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 144040 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 201028 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 201066 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 200384 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 200775 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 201202 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 222179 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 184831 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 184831 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 118029 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 118029 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 201259 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 7183 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 7183 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 7183 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 144330 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 144330 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 200675 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 121038 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 121038 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 201076 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 177682 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 177682 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 182890 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 182890 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 97088 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 97088 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 153902 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 153902 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 201104 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 10660 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 10660 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 10660 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 201296 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 151105 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 151105 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 200235 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 165890 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 165890 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 200566 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 188603 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 188603 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 118025 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 118025 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 200756 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 97085 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 97085 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 118022 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 118022 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 182085 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 182085 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 163973 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 163973 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 118027 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 118027 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 97090 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 97090 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 201196 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 184635 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 184635 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 7183 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 7183 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 7183 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 145640 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 145640 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 180444 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 180444 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 184246 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 184246 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 189336 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 189336 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 149875 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 149875 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 154676 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 154676 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 200279 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 200533 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 188998 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 188998 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 87572 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 87572 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 200957 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 200329 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 200758 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 87572 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 87572 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 118031 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 118031 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 165882 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 165882 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 188985 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 188985 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 189593 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 189593 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 199458 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 199458 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 201053 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 189840 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 189840 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 189123 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 189123 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 200903 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 10658 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 10658 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 10658 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 97087 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 97087 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 200648 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 200716 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 201161 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 200890 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 201167 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 201104 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 200273 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 177819 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 177819 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 68586 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 68586 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 121037 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 121037 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 144092 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 144092 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 144154 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 144154 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 200757 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 200938 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 186819 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 186819 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 189239 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 189239 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 152397 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 152397 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 153413 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 153413 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 189666 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 189666 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 190265 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 190265 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 190364 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 190364 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 149185 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 149185 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 7183 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 7183 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 7183 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 189377 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 189377 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 200338 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 121038 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 121038 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 159760 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 159760 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 159760 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 200975 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 200589 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 200372 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 187481 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 187481 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 201209 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 164396 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 164396 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 164602 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 164602 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 144344 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 144344 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 97081 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 97081 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 97089 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 97089 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 162573 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 162573 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 10658 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 10658 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 10658 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 200262 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 200617 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 144349 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 144349 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 200630 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 200769 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 118024 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 118024 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 7183 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 7183 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 7183 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 189974 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 189974 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 200978 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 144053 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 144053 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 144197 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 144197 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 184522 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 184522 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 152397 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 152397 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 118032 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 118032 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 93304 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 93304 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 200342 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 144197 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 144197 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 200593 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 201264 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 182433 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 182433 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 118030 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 118030 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 189239 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 189239 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 76802 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 76802 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 118033 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 118033 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 200888 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 200600 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 200314 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 201150 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 183455 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 183455 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 183455 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 170982 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 170982 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 190265 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 190265 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 10658 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 10658 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 10658 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 200506 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 8405 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 8405 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 8405 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 8405 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 8683 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 8683 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 8683 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 118028 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 118028 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 187715 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 187715 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 118576 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 118576 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 200972 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 153106 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 153106 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 121037 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 121037 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 200941 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 200819 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 144095 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 144095 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 157372 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 157372 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 188865 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 188865 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 221169 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 7183 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 7183 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 7183 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 188786 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 188786 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 189150 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 189150 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 190234 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 190234 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 177857 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 177857 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 188985 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 188985 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 189593 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 189593 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 190085 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 190085 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 164546 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 164546 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 200731 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 164846 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 164846 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 200640 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 200778 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 200849 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 200924 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 117992 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 117992 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 144085 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 144085 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 166246 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 166246 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 186442 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 186442 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 187100 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 187100 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 201023 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 184257 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 184257 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 8683 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 8683 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 8683 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 201239 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 201132 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 188998 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 188998 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 164525 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 164525 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 201048 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 10658 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 10658 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 10658 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 200306 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 106983 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 106983 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 106983 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 118576 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 118576 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 118577 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 118577 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 118576 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 118576 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 164602 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 164602 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 144067 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 144067 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 144269 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 144269 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 200875 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 10659 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 10659 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 10659 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 188998 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 188998 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 201160 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 97073 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 97073 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 8405 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 8405 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 8405 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 8405 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 118575 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 118575 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 118581 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 118581 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 189336 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 189336 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 144215 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 144215 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 164324 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 164324 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 121036 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 121036 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 118020 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 118020 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 170945 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 170945 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 200658 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 118019 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 118019 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 176408 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 176408 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 97086 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 97086 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 149749 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 149749 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 188603 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 188603 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 184927 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 184927 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 93304 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 93304 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 153466 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 153466 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 189666 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 189666 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 153557 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 153557 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 190265 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 190265 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 189239 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 189239 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 156896 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 156896 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 144148 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 144148 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 200269 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 118580 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 118580 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 144247 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 144247 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 201297 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 183898 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 183898 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 200970 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 189233 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 189233 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 144215 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 144215 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 144064 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 144064 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 144177 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 144177 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 200330 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 200862 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 144347 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 144347 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 201058 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 162573 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 162573 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 8405 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 8405 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 8405 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 8405 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 200357 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 184447 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 184447 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 200692 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 184238 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 184238 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 8683 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 8683 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 8683 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 144117 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 144117 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 200972 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 200561 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 17371 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 17371 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 201104 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 184769 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 184769 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 188889 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 188889 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 188786 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 188786 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 189336 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 189336 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 200456 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 97093 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 97093 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 200264 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 200292 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 184254 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 184254 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 184750 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 184750 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 200903 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 97091 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 97091 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 189840 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 189840 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 184073 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 184073 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 8405 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 8405 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 8405 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 8405 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 7939 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 7939 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 7939 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 189898 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 189898 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 189665 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 189665 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 201004 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 65601 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 65601 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 184031 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 184031 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 184133 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 184133 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 188786 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 188786 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 121036 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 121036 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 144064 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 144064 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 164102 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 164102 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 189972 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 189972 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 118583 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 118583 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 188985 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 188985 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 144095 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 144095 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 200375 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 201242 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 184289 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 184289 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 144344 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 144344 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 183037 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 183037 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 183037 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 184804 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 184804 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 121040 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 121040 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 189665 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 189665 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 7183 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 7183 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 7183 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 201129 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 188603 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 188603 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 200358 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 201006 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 144349 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 144349 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 93304 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 93304 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 200473 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 144295 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 144295 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 184718 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 184718 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 184386 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 184386 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 189666 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 189666 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 163074 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 163074 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 183886 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 183886 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 201291 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 184741 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 184741 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 118576 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 118576 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 121040 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 121040 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 184231 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 184231 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 118579 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 118579 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 199461 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 199461 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 144117 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 144117 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 164546 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 164546 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 10657 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 10657 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 10657 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 184618 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 184618 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 184859 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 184859 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 190244 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 190244 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 117989 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 117989 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 182374 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 182374 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 166246 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 166246 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 189233 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 189233 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 164102 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 164102 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 118582 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 118582 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 144085 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 144085 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 200348 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 93304 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 93304 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 144033 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 144033 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 152764 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 152764 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 157372 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 157372 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 189974 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 189974 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 8405 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 8405 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 8405 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 8405 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 152278 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 152278 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 152246 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 152246 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 189327 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 189327 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 200290 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 200985 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 200812 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 201243 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 184497 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 184497 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 200866 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 184504 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 184504 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 201090 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 118435 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 118435 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 189898 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 189898 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 200300 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 201145 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 65606 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 65606 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 144333 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 144333 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 117990 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 117990 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 96747 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 96747 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 199461 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 199461 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 200767 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 200328 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 184109 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 184109 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 145619 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 145619 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 97092 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 97092 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 184551 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 184551 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 9067 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 9067 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 9067 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 9067 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 9067 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 183903 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 183903 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 190364 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 190364 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 8405 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 8405 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 8405 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 8405 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 152111 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 152111 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 159760 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 159760 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 159760 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 152397 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 152397 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 7183 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 7183 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 7183 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 97080 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 97080 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 200771 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 97078 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 97078 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 184917 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 184917 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 189974 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 189974 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 117987 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 117987 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 7183 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 7183 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 7183 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 144177 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 144177 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 190170 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 190170 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 8405 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 8405 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 8405 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 8405 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 97082 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 97082 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 117988 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 117988 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 8405 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 8405 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 8405 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 8405 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 145525 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 145525 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 163973 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 163973 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 144167 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 144167 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 200609 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 183877 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 183877 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 97083 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 97083 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 165882 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 165882 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 200605 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 144167 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 144167 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 68941 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 68941 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 68927 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 68927 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 68930 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 68930 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 68944 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 68944 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 68942 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 68942 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 143390 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 143390 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 68931 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 68931 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 68928 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 68928 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 68938 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 68938 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 68943 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 68943 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 68934 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 68934 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 68932 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 68932 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 143612 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 143612 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 68939 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 68939 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 68935 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 68935 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 68940 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 68940 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 68929 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 68929 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 68926 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 68926 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 68936 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 68936 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 68933 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 68933 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 68937 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 68937 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 68921 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 68921 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 143458 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 143458 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 144444 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 144444 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 179338 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 179338 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 7183 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 7183 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 7183 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 8405 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 8405 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 8405 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 8405 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 188889 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 188889 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 189656 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 189656 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 152397 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 152397 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 189327 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 189327 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 188603 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 188603 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 147505 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 147505 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 8405 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 8405 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 8405 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 8405 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 87572 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 87572 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 188998 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 188998 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 147505 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 147505 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 188786 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 188786 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 189286 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 189286 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 189765 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 189765 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 190154 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 190154 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 190234 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 190234 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 163804 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 163804 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 82601 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 82601 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 80877 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 80877 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 189840 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 189840 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 82595 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 82595 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 164102 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 164102 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 82400 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 82400 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 188786 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 188786 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 81247 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 81247 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 81247 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 82389 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 82389 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 82405 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 82405 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 80825 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 80825 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 80825 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 80825 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 82398 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 82398 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 82406 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 82406 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 82602 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 82602 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 83994 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 83994 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 83994 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 82402 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 82402 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 82596 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 82596 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 189593 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 189593 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 80827 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 80827 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 164304 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 164304 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 189336 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 189336 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 80833 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 80833 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 80836 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 80836 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 189974 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 189974 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 163224 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 163224 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 165826 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 165826 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 65601 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 65601 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 189239 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 189239 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 153902 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 153902 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 82399 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 82399 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 82600 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 82600 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 82605 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 82605 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 82599 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 82599 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 82606 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 82606 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 190265 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 190265 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 82606 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 82606 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 80833 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 80833 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 80835 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 80835 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 89432 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 89432 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 80825 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 80825 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 80834 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 80834 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 82392 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 82392 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 82394 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 82394 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 82395 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 82395 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 82397 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 82397 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 80825 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 80825 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 80877 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 80877 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 82404 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 82404 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 82609 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 82609 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 83995 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 83995 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 83995 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 165250 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 165250 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 165324 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 165324 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 82405 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 82405 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 82607 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 82607 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 82610 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 82610 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 82399 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 82399 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 7183 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 7183 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 7183 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 188865 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 188865 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 189377 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 189377 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 82603 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 82603 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 82608 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 82608 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 189666 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 189666 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 80878 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 80878 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 82404 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 82404 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 189898 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 189898 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 93304 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 93304 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 82388 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 82388 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 82604 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 82604 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 80821 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 80821 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 82391 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 82391 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 80821 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 80821 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 80882 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 80882 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 8683 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 8683 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 8683 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 82390 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 82390 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 82386 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 82386 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 82601 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 82601 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 221169 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 163925 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 163925 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 82394 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 82394 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 82386 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 82386 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 80823 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 80823 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 80823 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 80823 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 82389 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 82389 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 82598 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 82598 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 157372 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 157372 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 65636 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 65636 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 80826 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 80826 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 80880 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 80880 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 82390 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 82390 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 82403 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 82403 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 80826 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 80826 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 8405 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 8405 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 8405 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 8405 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 80881 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 80881 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 82387 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 82387 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 189123 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 189123 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 80831 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 80831 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 189150 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 189150 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 190085 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 190085 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 82594 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 82594 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 82393 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 82393 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 80878 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 80878 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 82397 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 82397 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 82403 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 82403 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 163655 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 163655 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 165701 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 165701 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 189665 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 189665 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 164546 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 164546 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 65623 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 65623 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 80878 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 80878 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 80878 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 80878 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 65623 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 65623 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 65623 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 65623 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 82402 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 82402 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 165098 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 165098 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 162573 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 162573 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 80836 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 80836 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 82392 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 82392 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 65623 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 65623 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 162719 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 162719 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 82398 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 82398 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 166246 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 166246 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 82395 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 82395 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 89432 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 89432 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 80822 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 80822 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 80822 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 80822 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 8405 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 163410 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 163410 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 80883 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 80883 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 190170 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 190170 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 190364 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 190364 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 82605 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 82605 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 10660 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 10660 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 10660 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 82602 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 82602 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 82608 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 82608 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 82610 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 82610 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 189656 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 189656 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 152397 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 152397 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 152397 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 152397 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 188889 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 188889 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 82401 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 82401 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 82401 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 82401 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 80830 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 80830 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 7183 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 7183 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 7183 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 189233 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 189233 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 81247 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 81247 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 81247 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 164215 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 164215 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 164525 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 164525 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 65636 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 65636 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 82597 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 82597 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 80830 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 80830 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 162665 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 162665 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 82609 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 82609 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 82599 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 82599 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 68586 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 68586 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 82393 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 82393 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 80821 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 80821 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 82595 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 82595 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 80821 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 80821 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 65623 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 65623 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 65623 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 65623 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 82400 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 82400 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 80835 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 80835 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 80832 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 80832 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 82594 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 82594 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 80822 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 80822 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 82406 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 82406 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 80822 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 80822 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 188985 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 188985 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 82598 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 82598 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 83995 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 83995 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 83995 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 82606 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 82606 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 82600 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 82600 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 82603 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 82603 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 83994 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 83994 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 83994 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 80834 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 80834 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 165197 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 165197 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 165882 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 165882 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 163973 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 163973 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 10657 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 10657 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 10657 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 163545 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 163545 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 83991 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 83991 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 83991 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 80883 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 80883 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 188998 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 188998 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 7939 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 7939 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 7939 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 8405 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 8405 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 8405 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 8405 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 163463 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 163463 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 82387 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 82387 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 188603 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 188603 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 166279 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 166279 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 82607 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 82607 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 189327 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 189327 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 83991 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 83991 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 83991 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 82391 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 82391 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 82388 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 82388 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 10658 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 10658 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 10658 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 82597 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 82597 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 166434 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 166434 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 82604 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 82604 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 162944 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 162944 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 82596 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 82596 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 7898 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 7898 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