Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL475027 ffar1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at GPR40 expressed in CHO cells by FLIPR assayAgonist activity at GPR40 expressed in CHO cells by FLIPR assay
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
CHEMBL4541658 ffar1_human Human No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL4463571 ffar1_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL4457303 ffar1_human Human No 9.6 EC50 = 0.3 nM Funct
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
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
CHEMBL3944424 ffar1_human Human No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL4541658 ffar1_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL4457303 ffar1_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1829174 ffar1_human Human Yes 9.5 EC50 = 0.4 nM Funct
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL3923877 ffar1_rat Rat No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL4463571 ffar1_rat Rat No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL4793371 ffar1_mouse Mouse No 9.4 EC50 = 0.4 nM Bind
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
505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1
CHEMBL4782004 ffar1_mouse Mouse Yes 9.3 EC50 = 0.5 nM Bind
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
497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4165147 ffar1_rat Rat Yes 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL4301092 ffar1_rat Rat Yes 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL4788206 ffar1_mouse Mouse No 9.3 EC50 = 0.5 nM Bind
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
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
CHEMBL4793371 ffar1_rat Rat No 9.3 EC50 = 0.5 nM Bind
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
505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1
CHEMBL4785057 ffar1_mouse Mouse No 9.2 EC50 = 0.6 nM Bind
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
542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1
CHEMBL4788206 ffar1_rat Rat No 9.2 EC50 = 0.6 nM Bind
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
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
CHEMBL3265149 ffar1_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL4782004 ffar1_human Human Yes 9.2 EC50 = 0.6 nM Funct
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
497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4797858 ffar1_mouse Mouse No 9.2 EC50 = 0.6 nM Bind
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
570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1
CHEMBL4797124 ffar1_mouse Mouse No 9.2 EC50 = 0.7 nM Bind
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
511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL3922381 ffar1_human Human No 9.1 EC50 = 0.8 nM Bind
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
501 11 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(F)(F)F)c2)cc1
CHEMBL4165147 ffar1_human Human Yes 9.1 EC50 = 0.8 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
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
CHEMBL4301092 ffar1_human Human Yes 9.1 EC50 = 0.8 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
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
CHEMBL4787010 ffar1_mouse Mouse No 9.1 EC50 = 0.8 nM Bind
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
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
CHEMBL4798993 ffar1_mouse Mouse No 9.1 EC50 = 0.8 nM Bind
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
525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1
CHEMBL4797858 ffar1_rat Rat No 9.1 EC50 = 0.8 nM Bind
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
570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1
CHEMBL3915620 ffar1_mouse Mouse Yes 9.1 EC50 = 0.9 nM Bind
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
491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1
CHEMBL4791842 ffar1_mouse Mouse Yes 9.1 EC50 = 0.9 nM Bind
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
493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1
CHEMBL4785057 ffar1_rat Rat No 9.1 EC50 = 0.9 nM Bind
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
542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1
CHEMBL4163182 ffar1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1
CHEMBL4301725 ffar1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1
CHEMBL4782004 ffar1_rat Rat Yes 9.0 EC50 = 0.9 nM Bind
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
497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4591657 ffar1_human Human No 9.0 EC50 = 0.9 nM Funct
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
426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL4797124 ffar1_human Human No 9.0 EC50 = 1.0 nM Funct
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
511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL3955132 ffar1_mouse Mouse Yes 9.0 EC50 = 1 nM Bind
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
475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1
CHEMBL4798993 ffar1_rat Rat No 9.0 EC50 = 1 nM Bind
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
525 8 1 3 7.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(Cl)c2)cc1
CHEMBL4097527 ffar1_human Human No 9.0 EC50 = 1 nM Funct
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
477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1
CHEMBL4787010 ffar1_rat Rat No 9.0 EC50 = 1.1 nM Bind
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
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
CHEMBL4797124 ffar1_rat Rat No 9.0 EC50 = 1.1 nM Bind
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
511 8 1 4 6.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4534836 ffar1_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL4787010 ffar1_human Human No 9.0 EC50 = 1.1 nM Bind
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
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
CHEMBL4159416 ffar1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL4300796 ffar1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL3884803 ffar1_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL4787498 ffar1_mouse Mouse Yes 8.9 EC50 = 1.2 nM Bind
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
499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1
CHEMBL4798023 ffar1_mouse Mouse No 8.9 EC50 = 1.2 nM Bind
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
509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1
CHEMBL4800563 ffar1_mouse Mouse No 8.9 EC50 = 1.2 nM Bind
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
536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1
CHEMBL3915620 ffar1_human Human Yes 8.9 EC50 = 1.2 nM Funct
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
491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1
CHEMBL4160527 ffar1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
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
CHEMBL4301726 ffar1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
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
CHEMBL4159416 ffar1_rat Rat No 8.9 EC50 = 1.2 nM Funct
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
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL4300796 ffar1_rat Rat No 8.9 EC50 = 1.2 nM Funct
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
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL4791842 ffar1_rat Rat Yes 8.9 EC50 = 1.3 nM Bind
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
493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1
CHEMBL4798023 ffar1_rat Rat No 8.9 EC50 = 1.3 nM Bind
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
509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1
CHEMBL3287571 ffar1_human Human No 8.9 EC50 = 1.3 nM Funct
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
462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1
CHEMBL1829173 ffar1_human Human Yes 8.9 EC50 = 1.3 nM Funct
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL4781604 ffar1_mouse Mouse No 8.9 EC50 = 1.4 nM Bind
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
521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1
CHEMBL3904378 ffar1_human Human No 8.9 EC50 = 1.4 nM Bind
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
475 12 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC(C)C)c2)cc1
CHEMBL1829173 ffar1_mouse Mouse Yes 8.8 EC50 = 1.5 nM Bind
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL4797858 ffar1_human Human No 8.8 EC50 = 1.5 nM Bind
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
570 9 1 4 7.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(c3ccccc3)c3ccccc34)cc2)cc1
CHEMBL4792075 ffar1_human Human No 8.8 EC50 = 1.6 nM Funct
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
481 8 1 4 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)o2)cc1
CHEMBL4165008 ffar1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
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
CHEMBL4300503 ffar1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
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
CHEMBL4166625 ffar1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1
CHEMBL4302869 ffar1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
443 7 1 4 6.0 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)ccn1
CHEMBL3265144 ffar1_human Human No 8.8 EC50 = 1.7 nM Funct
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
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
CHEMBL4787498 ffar1_rat Rat Yes 8.8 EC50 = 1.7 nM Bind
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
499 8 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)s2)cc1
CHEMBL4793371 ffar1_human Human No 8.8 EC50 = 1.7 nM Bind
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
505 8 1 3 6.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(C)c2)cc1
CHEMBL3883819 ffar1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL4162778 ffar1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL3883819 ffar1_human Human No 8.8 EC50 = 1.7 nM Funct
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
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL4162778 ffar1_human Human No 8.8 EC50 = 1.7 nM Funct
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
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL1829174 ffar1_human Human Yes 8.7 EC50 = 1.9 nM Bind
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL3896509 ffar1_human Human No 8.7 EC50 = 1.9 nM Bind
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
510 12 1 5 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccncc3)Cc3ccsc3)c2)cc1
CHEMBL3966739 ffar1_human Human No 8.7 EC50 = 1.9 nM Bind
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
459 11 1 4 6.1 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CC3)c2)cc1
CHEMBL4787010 ffar1_human Human No 8.7 EC50 = 1.9 nM Funct
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
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
CHEMBL4159022 ffar1_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1
CHEMBL4302640 ffar1_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
444 7 1 5 5.4 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)ccn1
CHEMBL4281133 ffar1_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
372 9 1 3 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OCCCOc2cccc(Cl)c2)cc1
CHEMBL514337 ffar1_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at GPR40Agonist activity at GPR40
402 6 1 3 6.1 CC#CC(CC(=O)O)c1ccc(OC2CCc3cc(-c4cccs4)ccc32)cc1
CHEMBL3954235 ffar1_human Human No 8.0 EC50 = 10 nM Funct
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
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
CHEMBL4203795 ffar1_human Human No 8.0 EC50 = 10 nM Funct
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
512 8 1 6 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(F)c3scc(-c4ccc(OC)cc4C)c3c2)cc1
CHEMBL604126 ffar1_human Human Yes 8.0 EC50 = 10 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F
CHEMBL611821 ffar1_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
432 6 2 4 5.9 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(C2CC2C(=O)O)cc1
CHEMBL3288358 ffar1_human Human No 8.0 EC50 = 10 nM Funct
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
375 7 1 3 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C)CC(=O)O)cn2)c1
CHEMBL3893141 ffar1_human Human No 8.0 EC50 = 10 nM Bind
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
523 12 1 5 5.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)S(=O)(=O)C3CC3)c2)cc1
CHEMBL2022256 ffar1_human Human No 8.0 EC50 = 10 nM Funct
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
494 9 1 4 7.1 Cc1cccc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1OCc1ccccc1
CHEMBL4783033 ffar1_human Human No 8.0 EC50 = 10 nM Funct
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
512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4781604 ffar1_human Human No 8.0 EC50 = 10 nM Bind
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
521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1
CHEMBL4208095 ffar1_rat Rat No 8.0 EC50 = 10 nM Funct
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
478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C)c(-c4ccccc4C)c3c2)cc1
CHEMBL3927863 ffar1_rat Rat No 8.0 EC50 = 10 nM Funct
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
358 8 1 3 4.4 CC#C[C@@H](CC(=O)O)c1ccc(OCCOc2cccc(Cl)c2)cc1
CHEMBL3930086 ffar1_human Human No 8.0 EC50 = 10.5 nM Funct
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
461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1
CHEMBL3975239 ffar1_human Human No 8.0 EC50 = 10.5 nM Funct
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
461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1
CHEMBL380884 ffar1_human Human No 8.0 EC50 = 11.0 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
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
CHEMBL4206969 ffar1_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL4214632 ffar1_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL4794233 ffar1_rat Rat No 7.0 EC50 = 100 nM Bind
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
512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1
CHEMBL1829173 ffar1_human Human Yes 7.0 EC50 = 100 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL207881 ffar1_human Human Yes 7.0 EC50 = 100 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1
CHEMBL3604043 ffar1_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
360 11 1 5 3.8 CCOC(CC(=O)O)c1ccc(OCc2cccc(OCOC)c2)cc1
CHEMBL4742099 ffar1_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL4746614 ffar1_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL4060840 ffar1_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4288867 ffar1_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
386 6 1 4 4.1 CC#CC(CC(=O)O)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1
CHEMBL4784555 ffar1_human Human No 7.0 EC50 = 100 nM Bind
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
538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1
CHEMBL1777872 ffar1_mouse Mouse No 7.0 EC50 = 100 nM Funct
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
431 6 1 4 6.2 CC#CC(CC(=O)O)c1ccc(OC2CCCc3nc(-c4ccc(C)cc4)sc32)cc1
CHEMBL203520 ffar1_human Human No 7.0 EC50 = 100 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
361 8 2 3 5.4 CC(Cc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)C(=O)O
CHEMBL205263 ffar1_human Human No 7.0 EC50 = 100 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
461 8 2 4 6.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(=O)NC(C)C)cc1
CHEMBL233835 ffar1_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
289 6 2 2 4.0 O=C(O)CCc1ccc(NCc2ccc(Cl)cc2)cc1
CHEMBL2315546 ffar1_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
326 4 1 1 4.8 O=C(O)CCc1ccc(C#Cc2ccccc2-c2ccccc2)cc1
CHEMBL2315557 ffar1_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
264 4 1 1 3.5 O=C(O)CCCc1ccc(C#Cc2ccccc2)cc1
CHEMBL4754718 ffar1_human Human No 6.0 EC50 = 1000 nM Funct
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
508 13 1 5 6.0 COc1ccc(CN(C)CC(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL1688455 ffar1_human Human Yes 5.0 EC50 = 10000 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1
CHEMBL4213909 ffar1_human Human Yes 5.0 EC50 = 10000 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1
CHEMBL4085843 ffar1_human Human No 5.0 EC50 = 10000 nM Funct
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
304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1
CHEMBL3287569 ffar1_human Human Yes 5.0 EC50 = 10000 nM Bind
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
460 8 1 4 6.2 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nccn3C)cc2)c1
CHEMBL602867 ffar1_human Human No 7.0 EC50 = 101 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
367 4 1 4 4.7 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cc3Cl)cc2)S1
CHEMBL3883449 ffar1_human Human No 7.0 EC50 = 101 nM Funct
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
490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F
CHEMBL4161206 ffar1_human Human No 6.0 EC50 = 1016 nM Funct
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
349 5 2 2 4.8 O=C(O)CCc1ccc2[nH]c(-c3ccccc3OC(F)(F)F)cc2c1
CHEMBL3780725 ffar1_human Human No 7.0 EC50 = 102 nM Bind
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
381 6 1 5 4.6 Cc1nc(-c2ccccc2)sc1COc1ccc2c(c1)OCC2CC(=O)O
CHEMBL3798992 ffar1_human Human No 7.0 EC50 = 102 nM Funct
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
453 9 1 5 6.0 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OC2CCCC2)c1
CHEMBL4538821 ffar1_human Human No 6.0 EC50 = 1020 nM Funct
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
466 7 1 5 5.0 O=C(O)CC1(c2ccc(OC[C@H]3COc4ccc(-c5ccc(Cl)cc5)cc4O3)cc2)COC1
CHEMBL4218014 ffar1_human Human No 6.0 EC50 = 1020 nM Funct
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
475 9 2 5 5.3 O=C(O)CCc1ccc(NC(=O)c2nnc(CC(c3ccccc3)c3ccccc3F)s2)cc1
CHEMBL4085843 ffar1_human Human No 5.0 EC50 = 10268 nM Funct
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
304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1
CHEMBL3628763 ffar1_human Human No 7.0 EC50 = 103.6 nM Funct
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
454 11 1 5 5.2 COCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1
CHEMBL4225643 ffar1_human Human No 7.0 EC50 = 103.7 nM Funct
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
392 6 1 5 4.2 Cc1nn(C)c(C)c1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1
CHEMBL4277516 ffar1_human Human No 6.0 EC50 = 1030 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
415 7 1 6 4.2 O=C(O)CC(c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1)c1cnco1
CHEMBL4168422 ffar1_human Human No 6.0 EC50 = 1031 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1
CHEMBL4300181 ffar1_human Human No 6.0 EC50 = 1031 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
462 7 1 5 5.6 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c(F)cn1
CHEMBL1829173 ffar1_human Human Yes 7.0 EC50 = 104 nM Bind
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL1777855 ffar1_mouse Mouse No 7.0 EC50 = 104 nM Funct
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
432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F
CHEMBL3968947 ffar1_human Human No 6.0 EC50 = 1042 nM Funct
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
374 7 1 3 5.1 O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1
CHEMBL4633625 ffar1_human Human No 6.0 EC50 = 1046 nM Bind
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4cccc(C)c4)cn3c2)cc1
CHEMBL3265139 ffar1_human Human No 7.0 EC50 = 105 nM Bind
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
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
CHEMBL2385464 ffar1_human Human No 7.0 EC50 = 105 nM Bind
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
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
CHEMBL3781162 ffar1_human Human No 7.0 EC50 = 105 nM Bind
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
415 6 1 5 5.3 Cc1nc(-c2ccc(Cl)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O
CHEMBL4163182 ffar1_human Human No 7.0 EC50 = 105 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1
CHEMBL4301725 ffar1_human Human No 7.0 EC50 = 105 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
461 7 1 4 6.2 COc1cc(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c(F)cn1
CHEMBL2381292 ffar1_human Human No 7.0 EC50 = 105.1 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
408 3 1 4 4.1 O=C(O)C[C@@H]1COc2cc3c(cc21)OCC(c1cc(F)cc(Br)c1)O3
CHEMBL3628757 ffar1_human Human No 7.0 EC50 = 105.8 nM Funct
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
438 10 1 4 5.9 CCCOc1cc(C)c(-c2cccc(COc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1
CHEMBL2058520 ffar1_human Human No 5.0 EC50 = 10500 nM Funct
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
346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1
CHEMBL4210970 ffar1_human Human No 5.0 EC50 = 10500 nM Funct
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
346 7 1 2 5.3 Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1
CHEMBL4176612 ffar1_human Human No 7.0 EC50 = 106 nM Funct
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
453 7 1 3 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCc4ccccc4C3)cc2)cc1
CHEMBL3806208 ffar1_human Human No 6.0 EC50 = 1060 nM Funct
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
383 8 2 6 3.4 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3ccccc3)s2)cc1
CHEMBL3805377 ffar1_human Human No 5.0 EC50 = 10620 nM Funct
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
417 8 2 6 4.0 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(Cl)c3)s2)cc1
CHEMBL4218110 ffar1_human Human No 7.0 EC50 = 107 nM Funct
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
456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1
CHEMBL485738 ffar1_human Human No 7.0 EC50 = 107.2 nM Funct
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
264 3 1 1 3.4 Cc1ccc(C#Cc2ccc(CCC(=O)O)cc2)cc1
CHEMBL3600997 ffar1_human Human Yes 6.0 EC50 = 1070 nM Funct
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
341 7 1 4 4.1 O=C(O)CCc1ccc(OCc2ncc(-c3cccc(F)c3)o2)cc1
CHEMBL1829163 ffar1_human Human No 6.0 EC50 = 1071.5 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
341 4 1 2 4.5 Cc1ccccc1-c1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1
CHEMBL1773259 ffar1_human Human No 6.0 EC50 = 1071.5 nM Funct
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
331 7 2 2 5.0 O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1
CHEMBL3265144 ffar1_human Human No 7.0 EC50 = 108 nM Bind
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
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
CHEMBL1777866 ffar1_human Human No 7.0 EC50 = 108 nM Funct
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
383 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ncc(C(F)(F)F)cc2Cl)cc1
CHEMBL3927519 ffar1_human Human Yes 7.0 EC50 = 108 nM Bind
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
439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1
CHEMBL4210878 ffar1_rat Rat No 7.0 EC50 = 108 nM Funct
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
498 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(Cl)c3scc(-c4ccccc4C)c3c2)cc1
CHEMBL3616657 ffar1_human Human No 7.0 EC50 = 108.2 nM Funct
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
333 7 2 4 2.6 Cc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1
CHEMBL598040 ffar1_human Human No 6.0 EC50 = 1082 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
311 5 1 3 3.4 O=C1NC(=O)C(Cc2ccc(CCc3ccccc3)cc2)S1
CHEMBL603065 ffar1_human Human No 6.0 EC50 = 1087 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
314 4 1 5 3.1 Cc1cccnc1Oc1ccc(CC2SC(=O)NC2=O)cc1
CHEMBL4172250 ffar1_human Human No 7.0 EC50 = 109 nM Funct
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
473 8 2 4 5.7 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)s2)cc1
CHEMBL3629046 ffar1_human Human No 7.0 EC50 = 109.5 nM Funct
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
454 11 2 5 4.9 Cc1cc(OCCCO)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1
CHEMBL2058530 ffar1_human Human No 7.0 EC50 = 109.7 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
366 7 1 2 5.6 O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1
CHEMBL446575 ffar1_human Human No 6.0 EC50 = 1096.5 nM Funct
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
265 3 2 2 2.7 Nc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1
CHEMBL1829147 ffar1_human Human No 5.0 EC50 = 10964.8 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
296 4 1 4 2.4 O=C(O)CCc1ccc(C#Cc2ncccc2[N+](=O)[O-])cc1
CHEMBL4784555 ffar1_mouse Mouse No 8.0 EC50 = 11 nM Bind
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
538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1
CHEMBL4790921 ffar1_rat Rat No 8.0 EC50 = 11 nM Bind
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
498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4748702 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
507 12 1 4 7.3 COc1ccc(CCCC(C)(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL4203974 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
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
CHEMBL3287570 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
461 8 1 5 5.6 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3ncnn3C)cc2)c1
CHEMBL3927519 ffar1_human Human Yes 8.0 EC50 = 11 nM Funct
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
439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1
CHEMBL4764729 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1
CHEMBL4787007 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
515 10 1 4 7.6 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1
CHEMBL4785057 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1
CHEMBL4800563 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
536 9 1 4 6.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C(C)C)c3ccccc34)cc2)cc1
CHEMBL4783033 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL1829173 ffar1_human Human Yes 8.0 EC50 = 11 nM Bind
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL4791842 ffar1_human Human Yes 8.0 EC50 = 11 nM Bind
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
493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1
CHEMBL3427712 ffar1_rat Rat Yes 8.0 EC50 = 11 nM Funct
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
394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c2cccc3C(F)(F)F)cc1
CHEMBL4170346 ffar1_human Human No 8.0 EC50 = 11 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1
CHEMBL4565467 ffar1_human Human No 8.0 EC50 = 11 nM Funct
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
443 8 1 4 6.0 COc1cc(-c2ccc3c(c2)CC[C@H]3Oc2cccc([C@H](C3CC3)[C@H](C)C(=O)O)c2)ccn1
CHEMBL3798044 ffar1_human Human No 8.0 EC50 = 11.1 nM Funct
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
387 7 1 4 4.8 Cc1noc(C)c1-c1ccc(F)c(COc2ccc(CCC(=O)O)c(F)c2)c1
CHEMBL1773261 ffar1_human Human Yes 8.0 EC50 = 11.2 nM Bind
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
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL2381289 ffar1_human Human No 8.0 EC50 = 11.3 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
380 3 1 4 4.2 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(C(F)(F)F)c1)O3
CHEMBL2152070 ffar1_rat Rat Yes 7.9 EC50 = 11.4 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL4575598 ffar1_human Human No 7.9 EC50 = 11.6 nM Funct
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
409 9 2 4 5.3 CCOc1ccc(-c2cccc(CNc3ccc(OCC(=O)O)c(F)c3)c2)c(C)c1
CHEMBL3930086 ffar1_human Human No 7.9 EC50 = 11.6 nM Funct
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
461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1
CHEMBL3975239 ffar1_human Human No 7.9 EC50 = 11.6 nM Funct
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
461 11 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C(C)C)c2)cc1
CHEMBL4203561 ffar1_human Human No 7.0 EC50 = 110 nM Funct
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
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
CHEMBL4794904 ffar1_mouse Mouse No 7.0 EC50 = 110 nM Bind
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
487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl
CHEMBL1939650 ffar1_human Human No 7.0 EC50 = 110 nM Funct
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
324 7 1 3 3.9 CC#CC(CC(=O)O)c1ccc(OCc2cccc(OC)c2)cc1
CHEMBL4091211 ffar1_human Human No 7.0 EC50 = 110 nM Funct
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
391 7 1 4 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(C(C#N)CC(=O)O)s2)c1
CHEMBL4083365 ffar1_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
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
CHEMBL4090240 ffar1_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
393 5 1 3 5.3 Cc1cccc(Oc2ccc(N3C[C@@H](C(F)(F)F)C[C@H]3CC(=O)O)cc2)c1C
CHEMBL4073270 ffar1_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4105324 ffar1_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4283655 ffar1_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)ccc3O2)cc1
CHEMBL3628762 ffar1_human Human No 7.0 EC50 = 110.3 nM Funct
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
396 7 2 4 4.9 Cc1cc(O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)c(F)c2)c1
CHEMBL1688456 ffar1_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccccc2Oc2ccccc2)cc1
CHEMBL2152071 ffar1_human Human Yes 6.0 EC50 = 1100 nM Funct
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
514 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1
CHEMBL1939637 ffar1_human Human Yes 6.0 EC50 = 1100 nM Funct
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
286 7 1 3 3.3 COc1ccc(COc2ccc(CCC(=O)O)cc2)cc1
CHEMBL4061093 ffar1_mouse Mouse No 6.0 EC50 = 1100 nM Funct
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
323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1
CHEMBL4101348 ffar1_mouse Mouse No 6.0 EC50 = 1100 nM Funct
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
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
CHEMBL4076004 ffar1_mouse Mouse No 6.0 EC50 = 1100 nM Funct
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
371 6 1 4 4.7 CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12
CHEMBL3288352 ffar1_rat Rat No 6.0 EC50 = 1100 nM Funct
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
375 7 1 3 5.3 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(C)n2)c1
CHEMBL4285594 ffar1_human Human No 6.0 EC50 = 1100 nM Funct
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
344 5 1 3 4.5 O=C(O)C#Cc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL4059947 ffar1_human Human No 5.0 EC50 = 11000 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
407 6 1 3 5.8 O=C(O)CC1CCCCCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1
CHEMBL4082975 ffar1_human Human No 5.0 EC50 = 11000 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
385 6 1 2 5.4 Cc1ccccc1Cc1ccc(N2CC[C@H](c3ccccc3)[C@H]2CC(=O)O)cc1
CHEMBL4250132 ffar1_human Human No 5.0 EC50 = 11010 nM Funct
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
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
CHEMBL8739 ffar1_human Human Yes 5.0 EC50 = 11090 nM Funct
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
278 13 1 1 5.7 CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O
CHEMBL2381283 ffar1_human Human No 7.0 EC50 = 111.1 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1cccc(Br)c1)O3
CHEMBL3601006 ffar1_human Human Yes 6.0 EC50 = 1110 nM Funct
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
392 7 1 5 4.4 O=C(O)CCc1ccc(OCc2nc(-c3cccc(C(F)(F)F)c3)no2)cc1
CHEMBL4071849 ffar1_human Human No 6.0 EC50 = 1110 nM Funct
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
558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1
CHEMBL4116363 ffar1_human Human No 6.0 EC50 = 1110 nM Funct
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
558 12 1 6 6.2 Cc1ccnc(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)c1
CHEMBL4463798 ffar1_human Human No 7.0 EC50 = 112 nM Bind
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
391 7 1 5 4.4 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1
CHEMBL3754173 ffar1_human Human No 7.0 EC50 = 112 nM Bind
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
496 9 1 5 6.2 Cn1ccnc1[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccccc3OC(F)(F)F)c2)cc1
CHEMBL1829157 ffar1_human Human No 6.0 EC50 = 1122.0 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
265 3 1 2 2.8 Cc1cc(C#Cc2ccc(CCC(=O)O)cc2)ccn1
CHEMBL205090 ffar1_human Human No 6.0 EC50 = 1122.0 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
361 9 2 3 5.5 O=C(O)CCCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL3924759 ffar1_human Human No 6.0 EC50 = 1126 nM Funct
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
334 8 1 3 4.6 CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1
CHEMBL599067 ffar1_human Human Yes 5.0 EC50 = 11270 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
299 4 1 4 3.4 O=C1NC(=O)C(Cc2ccccc2Oc2ccccc2)S1
CHEMBL3780211 ffar1_human Human No 7.0 EC50 = 113 nM Bind
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
449 6 1 5 5.7 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc2c(c1)OCC2CC(=O)O
CHEMBL1777855 ffar1_human Human No 7.0 EC50 = 113 nM Funct
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
432 7 1 3 5.8 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1F
CHEMBL4171827 ffar1_human Human No 7.0 EC50 = 113 nM Funct
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
506 8 1 5 5.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)s2)cc1
CHEMBL3601007 ffar1_human Human Yes 6.0 EC50 = 1130 nM Funct
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
324 7 1 5 3.3 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)cc1
CHEMBL4212573 ffar1_human Human No 6.0 EC50 = 1130 nM Funct
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
411 8 2 6 4.0 Cc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1C
CHEMBL4130213 ffar1_human Human No 5.0 EC50 = 11330 nM Funct
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
501 9 1 5 5.8 O=C1NC(=O)C(Cc2ccc(OCCOC(c3ccccc3)c3ccc(C(F)(F)F)cc3)cc2)S1
CHEMBL4169459 ffar1_human Human No 6.0 EC50 = 1136 nM Funct
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
489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccnc4)CC3)s2)cc1
CHEMBL3265141 ffar1_human Human No 6.9 EC50 = 114 nM Bind
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
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
CHEMBL1777873 ffar1_human Human No 6.9 EC50 = 114 nM Funct
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
272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1
CHEMBL3798642 ffar1_human Human No 6.9 EC50 = 114 nM Funct
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
437 7 1 4 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(C(F)(F)F)c1
CHEMBL4162561 ffar1_human Human No 6.9 EC50 = 114 nM Funct
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
500 8 1 4 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(F)cc4)CC3)cc2)cc1
CHEMBL382341 ffar1_human Human No 6.9 EC50 = 114.8 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
400 8 1 3 5.6 O=C(CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1)N1CCCC1
CHEMBL4091587 ffar1_human Human No 5.9 EC50 = 1140 nM Funct
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
573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1
CHEMBL4117177 ffar1_human Human No 5.9 EC50 = 1140 nM Funct
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
573 12 1 7 5.9 Cc1cnc(C)c(OCCC2CCOC3(CCN(Cc4ccc(COc5ccc(CCC(=O)O)cc5)cc4)CC3)C2)n1
CHEMBL2058524 ffar1_human Human No 5.9 EC50 = 1148.2 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
400 7 1 2 6.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1
CHEMBL234834 ffar1_human Human Yes 5.9 EC50 = 1148.2 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
255 6 2 2 3.3 O=C(O)CCc1ccc(NCc2ccccc2)cc1
CHEMBL121 ffar1_human Human Yes 4.9 EC50 = 11481.5 nM Bind
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
357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C
CHEMBL108766 ffar1_human Human Yes 4.9 EC50 = 11481.5 nM Funct
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
200 10 1 1 4.0 CCCCCCCCCCCC(=O)O
CHEMBL3186422 ffar1_human Human Yes 4.9 EC50 = 11481.5 nM Funct
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
298 15 2 2 5.1 CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O
CHEMBL3616660 ffar1_human Human No 6.9 EC50 = 115.6 nM Funct
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
361 8 2 4 3.4 CC(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1
CHEMBL3759212 ffar1_human Human No 5.9 EC50 = 1150 nM Funct
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
417 6 1 4 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(CC3SC(=O)NC3=O)cc2)c1
CHEMBL4101323 ffar1_human Human Yes 4.9 EC50 = 11588 nM Funct
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
304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl
CHEMBL3890182 ffar1_human Human No 5.9 EC50 = 1160 nM Funct
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
529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1
CHEMBL3990066 ffar1_human Human No 5.9 EC50 = 1160 nM Funct
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
529 11 1 5 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3ccccc3)CCO4)cc2)cc1
CHEMBL4075819 ffar1_human Human No 6.9 EC50 = 117 nM Funct
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
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
CHEMBL4294582 ffar1_human Human No 5.9 EC50 = 1170 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
425 7 1 5 4.6 O=C(O)CC(c1ccncc1)c1ccc(OCC2COc3ccc(Cl)cc3O2)cc1
CHEMBL4212664 ffar1_human Human No 5.9 EC50 = 1170 nM Funct
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
411 9 2 6 3.9 CCc1ccc(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)cc1
CHEMBL367149 ffar1_human Human Yes 4.9 EC50 = 11700 nM Funct
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
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
CHEMBL3931296 ffar1_human Human No 6.9 EC50 = 118.3 nM Bind
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
419 10 2 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CNCc3ccsc3)c2)cc1
CHEMBL3781145 ffar1_human Human No 6.9 EC50 = 118.5 nM Funct
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
395 6 1 5 5.0 Cc1cccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)c1
CHEMBL4080516 ffar1_human Human No 5.9 EC50 = 1180 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4065397 ffar1_human Human No 4.9 EC50 = 11800 nM Funct
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
368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C
CHEMBL598674 ffar1_human Human No 5.9 EC50 = 1189 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
333 4 1 4 4.0 O=C1NC(=O)C(Cc2ccc(Oc3ccccc3Cl)cc2)S1
CHEMBL3927519 ffar1_human Human Yes 6.9 EC50 = 119 nM Funct
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
439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1
CHEMBL3805903 ffar1_human Human No 5.9 EC50 = 1190 nM Funct
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
401 8 2 6 3.5 O=C(O)CCc1ccc(OCc2nnc(C(=O)Nc3cccc(F)c3)s2)cc1
CHEMBL4206318 ffar1_human Human No 7.9 EC50 = 12 nM Funct
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
600 12 1 8 6.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCCCS(C)(=O)=O)cc4C)c3c2)cc1
CHEMBL3604037 ffar1_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
386 8 1 3 5.3 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)cc1F
CHEMBL3604047 ffar1_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)cc2)cc1
CHEMBL3604061 ffar1_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
354 8 1 3 4.9 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(CC)cccc32)cc1
CHEMBL3604062 ffar1_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
368 8 1 3 5.4 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C(C)C)cccc32)cc1
CHEMBL3800362 ffar1_human Human No 7.9 EC50 = 12 nM Funct
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
383 7 1 4 5.0 Cc1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(-c2c(C)noc2C)c1
CHEMBL3287571 ffar1_human Human No 7.9 EC50 = 12 nM Bind
Agonist activity at human GPR40 expressed in CHO cells by aequorin assayAgonist activity at human GPR40 expressed in CHO cells by aequorin assay
462 8 1 6 5.0 Cc1cc(Cl)ccc1-c1cccc(COc2ccc([C@H](CC(=O)O)c3nnnn3C)cc2)c1
CHEMBL4794409 ffar1_human Human Yes 7.9 EC50 = 12 nM Funct
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
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
CHEMBL3957744 ffar1_human Human No 7.9 EC50 = 12 nM Bind
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
463 12 2 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(CCO)Cc3ccsc3)c2)cc1
CHEMBL2048614 ffar1_human Human No 7.9 EC50 = 12 nM Funct
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
390 8 1 3 5.6 COc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1
CHEMBL4780641 ffar1_human Human No 7.9 EC50 = 12 nM Funct
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
508 8 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccccc34)cc2)cc1
CHEMBL4795763 ffar1_human Human No 7.9 EC50 = 12 nM Funct
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
498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ncc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4782004 ffar1_human Human Yes 7.9 EC50 = 12 nM Funct
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
497 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL1829174 ffar1_human Human Yes 7.9 EC50 = 12 nM Bind
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL4218348 ffar1_rat Rat No 7.9 EC50 = 12 nM Funct
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
532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1
CHEMBL207753 ffar1_human Human No 7.9 EC50 = 12.3 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL4740846 ffar1_human Human No 7.9 EC50 = 12.4 nM Funct
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
516 10 1 5 7.0 COc1ccc(F)c(-c2cnc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c1
CHEMBL203126 ffar1_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
400 8 2 3 5.7 CC(C)NC(=O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL1773261 ffar1_human Human Yes 7.9 EC50 = 12.9 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL381958 ffar1_human Human No 7.9 EC50 = 12.9 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
419 7 2 4 5.2 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1CNc1ccc(CCC(N)=O)cc1
CHEMBL1688463 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
346 7 1 2 5.3 Cc1ccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)cc1
CHEMBL1688483 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
350 7 1 2 5.1 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3F)c2)cc1
CHEMBL3264817 ffar1_human Human No 6.9 EC50 = 120 nM Bind
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
515 10 1 4 7.6 COc1cc(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c(F)cn1
CHEMBL4205882 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL4786299 ffar1_mouse Mouse No 6.9 EC50 = 120 nM Bind
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
509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL4792027 ffar1_rat Rat Yes 6.9 EC50 = 120 nM Bind
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
491 8 1 3 6.4 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1
CHEMBL4443509 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
446 7 1 4 5.3 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(F)cc4)cc3O2)cc1
CHEMBL4451050 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
456 7 1 4 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4c(C)cccc4C)cc3O2)cc1
CHEMBL596667 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
352 4 1 5 3.9 Cc1cc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc(C)c1C#N
CHEMBL1939641 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
340 8 1 3 4.8 COc1ccc(COc2ccc(C(C=C(C)C)CC(=O)O)cc2)cc1
CHEMBL3604060 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
341 7 1 5 4.5 CCO[C@@H](CC(=O)O)c1ccc(Oc2noc3c(C)cccc23)cc1
CHEMBL3288356 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
391 8 1 4 4.6 COC(Cc1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1)C(=O)O
CHEMBL4748658 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL4760668 ffar1_human Human No 6.9 EC50 = 120 nM Funct
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
451 10 1 4 6.1 COc1ccc(C(C)C)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL4073525 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1
CHEMBL4095599 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1
CHEMBL4279126 ffar1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
366 6 1 4 3.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(C)cc3O2)cc1
CHEMBL3752026 ffar1_human Human No 6.9 EC50 = 120 nM Bind
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
483 8 1 4 7.0 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1nccs1
CHEMBL1829165 ffar1_human Human No 6.9 EC50 = 120.2 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
283 3 1 2 2.9 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1F
CHEMBL1688482 ffar1_human Human No 6.9 EC50 = 120.2 nM Funct
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
362 8 1 3 5.0 COc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1
CHEMBL2381298 ffar1_human Human No 6.9 EC50 = 120.7 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
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
CHEMBL3601008 ffar1_human Human Yes 5.9 EC50 = 1200 nM Funct
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
358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3Cl)no2)cc1
CHEMBL2151292 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
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
380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3cccc(CCC(=O)O)c3)cc2)c1
CHEMBL2151302 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
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
512 9 1 3 8.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)c4ccccc4)c3)cc2C(C)(C)C)c1
CHEMBL207881 ffar1_human Human Yes 5.9 EC50 = 1200 nM Funct
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
347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1
CHEMBL1939642 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
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
326 7 1 3 4.5 COc1ccc(COc2ccc(C(CC(=O)O)=C(C)C)cc2)cc1
CHEMBL1939651 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
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
370 7 1 2 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(-c3ccccc3)cc2)cc1
CHEMBL4097617 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
428 7 1 5 4.3 COc1ccc(F)c(N2CCC(Oc3ccc(N4CCC[C@@H]4CC(=O)O)cc3)CC2)c1
CHEMBL4101071 ffar1_mouse Mouse No 5.9 EC50 = 1200 nM Funct
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
391 5 1 4 5.1 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12
CHEMBL4248694 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
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
505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21
CHEMBL4300846 ffar1_human Human No 5.9 EC50 = 1200 nM Funct
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
505 8 1 4 6.4 O=C(O)C[C@@H]1COc2cc(OCc3cccc(-c4ccc5c(c4)CCN(Cc4ccccc4)C5)c3)ccc21
CHEMBL4170346 ffar1_human Human No 5.9 EC50 = 1206 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
447 7 1 4 5.9 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c(F)cn1
CHEMBL4175260 ffar1_human Human No 5.9 EC50 = 1207 nM Funct
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
283 4 2 1 4.0 O=C(O)CCc1ccc2[nH]c(-c3ccccc3F)cc2c1
CHEMBL599280 ffar1_human Human No 6.9 EC50 = 121 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
327 4 1 4 4.0 Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)c(C)c1
CHEMBL3353261 ffar1_human Human No 6.9 EC50 = 121.1 nM Funct
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
498 12 1 6 4.8 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(OCC(=O)O)cc2)c1
CHEMBL3616662 ffar1_human Human No 6.9 EC50 = 121.7 nM Funct
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
375 7 2 4 3.6 CC(C)(C)c1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1
CHEMBL4091100 ffar1_human Human No 5.9 EC50 = 1210 nM Funct
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
625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1
CHEMBL4117940 ffar1_human Human No 5.9 EC50 = 1210 nM Funct
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
625 13 1 7 6.7 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3nc(C5CC5)nc5c3CCC5)CCO4)cc2)cc1
CHEMBL3884609 ffar1_human Human No 5.9 EC50 = 1210 nM Funct
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
530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1
CHEMBL2381301 ffar1_human Human No 6.9 EC50 = 122.6 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
538 9 1 7 4.9 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(C2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1
CHEMBL254859 ffar1_human Human Yes 4.9 EC50 = 12200 nM Funct
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
385 7 1 4 4.7 O=C(O)CCCCCN1C(=O)/C(=C\c2cccc3ccccc23)SC1=S
CHEMBL3883407 ffar1_human Human No 5.9 EC50 = 1227 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1
CHEMBL3883532 ffar1_human Human No 6.9 EC50 = 123 nM Funct
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
540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1
CHEMBL2315541 ffar1_human Human No 6.9 EC50 = 123.0 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
278 3 1 1 3.7 Cc1ccc(C)c(C#Cc2ccc(CCC(=O)O)cc2)c1
CHEMBL4207283 ffar1_human Human No 6.9 EC50 = 123.0 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
434 7 1 4 6.2 COc1cc(C)c(-c2cccc(COc3ccc4c(c3)SCC4CC(=O)O)c2)c(C)c1
CHEMBL3781779 ffar1_human Human No 6.9 EC50 = 123.4 nM Funct
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
411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1
CHEMBL233223 ffar1_human Human No 4.9 EC50 = 12302.7 nM Funct
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
317 6 2 2 4.6 O=C(O)Cc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1
CHEMBL597436 ffar1_human Human No 6.9 EC50 = 124 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
313 4 1 4 3.7 Cc1ccccc1Oc1ccc(CC2SC(=O)NC2=O)cc1
CHEMBL1777876 ffar1_human Human No 6.9 EC50 = 124 nM Funct
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
455 6 1 5 4.8 CC#CC(c1ccc(Oc2ccc(C(F)(F)F)cc2OC(F)F)cc1)C1OC(=O)NC1=O
CHEMBL1777873 ffar1_mouse Mouse No 6.9 EC50 = 124 nM Funct
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
272 5 1 2 3.6 CC#CC(CC(=O)O)c1ccc(OC2CCCC2)cc1
CHEMBL1777865 ffar1_mouse Mouse No 5.9 EC50 = 1248 nM Funct
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
398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1
CHEMBL2381304 ffar1_human Human No 6.9 EC50 = 125 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
576 9 1 7 5.4 CS(=O)(=O)CCCOc1ccc(-c2cc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)ccc2F)c(Cl)c1
CHEMBL4205241 ffar1_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
484 11 1 6 4.4 COCCOc1cc(C)c(-c2cccc(COc3ccc(S(=O)(=O)CC(=O)O)cc3)c2)c(C)c1
CHEMBL1773260 ffar1_human Human No 6.9 EC50 = 125.9 nM Funct
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
345 7 2 2 5.3 Cc1ccc(-c2cccc(CNc3ccc(CCC(=O)O)cc3)c2)cc1
CHEMBL380719 ffar1_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
361 8 2 3 5.7 CC(CC(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL3883983 ffar1_human Human No 5.9 EC50 = 1252 nM Funct
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
416 6 1 2 6.9 CC1(C)CCC=C1c1cccc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)c1
CHEMBL4647211 ffar1_human Human No 5.9 EC50 = 1258 nM Bind
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
410 7 1 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4ccccc4)nc3c2)cc1
CHEMBL393661 ffar1_human Human No 5.9 EC50 = 1258.9 nM Funct
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
285 7 2 3 3.3 COc1ccc(CNc2ccc(CCC(=O)O)cc2)cc1
CHEMBL473459 ffar1_human Human Yes 5.9 EC50 = 1258.9 nM Funct
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
252 3 1 2 2.6 O=C(O)COc1ccc(C#Cc2ccccc2)cc1
CHEMBL4065397 ffar1_human Human No 4.9 EC50 = 12589.3 nM Funct
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
368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C
CHEMBL4083440 ffar1_human Human No 4.9 EC50 = 12589.3 nM Funct
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
370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1
CHEMBL4101323 ffar1_human Human Yes 4.9 EC50 = 12589.3 nM Funct
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
304 6 1 2 4.2 Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl
CHEMBL1773250 ffar1_human Human No 4.9 EC50 = 12589.3 nM Funct
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
382 6 1 2 3.9 O=C(O)CCc1ccc(OCc2ccccc2)c(I)c1
CHEMBL3601049 ffar1_human Human Yes 5.9 EC50 = 1260 nM Funct
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
402 7 1 5 4.1 O=C(O)CCc1ccc(OCc2nc(-c3cccc(Br)c3)no2)cc1
CHEMBL4063785 ffar1_human Human No 5.9 EC50 = 1260 nM Funct
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
585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1
CHEMBL4116078 ffar1_human Human No 5.9 EC50 = 1260 nM Funct
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
585 12 1 7 5.8 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3ncnc5c3CCC5)CCO4)cc2)cc1
CHEMBL1777860 ffar1_mouse Mouse No 6.9 EC50 = 127 nM Funct
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
362 5 1 2 5.4 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)cc2C)cc1
CHEMBL4159416 ffar1_human Human No 6.9 EC50 = 127 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL4300796 ffar1_human Human No 6.9 EC50 = 127 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL3883380 ffar1_human Human No 6.9 EC50 = 127 nM Funct
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
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
CHEMBL4435837 ffar1_human Human No 6.9 EC50 = 127 nM Funct
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
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
CHEMBL3976110 ffar1_human Human No 5.9 EC50 = 1270 nM Funct
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
581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1
CHEMBL3990146 ffar1_human Human No 5.9 EC50 = 1270 nM Funct
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
581 10 1 4 7.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(Cc3ccc(C(F)(F)F)cc3)CCO4)cc2)cc1
CHEMBL4072869 ffar1_human Human No 5.9 EC50 = 1270 nM Funct
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
559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1
CHEMBL4116895 ffar1_human Human No 5.9 EC50 = 1270 nM Funct
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
559 12 1 7 5.6 Cc1nccnc1OCCC1CCOC2(CCN(Cc3ccc(COc4ccc(CCC(=O)O)cc4)cc3)CC2)C1
CHEMBL3265147 ffar1_human Human No 6.9 EC50 = 128 nM Bind
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
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
CHEMBL4212041 ffar1_rat Rat No 6.9 EC50 = 128 nM Funct
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
542 8 1 7 5.7 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(S(C)(=O)=O)c(-c4ccccc4C)c3c2)cc1
CHEMBL4218236 ffar1_human Human No 6.9 EC50 = 128.8 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
399 7 1 5 3.5 Cc1ccc(C)n1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1
CHEMBL3805879 ffar1_human Human No 5.9 EC50 = 1280 nM Funct
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
371 6 2 5 3.6 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccc(F)cc3)c2)s1
CHEMBL1829173 ffar1_human Human Yes 7.9 EC50 = 13 nM Funct
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL1829173 ffar1_human Human Yes 7.9 EC50 = 13 nM Funct
Agonist activity at GPR40 (unknown origin) by calcium flux assayAgonist activity at GPR40 (unknown origin) by calcium flux assay
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL2152070 ffar1_human Human Yes 7.9 EC50 = 13 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL2047157 ffar1_human Human No 7.9 EC50 = 13 nM Funct
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
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
CHEMBL4207592 ffar1_human Human No 7.9 EC50 = 13 nM Funct
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
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
CHEMBL4209834 ffar1_human Human No 7.9 EC50 = 13 nM Funct
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
518 7 1 5 7.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccccc4C(F)(F)F)c3c2)cc1
CHEMBL3603843 ffar1_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3cc(C(F)(F)F)ccc32)cc1
CHEMBL3604052 ffar1_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
368 8 1 3 5.1 CCOC(CC(=O)O)c1ccc(OCc2ccc(F)c3ccccc23)cc1
CHEMBL3604057 ffar1_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
386 8 1 3 5.0 CCO[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(F)(F)F)cc2F)cc1
CHEMBL3604063 ffar1_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
366 8 1 3 5.2 CCO[C@@H](CC(=O)O)c1ccc(O[C@@H]2CCc3c(C4CC4)cccc32)cc1
CHEMBL207881 ffar1_human Human Yes 7.9 EC50 = 13 nM Funct
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
347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1
CHEMBL3931755 ffar1_human Human No 7.9 EC50 = 13 nM Funct
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
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
CHEMBL2048617 ffar1_human Human No 7.9 EC50 = 13 nM Funct
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
448 12 1 4 6.0 CCOCCOc1cc(C)c(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c(C)c1
CHEMBL1829173 ffar1_mouse Mouse Yes 7.9 EC50 = 13 nM Funct
Agonist activity at mouse GPR40Agonist activity at mouse GPR40
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL4171104 ffar1_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1
CHEMBL4302546 ffar1_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cn2)c1
CHEMBL1829173 ffar1_human Human Yes 7.9 EC50 = 13 nM Bind
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL207753 ffar1_human Human No 7.9 EC50 = 13.5 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
359 7 2 3 5.3 O=C(O)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL2381282 ffar1_human Human No 7.9 EC50 = 13.5 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
390 3 1 4 3.9 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1cccc(Br)c1)O3
CHEMBL1777878 ffar1_human Human No 6.9 EC50 = 130 nM Funct
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
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
CHEMBL3288350 ffar1_human Human No 6.9 EC50 = 130 nM Funct
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
362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1
CHEMBL4277181 ffar1_human Human No 6.9 EC50 = 130 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
382 7 1 5 3.5 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(OC)cc3O2)cc1
CHEMBL4784555 ffar1_human Human No 6.9 EC50 = 130 nM Funct
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
538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1
CHEMBL3288351 ffar1_rat Rat No 6.9 EC50 = 130 nM Funct
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
375 7 1 3 5.3 Cc1cc(OCc2cccc(-c3c(C)cccc3C)c2)ncc1CCC(=O)O
CHEMBL3288359 ffar1_rat Rat No 6.9 EC50 = 130 nM Funct
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
405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1
CHEMBL3754486 ffar1_human Human No 6.9 EC50 = 130 nM Bind
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
480 8 1 4 6.3 Cn1ccnc1C(CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1
CHEMBL2152070 ffar1_human Human Yes 6.9 EC50 = 130 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL2152070 ffar1_human Human Yes 6.9 EC50 = 130 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL3985181 ffar1_human Human No 5.9 EC50 = 1300 nM Funct
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
547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1
CHEMBL3990065 ffar1_human Human No 5.9 EC50 = 1300 nM Funct
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
547 11 1 5 6.2 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(OCc3cccc(F)c3)CCO4)cc2)cc1
CHEMBL4093180 ffar1_human Human No 5.9 EC50 = 1300 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
340 6 1 4 4.0 CN(C)c1cccc(Oc2ccc(N3CCC[C@H]3CC(=O)O)cc2)c1
CHEMBL4099410 ffar1_mouse Mouse No 5.9 EC50 = 1300 nM Funct
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
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
CHEMBL4100898 ffar1_mouse Mouse No 5.9 EC50 = 1300 nM Funct
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
373 6 1 3 5.6 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2-c2ccccc2)cc1
CHEMBL4065429 ffar1_mouse Mouse No 5.9 EC50 = 1300 nM Funct
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
449 8 1 5 5.7 O=C(O)CCc1ccc(-c2ccc3c(OCc4ccccc4)nn(-c4ccccn4)c3c2)cc1
CHEMBL4085805 ffar1_human Human No 4.9 EC50 = 13000 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
365 6 1 3 4.6 O=C(O)C[C@H]1CCN1c1ccc(OCc2ccc(Cl)cc2Cl)cc1
CHEMBL4171817 ffar1_human Human No 5.9 EC50 = 1308 nM Funct
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
333 4 2 1 4.9 O=C(O)CCc1ccc2[nH]c(-c3ccccc3C(F)(F)F)cc2c1
CHEMBL2151300 ffar1_human Human No 5.9 EC50 = 1310 nM Funct
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
504 9 1 3 8.1 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CCCC4)c3)cc2C(C)(C)C)c1
CHEMBL3330549 ffar1_human Human No 5.9 EC50 = 1310 nM Bind
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
528 8 1 4 7.0 CCC1C(C(F)(F)F)=NN(c2ccc(Cc3ccc(-c4cc(OC)ccc4F)cc3C)cc2)C1CC(=O)O
CHEMBL3601058 ffar1_human Human Yes 4.9 EC50 = 13100 nM Funct
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
358 7 1 5 4.0 O=C(O)CCc1ccc(OCc2nc(-c3ccccc3)no2)c(Cl)c1
CHEMBL4083440 ffar1_human Human No 4.9 EC50 = 13142 nM Funct
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
370 7 1 3 5.5 CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1
CHEMBL1829143 ffar1_human Human No 4.9 EC50 = 13182.6 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
251 3 1 2 2.5 O=C(O)CCc1ccc(C#Cc2ccccn2)cc1
CHEMBL2381316 ffar1_human Human No 6.9 EC50 = 132 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
416 4 1 4 5.4 Cc1cc(C)cc(-c2cccc(C3COc4cc5c(cc4O3)OC[C@H]5CC(=O)O)c2)c1
CHEMBL3616719 ffar1_human Human No 6.9 EC50 = 132.9 nM Funct
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
361 7 2 4 3.3 Cc1ccc(OC(C)C(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1C
CHEMBL4167397 ffar1_human Human No 6.9 EC50 = 133 nM Funct
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
522 8 1 5 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccc(Cl)cc4)CC3)s2)cc1
CHEMBL4177506 ffar1_human Human No 6.9 EC50 = 133 nM Funct
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
457 8 2 4 5.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)NC3CCCc4ccccc43)o2)cc1
CHEMBL4160127 ffar1_human Human No 6.9 EC50 = 133 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
398 6 1 2 6.4 O=C(O)C[C@H](c1ccc2c(c1)OC(c1ccc(-c3ccccc3)cc1)CC2)C1CC1
CHEMBL4216016 ffar1_human Human No 6.9 EC50 = 134 nM Funct
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
478 7 1 5 6.6 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2cc(C)c3scc(-c4ccccc4C)c3c2)cc1
CHEMBL3915620 ffar1_human Human Yes 6.9 EC50 = 134 nM Funct
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
491 8 1 3 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1
CHEMBL1829166 ffar1_human Human No 6.9 EC50 = 134.9 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
299 3 1 2 3.5 Cc1c(C#Cc2ccc(CCC(=O)O)cc2)ccnc1Cl
CHEMBL1688457 ffar1_human Human No 6.9 EC50 = 134.9 nM Funct
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
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1
CHEMBL4072314 ffar1_human Human No 5.9 EC50 = 1340 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL609615 ffar1_human Human No 6.9 EC50 = 135 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
349 4 1 4 4.5 O=C1NC(=O)C(Cc2ccc(Oc3cccc4ccccc34)cc2)S1
CHEMBL3616652 ffar1_human Human No 6.9 EC50 = 135.3 nM Funct
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
333 7 2 4 2.7 CC(Oc1ccccc1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1
CHEMBL3616656 ffar1_human Human No 6.9 EC50 = 135.9 nM Funct
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
351 7 2 4 2.8 CC(Oc1ccccc1F)C(=O)Nc1ccc(OCC(=O)O)c(F)c1
CHEMBL4454699 ffar1_human Human No 5.9 EC50 = 1350 nM Bind
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
357 7 1 5 3.8 Cc1nc(-c2ccccc2)oc1COc1ccc(OCC(=O)O)c(F)c1
CHEMBL3939004 ffar1_human Human No 5.9 EC50 = 1350 nM Funct
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
370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1
CHEMBL4215600 ffar1_human Human No 5.9 EC50 = 1350 nM Funct
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
487 10 2 6 5.2 COc1ccc(C(Cc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c2ccccc2)cc1
CHEMBL4282779 ffar1_human Human No 4.9 EC50 = 13570 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
365 6 2 4 3.7 O=C(O)CCc1ccc(NCC2COc3ccc(Cl)cc3O2)cc1F
CHEMBL1777856 ffar1_human Human Yes 5.9 EC50 = 1358 nM Funct
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
310 5 1 2 4.8 O=C(O)CCc1ccc(Oc2ccc(Cl)cc2Cl)cc1
CHEMBL1777878 ffar1_mouse Mouse No 6.9 EC50 = 136 nM Funct
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
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
CHEMBL3939004 ffar1_human Human No 5.9 EC50 = 1367 nM Funct
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
370 5 1 3 4.6 O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1
CHEMBL3780713 ffar1_human Human No 6.9 EC50 = 137.5 nM Funct
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
415 6 1 5 5.3 Cc1nc(-c2cccc(Cl)c2)sc1COc1ccc2c(c1)OCC2CC(=O)O
CHEMBL4591657 ffar1_human Human No 5.9 EC50 = 1370 nM Bind
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
426 9 1 3 6.2 COc1ccc(F)c([C@H]2CC[C@H](COc3cccc([C@@H](CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL3883819 ffar1_human Human No 5.9 EC50 = 1379 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL4162778 ffar1_human Human No 5.9 EC50 = 1379 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL4173953 ffar1_human Human No 6.9 EC50 = 138 nM Funct
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
489 8 1 6 4.3 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4ccccn4)CC3)s2)cc1
CHEMBL2315538 ffar1_human Human No 6.9 EC50 = 138.0 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
276 2 1 1 3.6 Cc1ccccc1C#Cc1ccc([C@H]2C[C@@H]2C(=O)O)cc1
CHEMBL2315543 ffar1_human Human No 6.9 EC50 = 138.0 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
298 3 1 1 4.1 Cc1cc(Cl)ccc1C#Cc1ccc(CCC(=O)O)cc1
CHEMBL2385471 ffar1_human Human No 5.9 EC50 = 1380 nM Bind
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
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
CHEMBL4215103 ffar1_human Human No 5.9 EC50 = 1380 nM Funct
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
423 8 2 6 3.9 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3ccc4c(c3)CCC4)s2)cc1
CHEMBL3883819 ffar1_human Human No 5.9 EC50 = 1380 nM Funct
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
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL4162778 ffar1_human Human No 5.9 EC50 = 1380 nM Funct
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
461 7 1 4 6.2 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)nc2)c1
CHEMBL598732 ffar1_human Human No 4.9 EC50 = 13850 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
432 5 1 6 4.4 COc1cc(Oc2ncc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O
CHEMBL3883532 ffar1_human Human No 6.9 EC50 = 139 nM Funct
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
540 8 1 3 8.7 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C2=CCCC2(C)C)c1
CHEMBL3952316 ffar1_human Human No 5.9 EC50 = 1391 nM Funct
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
350 5 1 3 5.0 O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1
CHEMBL1829174 ffar1_human Human Yes 7.9 EC50 = 14 nM Funct
Agonist activity at FFA1 (unknown origin)Agonist activity at FFA1 (unknown origin)
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL2047158 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
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
CHEMBL1829174 ffar1_human Human Yes 7.9 EC50 = 14 nM Funct
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL1829174 ffar1_human Human Yes 7.9 EC50 = 14 nM Funct
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL3288359 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
405 9 1 4 5.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(-c3c(C)cccc3C)c2)nc1
CHEMBL2048616 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
466 10 1 3 7.1 Cc1cc(OCc2ccccc2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1
CHEMBL4787628 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL4778264 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1
CHEMBL4788206 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
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
CHEMBL4167323 ffar1_rat Rat No 7.9 EC50 = 14 nM Funct
Agonist activity at rat GPR40Agonist activity at rat GPR40
467 8 2 3 5.7 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(C(=O)N[C@@H]3CCCc4ccccc43)cc2)cc1
CHEMBL4207592 ffar1_rat Rat No 7.9 EC50 = 14 nM Funct
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
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
CHEMBL4213548 ffar1_rat Rat No 7.9 EC50 = 14 nM Funct
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
538 11 1 7 6.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cccc(OCCOC)c4C)c3c2)cc1
CHEMBL4213937 ffar1_rat Rat No 7.9 EC50 = 14 nM Funct
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
482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1
CHEMBL3927519 ffar1_rat Rat Yes 7.9 EC50 = 14 nM Bind
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
439 7 1 5 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4c(C)cccc4C)nn3c2)cc1
CHEMBL3883627 ffar1_human Human No 7.9 EC50 = 14 nM Funct
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
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
CHEMBL2164242 ffar1_human Human Yes 7.9 EC50 = 14.1 nM Bind
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
499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C
CHEMBL1829174 ffar1_human Human Yes 7.9 EC50 = 14.1 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL380884 ffar1_human Human No 7.9 EC50 = 14.1 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
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
CHEMBL1688473 ffar1_human Human No 7.9 EC50 = 14.2 nM Funct
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
378 7 1 2 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1
CHEMBL1773261 ffar1_human Human Yes 7.8 EC50 = 14.8 nM Funct
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
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL2163925 ffar1_human Human No 7.8 EC50 = 14.8 nM Funct
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
495 12 2 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL203297 ffar1_human Human No 7.8 EC50 = 14.8 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
374 7 3 4 4.7 O=C(NO)[C@H]1C[C@@H]1c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL4218995 ffar1_human Human No 6.9 EC50 = 140 nM Funct
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
516 10 1 3 8.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2CCCC2(C)C)c1
CHEMBL4789994 ffar1_human Human No 6.9 EC50 = 140 nM Funct
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
542 11 1 5 6.2 COc1ccc(C(=O)N(C)c2ccccc2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL4061093 ffar1_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2C[C@@H](C)C[C@H]2CC(=O)O)cc1
CHEMBL3905435 ffar1_human Human No 6.9 EC50 = 140 nM Bind
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
516 11 1 5 6.0 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCN(C)CC3)c2)cc1
CHEMBL2022580 ffar1_human Human No 6.9 EC50 = 140 nM Funct
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
474 10 1 4 6.2 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)CCC(C(=O)O)C4)c2)c(C)c1
CHEMBL4794904 ffar1_human Human No 6.9 EC50 = 140 nM Funct
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
487 8 1 3 6.5 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1Cl
CHEMBL3616663 ffar1_human Human No 6.9 EC50 = 140.3 nM Funct
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
389 7 2 4 4.0 CC(Oc1cccc(C(C)(C)C)c1)C(=O)Nc1ccc(OCC(=O)O)c(F)c1
CHEMBL4077507 ffar1_mouse Mouse No 5.9 EC50 = 1400 nM Funct
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
357 5 1 4 4.4 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12
CHEMBL3288350 ffar1_rat Rat No 5.9 EC50 = 1400 nM Funct
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
362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2ncc(CCC(=O)O)cn2)c1
CHEMBL4778264 ffar1_rat Rat No 4.9 EC50 = 14000 nM Bind
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
440 8 1 7 4.6 O=C(O)C[C@@H](c1ccc(OCc2ccc3nc(-c4ccccc4)nn3c2)cc1)c1ccon1
CHEMBL4103681 ffar1_mouse Mouse No 4.9 EC50 = 14000 nM Funct
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
393 6 1 3 5.3 Cc1cc(OCc2ccc(Cl)cc2Cl)ccc1N1CCC[C@H]1CC(=O)O
CHEMBL1777865 ffar1_human Human No 5.9 EC50 = 1401 nM Funct
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
398 5 1 2 6.2 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C(F)(F)F)c3ccccc23)cc1
CHEMBL598731 ffar1_human Human No 5.9 EC50 = 1407 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
397 5 1 5 4.7 COc1cc(Oc2ccc(Cl)cc2Cl)ccc1CC1SC(=O)NC1=O
CHEMBL2386360 ffar1_human Human No 6.9 EC50 = 141.3 nM Funct
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
286 3 1 1 3.4 O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F
CHEMBL3265143 ffar1_human Human No 5.9 EC50 = 1410 nM Bind
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
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
CHEMBL4211335 ffar1_human Human No 5.9 EC50 = 1411 nM Funct
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
480 7 1 5 6.0 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3c(c2)c(-c2ccccc2C)c[s+]3[O-])cc1
CHEMBL2385466 ffar1_human Human No 5.9 EC50 = 1420 nM Bind
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
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
CHEMBL4105013 ffar1_human Human No 5.9 EC50 = 1423 nM Funct
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
356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1
CHEMBL3800255 ffar1_human Human No 6.8 EC50 = 143 nM Funct
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
441 10 1 5 5.7 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)cc(OCC(C)C)c1
CHEMBL601420 ffar1_human Human No 6.8 EC50 = 144 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
350 4 1 5 3.9 O=C1NC(=O)C(Cc2ccc(Oc3cc4ccccc4cn3)cc2)S1
CHEMBL4163436 ffar1_human Human No 6.8 EC50 = 144 nM Funct
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
474 8 2 5 5.1 CC#CC(CC(=O)O)c1ccc(OCc2cnc(C(=O)NC3CCCc4ccccc43)s2)cc1
CHEMBL2315537 ffar1_human Human No 6.8 EC50 = 144.5 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
262 2 1 1 3.3 O=C(O)[C@H]1C[C@@H]1c1ccc(C#Cc2ccccc2)cc1
CHEMBL2386358 ffar1_human Human No 6.8 EC50 = 144.5 nM Funct
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
268 3 1 1 3.2 O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1
CHEMBL205960 ffar1_human Human No 6.8 EC50 = 144.5 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
345 7 2 3 5.2 O=C(O)/C=C/c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL3785789 ffar1_human Human No 5.8 EC50 = 1445.4 nM Funct
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
272 8 1 1 4.4 CCCCCCCC#Cc1ccc(CCC(=O)O)cc1
CHEMBL2386366 ffar1_human Human No 5.8 EC50 = 1445.4 nM Funct
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
360 5 1 3 2.8 CS(=O)(=O)Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1
CHEMBL2381300 ffar1_human Human No 6.8 EC50 = 145.2 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
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
CHEMBL252528 ffar1_human Human Yes 4.8 EC50 = 14500 nM Funct
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
283 7 2 3 3.6 C=CCOc1ccc(CNc2cccc(C(=O)O)c2)cc1
CHEMBL3958983 ffar1_human Human No 6.8 EC50 = 146 nM Funct
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
425 7 1 5 4.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cc(-c3ccccc3C)cn3ncnc23)cc1
CHEMBL4159416 ffar1_human Human No 6.8 EC50 = 146 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL4300796 ffar1_human Human No 6.8 EC50 = 146 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
460 7 1 3 6.8 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@H](C5CC5)[C@H](C)C(=O)O)cc4O3)cc2)c1
CHEMBL3884803 ffar1_human Human No 6.8 EC50 = 146 nM Funct
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
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
CHEMBL3265140 ffar1_human Human No 6.8 EC50 = 147 nM Bind
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
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
CHEMBL3604056 ffar1_human Human No 6.8 EC50 = 147 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
368 8 1 3 5.1 CCOC(CC(=O)O)c1cccc(OCc2ccc(Cl)c(Cl)c2)c1
CHEMBL3616479 ffar1_human Human No 6.8 EC50 = 147.6 nM Funct
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
349 8 2 5 2.3 COc1cccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)c1
CHEMBL2386353 ffar1_mouse Mouse Yes 6.8 EC50 = 147.9 nM Funct
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
307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O
CHEMBL4289597 ffar1_human Human No 5.8 EC50 = 1470 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
362 7 1 5 3.1 COc1ccc2c(c1)OC(COc1ccc(CCC(=O)O)c(F)c1)CO2
CHEMBL4093521 ffar1_human Human No 4.8 EC50 = 14700 nM Funct
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
351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(OCc2cn(CCC(=O)O)nn2)c1
CHEMBL4210588 ffar1_human Human No 6.8 EC50 = 148 nM Funct
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
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
CHEMBL3616658 ffar1_human Human No 6.8 EC50 = 148.2 nM Funct
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
333 7 2 4 2.6 Cc1ccc(OCC(=O)Nc2ccc(OCC(=O)O)c(F)c2)cc1
CHEMBL4063221 ffar1_human Human No 5.8 EC50 = 1480 nM Funct
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
545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1
CHEMBL4117645 ffar1_human Human No 5.8 EC50 = 1480 nM Funct
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
545 12 1 7 5.3 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(CC3)CC(CCOc3cnccn3)CCO4)cc2)cc1
CHEMBL4065921 ffar1_human Human No 4.8 EC50 = 14800 nM Funct
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
351 7 1 5 3.6 Cc1cccc(C)c1-c1cccc(COc2cn(CCC(=O)O)nn2)c1
CHEMBL1777867 ffar1_mouse Mouse No 5.8 EC50 = 1484 nM Funct
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
360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1
CHEMBL4573403 ffar1_human Human No 6.8 EC50 = 149 nM Bind
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
441 7 1 5 5.3 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc(OCC(=O)O)c(F)c1
CHEMBL1777869 ffar1_mouse Mouse No 6.8 EC50 = 149 nM Funct
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
331 5 1 3 4.6 CC#CC(CC(=O)O)c1ccc(Oc2nccc3ccccc23)cc1
CHEMBL4075819 ffar1_human Human No 5.8 EC50 = 1490 nM Bind
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
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
CHEMBL4213937 ffar1_human Human No 7.8 EC50 = 15 nM Funct
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
482 7 1 5 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccccc4C)c3c2)cc1
CHEMBL4218348 ffar1_human Human No 7.8 EC50 = 15 nM Funct
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
532 7 1 5 7.3 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C(F)(F)F)c(-c4ccccc4C)c3c2)cc1
CHEMBL2048615 ffar1_human Human No 7.8 EC50 = 15 nM Funct
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
430 10 1 3 6.4 Cc1cc(OCC2CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1
CHEMBL2048624 ffar1_human Human No 7.8 EC50 = 15 nM Funct
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
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
CHEMBL1829173 ffar1_human Human Yes 7.8 EC50 = 15 nM Funct
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL4575265 ffar1_human Human No 7.8 EC50 = 15 nM Funct
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
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
CHEMBL4202452 ffar1_human Human No 7.8 EC50 = 15.5 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
496 12 1 5 5.4 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1
CHEMBL4793322 ffar1_rat Rat No 7.8 EC50 = 15.5 nM Funct
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
517 10 1 6 5.8 COc1ccc(F)c(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2N2CC3(CCC3)C2)c1
CHEMBL4593950 ffar1_human Human No 7.8 EC50 = 15.7 nM Funct
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
419 7 2 3 5.6 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3C(F)(F)F)c2)cc1F
CHEMBL3799274 ffar1_human Human No 7.8 EC50 = 15.9 nM Funct
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
403 7 1 4 5.3 Cc1noc(C)c1-c1cc(COc2ccc(CCC(=O)O)c(F)c2)ccc1Cl
CHEMBL3265145 ffar1_human Human No 6.8 EC50 = 150 nM Bind
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
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
CHEMBL2385473 ffar1_human Human No 6.8 EC50 = 150 nM Bind
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
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
CHEMBL4459626 ffar1_human Human No 6.8 EC50 = 150 nM Funct
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
453 7 1 5 5.0 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccc(C#N)cc4)cc3O2)cc1
CHEMBL2152070 ffar1_human Human Yes 6.8 EC50 = 150 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL4793427 ffar1_human Human No 6.8 EC50 = 150 nM Funct
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
491 10 1 4 7.0 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)(C)C)c1
CHEMBL4067052 ffar1_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
315 5 1 3 4.1 O=C(O)C[C@@H]1CCCN1c1ccc(Oc2ccccc2F)cc1
CHEMBL4082459 ffar1_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
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
CHEMBL4096887 ffar1_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
309 5 1 2 4.0 Cc1ccccc1Cc1ccc(N2CCC[C@H]2CC(=O)O)cc1
CHEMBL4066815 ffar1_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4093944 ffar1_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4283222 ffar1_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
420 6 1 4 4.8 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3cc(Cl)c(Cl)cc3O2)cc1
CHEMBL3604035 ffar1_human Human Yes 5.8 EC50 = 1500 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
382 8 1 3 5.4 CCOC(CC(=O)O)c1ccc(OCc2ccc(Cl)c(Cl)c2)c(C)c1
CHEMBL4073525 ffar1_mouse Mouse No 5.8 EC50 = 1500 nM Funct
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
485 8 1 4 6.6 Cc1cc(OCc2ccccc2)ccc1Oc1ccc(N2C[C@@H](C(F)(F)F)C[C@H]2CC(=O)O)cc1
CHEMBL4075162 ffar1_mouse Mouse No 5.8 EC50 = 1500 nM Funct
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
375 5 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12
CHEMBL4644239 ffar1_human Human No 5.8 EC50 = 1508 nM Bind
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
424 7 1 4 5.5 CC#CC(CC(=O)O)c1ccc(OCc2ccn3cc(-c4cccc(C)c4)nc3c2)cc1
CHEMBL4581212 ffar1_human Human No 6.8 EC50 = 151 nM Funct
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
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
CHEMBL2315547 ffar1_human Human No 6.8 EC50 = 151.4 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
284 3 1 1 3.8 O=C(O)CCc1ccc(C#Cc2ccccc2Cl)cc1
CHEMBL252330 ffar1_human Human Yes 4.8 EC50 = 15100 nM Funct
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
404 8 1 7 4.8 COc1ccc(CSc2nnc(SCc3ccc(C(=O)O)cc3)s2)cc1
CHEMBL3955132 ffar1_human Human Yes 6.8 EC50 = 152 nM Funct
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
475 9 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCCc4cccc(OC)c43)s2)cc1
CHEMBL3805668 ffar1_human Human No 5.8 EC50 = 1520 nM Funct
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
397 8 2 6 3.7 Cc1ccccc1NC(=O)c1nnc(COc2ccc(CCC(=O)O)cc2)s1
CHEMBL4203402 ffar1_human Human No 5.8 EC50 = 1520 nM Funct
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
397 8 2 6 3.7 Cc1ccccc1OCc1nnc(C(=O)Nc2ccc(CCC(=O)O)cc2)s1
CHEMBL3353738 ffar1_human Human No 6.8 EC50 = 153.3 nM Funct
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
512 12 1 6 5.1 Cc1cc(OCc2cccc(-c3c(C)cc(OCCCS(C)(=O)=O)cc3C)c2)ccc1OCC(=O)O
CHEMBL4207787 ffar1_human Human No 5.8 EC50 = 1530 nM Funct
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
411 8 2 6 4.0 Cc1ccc(C)c(OCc2nnc(C(=O)Nc3ccc(CCC(=O)O)cc3)s2)c1
CHEMBL3884609 ffar1_human Human No 6.8 EC50 = 154 nM Funct
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
530 10 1 4 7.6 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2C(OC)C2CC2)c1
CHEMBL1688454 ffar1_human Human No 6.8 EC50 = 154.9 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
348 8 1 3 5.1 O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1
CHEMBL1829173 ffar1_human Human Yes 6.8 EC50 = 154.9 nM Bind
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL487570 ffar1_human Human No 6.8 EC50 = 154.9 nM Funct
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
274 3 1 1 3.1 C#Cc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1
CHEMBL4061630 ffar1_human Human No 5.8 EC50 = 1544 nM Funct
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
370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O
CHEMBL4167766 ffar1_human Human No 6.8 EC50 = 155 nM Funct
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
502 9 1 5 4.9 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(Cc4ccccc4)CC3)s2)cc1
CHEMBL4581859 ffar1_human Human No 6.8 EC50 = 155 nM Funct
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
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
CHEMBL3781779 ffar1_human Human No 6.8 EC50 = 156 nM Bind
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
411 7 1 6 4.7 COc1ccc(-c2nc(C)c(COc3ccc4c(c3)OCC4CC(=O)O)s2)cc1
CHEMBL4534812 ffar1_human Human No 6.8 EC50 = 156 nM Bind
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
387 7 1 5 4.6 Cc1ccc(-c2nc(C)c(COc3ccc(OCC(=O)O)c(F)c3)s2)cc1
CHEMBL1777867 ffar1_human Human No 5.8 EC50 = 1568 nM Funct
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
360 5 1 4 3.6 CC#CC(CC(=O)O)c1ccc(Oc2ncc(Br)cn2)cc1
CHEMBL4639050 ffar1_human Human No 6.8 EC50 = 157 nM Bind
Agonist activity at GPR40 (unknown origin)Agonist activity at GPR40 (unknown origin)
454 9 1 5 5.6 CC#CC(CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccccc4OCC)cn3c2)cc1
CHEMBL4226029 ffar1_human Human No 6.8 EC50 = 157.1 nM Funct
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
380 6 1 4 5.3 Cc1ccsc1-c1cccc(COc2ccc3c(c2)OCC3CC(=O)O)c1
CHEMBL4203431 ffar1_human Human No 5.8 EC50 = 1570 nM Funct
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
417 8 2 6 4.0 O=C(O)CCc1ccc(NC(=O)c2nnc(COc3cccc(Cl)c3)s2)cc1
CHEMBL1777868 ffar1_human Human No 5.8 EC50 = 1578 nM Funct
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
307 5 1 5 2.7 CC#CC(CC(=O)O)c1ccc(Oc2nccnc2C#N)cc1
CHEMBL397776 ffar1_human Human No 5.8 EC50 = 1584.9 nM Funct
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
345 8 2 2 5.4 O=C(O)CCCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1
CHEMBL4061630 ffar1_human Human No 5.8 EC50 = 1584.9 nM Funct
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
370 7 1 3 5.2 Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O
CHEMBL4103243 ffar1_human Human No 5.8 EC50 = 1584.9 nM Funct
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
376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1
CHEMBL4105013 ffar1_human Human No 5.8 EC50 = 1584.9 nM Funct
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
356 7 1 3 4.9 O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1
CHEMBL4787628 ffar1_rat Rat No 7.8 EC50 = 16 nM Bind
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
509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL1829174 ffar1_human Human Yes 7.8 EC50 = 16 nM Funct
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL2047149 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
476 11 1 5 5.9 CCOCCOc1cc(C)c(-c2cccc(COc3ccc4c(c3)OC[C@H]4CC(=O)O)c2)c(C)c1
CHEMBL2047168 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
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
CHEMBL2047169 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
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
CHEMBL4206968 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1
CHEMBL4459220 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
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
CHEMBL3286409 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
501 8 1 6 6.1 Cc1nc(-c2ccc(C(F)(F)F)cc2)sc1COc1ccc([C@H](CC(=O)O)c2nccn2C)cc1
CHEMBL4077366 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
485 11 1 7 4.6 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OCCOC)cc4)nn3c2)cc1
CHEMBL2381287 ffar1_human Human No 7.8 EC50 = 16 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@@H](c1ccc(Cl)c(Cl)c1)O3
CHEMBL4218110 ffar1_rat Rat No 7.8 EC50 = 16 nM Funct
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
456 7 1 5 6.4 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(C4CCCCC4)c3c2)cc1
CHEMBL3288348 ffar1_rat Rat No 7.8 EC50 = 16 nM Funct
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
362 7 1 4 4.4 Cc1cccc(C)c1-c1cccc(COc2cnc(CCC(=O)O)cn2)c1
CHEMBL3883790 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
447 7 1 4 5.9 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)nc2)c1
CHEMBL4542487 ffar1_human Human No 7.8 EC50 = 16 nM Funct
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
448 8 1 4 6.0 COc1ccc(F)c(-c2ccc3c(c2)OC[C@@H]3Oc2cccc([C@@H](CC(=O)O)C3CC3)c2)c1
CHEMBL3895442 ffar1_human Human No 7.8 EC50 = 16.1 nM Bind
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
473 12 1 4 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)CC3CC3)c2)cc1
CHEMBL1688465 ffar1_human Human No 7.8 EC50 = 16.6 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
346 7 1 2 5.3 Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1
CHEMBL3933446 ffar1_human Human No 7.8 EC50 = 16.7 nM Bind
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
551 11 1 6 5.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(CN(Cc3ccsc3)C3CCS(=O)(=O)CC3)c2)cc1
CHEMBL2386363 ffar1_human Human No 7.8 EC50 = 17.0 nM Funct
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
307 3 1 2 3.4 Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1
CHEMBL3600994 ffar1_human Human Yes 6.8 EC50 = 160 nM Funct
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
357 7 1 4 4.6 O=C(O)CCc1ccc(OCc2coc(-c3cccc(Cl)c3)n2)cc1
CHEMBL2152070 ffar1_human Human Yes 6.8 EC50 = 160 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL2152070 ffar1_human Human Yes 6.8 EC50 = 160 nM Funct
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL4783190 ffar1_rat Rat No 6.8 EC50 = 160 nM Bind
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
471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL2152070 ffar1_human Human Yes 6.8 EC50 = 160 nM Bind
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL4469136 ffar1_human Human No 6.8 EC50 = 160 nM Funct
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
428 7 1 4 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3ccc(-c4ccccc4)cc3O2)cc1
CHEMBL4752289 ffar1_human Human No 6.8 EC50 = 160 nM Funct
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
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
CHEMBL1829174 ffar1_human Human Yes 6.8 EC50 = 160 nM Funct
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
524 11 1 6 5.3 OC(=O)C[C@@H]1COc2c1ccc(c2)OCc1cccc(c1)c1c(C)cc(cc1C)OCCCS(=O)(=O)C
CHEMBL3600998 ffar1_human Human Yes 5.8 EC50 = 1600 nM Funct
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
323 7 1 4 3.9 O=C(O)CCc1ccc(OCc2ncc(-c3ccccc3)o2)cc1
CHEMBL3604032 ffar1_human Human No 5.8 EC50 = 1600 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
327 7 2 3 3.8 CCOC(CC(=O)O)c1ccc(NC(=O)c2ccccc2C)cc1
CHEMBL2152070 ffar1_human Human Yes 6.8 EC50 = 161 nM Bind
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
514 10 1 3 8.3 CC1(CCC=C1C2=C(C=CC(=C2)COC3=CC=CC(=C3)[C@@H](CC(=O)O)C4CC4)C5=C(C=CC(=C5)OC)F)C
CHEMBL404008 ffar1_human Human Yes 4.8 EC50 = 16100 nM Funct
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
345 5 2 3 3.9 O=C(O)c1ccc(NC(=O)c2ccc(C(=O)c3ccccc3)cc2)cc1
CHEMBL3265149 ffar1_human Human No 6.8 EC50 = 162 nM Bind
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
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
CHEMBL2315550 ffar1_human Human No 4.8 EC50 = 16218.1 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
266 3 2 2 2.8 O=C(O)CCc1ccc(C#Cc2ccccc2O)cc1
CHEMBL3883449 ffar1_human Human No 5.8 EC50 = 1623 nM Funct
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
490 9 1 4 6.7 COCc1cc(C2CCc3ccc([C@@H](CC(=O)O)C4CC4)cc3O2)ccc1-c1cc(OC)ccc1F
CHEMBL4443853 ffar1_rat Rat No 6.8 EC50 = 163 nM Funct
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
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
CHEMBL4103243 ffar1_human Human No 5.8 EC50 = 1631 nM Funct
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
376 8 1 3 5.7 Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1
CHEMBL606213 ffar1_human Human No 5.8 EC50 = 1635 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
368 4 1 5 3.8 O=C1NC(=O)C(Cc2ccc(Oc3cccc(C(F)(F)F)n3)cc2)S1
CHEMBL3805303 ffar1_human Human No 5.8 EC50 = 1640 nM Funct
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
343 6 2 6 3.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3ccco3)c2)s1
CHEMBL4171391 ffar1_human Human No 6.8 EC50 = 165 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
444 7 1 3 7.1 CSc1cccc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1
CHEMBL1773252 ffar1_human Human Yes 6.8 EC50 = 166.0 nM Funct
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayAgonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
334 6 1 2 4.0 O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1
CHEMBL234268 ffar1_human Human No 4.8 EC50 = 16595.9 nM Funct
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
347 7 2 3 5.3 CC(C(=O)O)c1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL4097527 ffar1_human Human No 6.8 EC50 = 166 nM Bind
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
477 9 1 6 5.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc3nc(-c4ccc(OC(F)F)cc4)nn3c2)cc1
CHEMBL3758719 ffar1_human Human No 5.8 EC50 = 1660 nM Funct
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
501 9 1 5 6.5 O=C1NC(=O)C(Cc2ccc(OCC[C@H](Oc3ccc(Cl)cc3Cl)c3ccccc3)cc2)S1
CHEMBL3759448 ffar1_human Human No 4.8 EC50 = 16600 nM Funct
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
395 6 1 6 4.1 CC(C)n1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21
CHEMBL252526 ffar1_human Human Yes 4.8 EC50 = 16700 nM Funct
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
312 6 0 7 3.1 COC(=O)CSc1nnc(SCc2ccccc2)s1
CHEMBL402053 ffar1_human Human Yes 4.8 EC50 = 16800 nM Funct
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
297 5 1 5 2.3 O=C(O)CCCN1C(=O)/C(=C\c2ccco2)SC1=S
CHEMBL1829173 ffar1_human Human Yes 6.8 EC50 = 169.8 nM Funct
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
438 7 1 2 6.5 CC#C[C@H](c1ccc(cc1)OCc1cccc(c1)c1ccc(cc1)C(F)(F)F)CC(=O)O
CHEMBL4210139 ffar1_human Human No 6.8 EC50 = 169.8 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
546 12 1 7 4.2 Cc1cc(OCCCS(C)(=O)=O)cc(C)c1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1
CHEMBL3805558 ffar1_human Human No 5.8 EC50 = 1690 nM Funct
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
387 6 2 5 4.1 O=C(O)CCc1nnc(C(=O)Nc2cccc(-c3cccc(Cl)c3)c2)s1
CHEMBL3883407 ffar1_human Human No 5.8 EC50 = 1690 nM Funct
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
446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1
CHEMBL4783033 ffar1_rat Rat No 7.8 EC50 = 17 nM Bind
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
512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2nc(C)c(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL2047160 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
529 11 1 5 5.9 Cc1cc(OCCCN2CCCC2=O)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
CHEMBL2047163 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
534 9 1 6 6.7 Cc1cc(OCc2cccc3nccn23)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
CHEMBL2047164 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
552 13 1 6 5.8 CCc1cc(OCCCS(C)(=O)=O)cc(CC)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
CHEMBL2047170 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
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
CHEMBL4763105 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
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
CHEMBL4800194 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
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
CHEMBL4781604 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
521 9 1 4 6.4 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(OC)c2)cc1
CHEMBL4785057 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
542 8 1 4 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3c(Cl)cccc34)cc2)cc1
CHEMBL4794233 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1
CHEMBL4798023 ffar1_human Human No 7.8 EC50 = 17 nM Funct
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
509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)c(F)c2)cc1
CHEMBL4764485 ffar1_rat Rat Yes 7.8 EC50 = 17 nM Funct
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
479 11 1 6 5.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2CC(C)C)c(F)cn1
CHEMBL2163924 ffar1_human Human No 7.8 EC50 = 17.4 nM Funct
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
481 12 2 5 5.1 Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL2164241 ffar1_human Human No 7.8 EC50 = 17.8 nM Funct
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
377 7 2 2 5.7 Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1
CHEMBL1688470 ffar1_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
378 7 1 2 5.5 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(F)C(=O)O)cc2)c1
CHEMBL1688471 ffar1_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
374 7 1 2 5.8 Cc1cccc(C)c1-c1cccc(COc2ccc(CC(C)C(=O)O)cc2)c1
CHEMBL4215771 ffar1_human Human No 6.8 EC50 = 170 nM Funct
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
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
CHEMBL4094160 ffar1_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
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
CHEMBL4291567 ffar1_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assayAgonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay
386 6 1 4 4.1 CC#C[C@@H](CC(=O)O)c1ccc(OC[C@H]2COc3c(Cl)cccc3O2)cc1
CHEMBL4790921 ffar1_human Human No 6.8 EC50 = 170 nM Bind
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
498 8 1 5 5.9 CC#C[C@@H](CC(=O)O)c1ccc(OCc2cnc(CN3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL4069191 ffar1_mouse Mouse No 6.8 EC50 = 170 nM Funct
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
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
CHEMBL1688491 ffar1_human Human No 5.8 EC50 = 1700 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
298 9 1 2 4.1 O=C(O)CCc1ccc(OCCCCc2ccccc2)cc1
CHEMBL2022246 ffar1_human Human No 5.8 EC50 = 1700 nM Funct
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
386 6 1 3 5.9 Cc1cccc(C)c1-c1cccc(COc2ccc3c(CC(=O)O)coc3c2)c1
CHEMBL3604029 ffar1_human Human No 5.8 EC50 = 1700 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
338 8 1 5 3.4 CCOC(Cc1nnn[nH]1)c1ccc(OCc2ccccc2C)cc1
CHEMBL4075885 ffar1_human Human No 5.8 EC50 = 1700 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
341 7 1 4 4.3 CCOc1ccccc1Oc1ccc(N2CCC[C@H]2CC(=O)O)cc1
CHEMBL4101348 ffar1_human Human No 5.8 EC50 = 1700 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
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
CHEMBL1777864 ffar1_human Human No 6.8 EC50 = 172 nM Funct
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
355 5 1 3 5.1 CC#CC(CC(=O)O)c1ccc(Oc2ccc(C#N)c3ccccc23)cc1
CHEMBL4173085 ffar1_human Human No 6.8 EC50 = 172 nM Funct
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
511 7 1 4 6.1 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)s2)cc1
CHEMBL394666 ffar1_human Human No 6.8 EC50 = 173.8 nM Funct
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
333 6 2 2 4.1 O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1
CHEMBL206779 ffar1_human Human No 6.8 EC50 = 173.8 nM Funct
Agonist potency at human GPR40 expressed in CHO cellsAgonist potency at human GPR40 expressed in CHO cells
374 8 1 3 5.1 CN(C)C(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1
CHEMBL4213829 ffar1_human Human No 6.8 EC50 = 177.8 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
469 11 1 7 3.6 CO/N=C(\COc1ccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)cc1)c1ccccc1
CHEMBL1829164 ffar1_human Human No 6.8 EC50 = 177.8 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
283 3 1 2 2.9 Cc1cnc(F)cc1C#Cc1ccc(CCC(=O)O)cc1
CHEMBL604126 ffar1_human Human Yes 6.8 EC50 = 177.8 nM Funct
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
416 4 1 5 4.7 O=C1NC(=O)C(S1)Cc1ccc(cc1C)Oc1ncc(cc1Cl)C(F)(F)F
CHEMBL3806055 ffar1_human Human No 5.8 EC50 = 1770 nM Funct
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
397 8 2 6 3.7 Cc1cccc(NC(=O)c2nnc(COc3ccc(CCC(=O)O)cc3)s2)c1
CHEMBL4126802 ffar1_human Human No 4.8 EC50 = 17750 nM Funct
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
463 10 1 6 4.8 COc1ccc(C(OCCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)cc1
CHEMBL4444223 ffar1_human Human No 5.8 EC50 = 1780 nM Funct
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
442 7 1 4 5.4 O=C(O)CCc1ccc(OC[C@@H]2COc3ccc(-c4ccc(Cl)cc4)cc3O2)cc1F
CHEMBL207881 ffar1_human Human Yes 4.8 EC50 = 17800 nM Funct
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
347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1
CHEMBL4165184 ffar1_human Human No 6.8 EC50 = 179 nM Funct
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
505 7 1 3 6.0 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)cc2)cc1
CHEMBL3804883 ffar1_human Human No 4.8 EC50 = 17940 nM Funct
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
383 8 2 6 3.4 O=C(O)CCc1nnc(C(=O)Nc2ccc(OCc3ccccc3)cc2)s1
CHEMBL4794233 ffar1_mouse Mouse No 7.8 EC50 = 18 nM Bind
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
512 8 1 5 6.2 CC#C[C@@H](CC(=O)O)c1ccc(OCc2sc(CN3CCC4(C=Cc5ccccc54)CC3)nc2C)cc1
CHEMBL4784555 ffar1_rat Rat No 7.8 EC50 = 18 nM Bind
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
538 9 1 5 5.8 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CC3)CN(C)c3ccc(OC)cc34)cc2)cc1
CHEMBL2047152 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
488 9 1 5 5.9 Cc1cc(OCC2(C)COC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
CHEMBL2047162 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
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
CHEMBL2047166 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
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
CHEMBL4217348 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
556 11 1 7 6.5 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(F)c(-c4ccc(OCCOC)cc4C)c3c2)cc1
CHEMBL600799 ffar1_human Human No 7.8 EC50 = 18 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
415 4 1 4 5.4 Cc1cc(Oc2ccc(C(F)(F)F)cc2Cl)ccc1CC1SC(=O)NC1=O
CHEMBL3288357 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
379 7 1 3 5.4 Cc1cccc(C)c1-c1cccc(COc2ccc(C(F)CC(=O)O)cn2)c1
CHEMBL4787628 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
509 8 1 3 6.5 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL4207273 ffar1_rat Rat No 7.8 EC50 = 18 nM Funct
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
466 7 1 7 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4cncnc4C)c3c2)cc1
CHEMBL1688486 ffar1_rat Rat No 7.8 EC50 = 18 nM Funct
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
360 7 1 2 5.6 Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1
CHEMBL4764729 ffar1_rat Rat No 7.8 EC50 = 18 nM Funct
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
517 10 1 6 6.4 COc1cc(-c2ncc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)nc2C2=CCCC2(C)C)c(F)cn1
CHEMBL3883407 ffar1_human Human No 7.8 EC50 = 18 nM Funct
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
446 7 1 3 6.5 COc1ccc(F)c(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)c1
CHEMBL2386355 ffar1_human Human No 7.7 EC50 = 18.2 nM Funct
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
321 5 1 2 3.7 N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1
CHEMBL2386364 ffar1_human Human No 7.7 EC50 = 18.2 nM Funct
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
336 4 1 1 4.3 O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F
CHEMBL4228406 ffar1_human Human No 7.7 EC50 = 18.6 nM Funct
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
413 6 1 5 5.1 Cc1noc(C)c1-c1cc(COc2ccc3c(c2)OCC3CC(=O)O)ccc1Cl
CHEMBL2386353 ffar1_human Human Yes 7.7 EC50 = 18.6 nM Bind
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
307 4 1 2 3.3 N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O
CHEMBL1773261 ffar1_human Human Yes 7.7 EC50 = 18.6 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL1773261 ffar1_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL1773261 ffar1_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL2385470 ffar1_human Human No 6.8 EC50 = 180 nM Bind
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
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
CHEMBL1939648 ffar1_human Human No 6.8 EC50 = 180 nM Funct
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
308 6 1 2 4.2 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C)cc2)cc1
CHEMBL4786992 ffar1_human Human No 6.8 EC50 = 180 nM Funct
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
543 11 1 6 5.6 COc1ccc(C(=O)N(C)c2ccccn2)c(N2CCC(COc3cccc(C(CC(=O)O)C4CC4)c3)CC2)c1
CHEMBL4070721 ffar1_human Human No 6.8 EC50 = 180 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL2022254 ffar1_human Human No 6.8 EC50 = 180 nM Funct
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
416 6 1 4 6.1 O=C(O)CC1COc2cc(OCc3cccc(-c4ccc5sccc5c4)c3)ccc21
CHEMBL4783190 ffar1_human Human No 6.8 EC50 = 180 nM Funct
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
471 8 1 3 6.0 O=C(O)CCc1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL251963 ffar1_human Human Yes 5.8 EC50 = 1800 nM Funct
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
348 6 1 6 4.2 O=C(O)CSc1nnc(SCc2cccc3ccccc23)s1
CHEMBL1688469 ffar1_human Human No 5.8 EC50 = 1800 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
376 7 1 2 6.3 Cc1cccc(C)c1-c1cccc(CSc2ccc(CCC(=O)O)cc2)c1
CHEMBL4165039 ffar1_human Human No 5.8 EC50 = 1800 nM Funct
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
293 5 2 1 4.4 CCc1ccccc1-c1cc2cc(CCC(=O)O)ccc2[nH]1
CHEMBL4171403 ffar1_human Human No 5.8 EC50 = 1800 nM Funct
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
343 4 2 1 4.6 O=C(O)CCc1ccc2[nH]c(-c3cccc(Br)c3)cc2c1
CHEMBL267476 ffar1_human Human Yes 5.8 EC50 = 1800 nM Funct
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
280 14 1 1 5.9 CCCCC/C=C\C/C=C\CCCCCCCC(=O)O
CHEMBL4289432 ffar1_human Human No 5.8 EC50 = 1800 nM Funct
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
346 4 1 2 4.5 O=C(O)C#Cc1ccc(OCc2cccc(-c3cccc(F)c3)c2)cc1
CHEMBL4071290 ffar1_human Human No 4.7 EC50 = 18051 nM Funct
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
318 6 1 2 4.6 Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1
CHEMBL2164242 ffar1_rat Rat Yes 6.7 EC50 = 182.0 nM Funct
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
499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C
CHEMBL234057 ffar1_human Human No 6.7 EC50 = 182.0 nM Funct
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
347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1
CHEMBL3787151 ffar1_human Human No 5.7 EC50 = 1819.7 nM Funct
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
278 5 1 1 3.7 O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1
CHEMBL3896657 ffar1_human Human No 5.7 EC50 = 1829 nM Funct
Agonist activity at human GPR40 assessed as induction of IP1 accumulationAgonist activity at human GPR40 assessed as induction of IP1 accumulation
368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1
CHEMBL3896657 ffar1_human Human No 5.7 EC50 = 1829 nM Funct
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
368 5 1 3 5.2 O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1
CHEMBL4205339 ffar1_human Human No 5.7 EC50 = 1830 nM Funct
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
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
CHEMBL4456869 ffar1_human Human No 6.7 EC50 = 185 nM Bind
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
391 7 1 5 4.4 Cc1nc(-c2cccc(F)c2)sc1COc1ccc(OCC(=O)O)c(F)c1
CHEMBL2315248 ffar1_human Human No 6.7 EC50 = 186.2 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
292 4 1 2 3.3 CC(=O)c1ccccc1C#Cc1ccc(CCC(=O)O)cc1
CHEMBL1829162 ffar1_human Human No 6.7 EC50 = 186.2 nM Funct
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryAgonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
327 4 1 2 4.2 O=C(O)CCc1ccc(C#Cc2ccnc(-c3ccccc3)c2)cc1
CHEMBL1773256 ffar1_human Human No 6.7 EC50 = 186.2 nM Funct
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
323 6 2 2 4.3 O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1
CHEMBL1688455 ffar1_human Human Yes 4.7 EC50 = 18600 nM Funct
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
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1
CHEMBL4213909 ffar1_human Human Yes 4.7 EC50 = 18600 nM Funct
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
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1
CHEMBL4279005 ffar1_human Human Yes 4.7 EC50 = 18620.9 nM Funct
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
216 10 2 2 3.0 CCCCCCC(O)CCCCC(=O)O
CHEMBL3817889 ffar1_human Human No 6.7 EC50 = 187 nM Funct
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
630 16 2 10 6.3 Cc1cc(OCCOCCNc2ccc([N+](=O)[O-])c3nonc23)ccc1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1
CHEMBL4160566 ffar1_human Human No 6.7 EC50 = 187 nM Funct
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
533 9 1 7 4.8 CC#CC(CC(=O)O)c1ccc(OCc2ccc(C(=O)N3CCN(c4cccc([N+](=O)[O-])c4)CC3)s2)cc1
CHEMBL601850 ffar1_human Human No 5.7 EC50 = 1872 nM Funct
Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAAgonist activity at human GPR40 by FLIPR assay in presence of 1% BSA
334 4 1 5 3.4 O=C1NC(=O)C(Cc2ccc(Oc3ccc(Cl)cn3)cc2)S1
CHEMBL3601061 ffar1_human Human Yes 4.7 EC50 = 18800 nM Funct
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
344 6 1 5 3.6 O=C(O)Cc1ccc(OCc2nc(-c3cccc(Cl)c3)no2)cc1
CHEMBL3758197 ffar1_human Human No 5.7 EC50 = 1890 nM Funct
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
409 7 1 6 4.2 CC(C)Cn1c(COc2ccc(CC3SC(=O)NC3=O)cc2)nc2ccccc21
CHEMBL1773261 ffar1_mouse Mouse Yes 7.7 EC50 = 19 nM Bind
Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretionActivation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
345 7 2 2 5.3 Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1
CHEMBL1688487 ffar1_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSAAgonist activity against human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR assay in presence of 0.1% BSA
360 7 1 2 5.6 Cc1cccc(-c2cccc(COc3ccc(CCC(=O)O)cc3)c2)c1C
CHEMBL474195 ffar1_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at GPR40Agonist activity at GPR40
548 13 1 5 7.8 O=C(O)CCc1ccc(OCc2ccc(CC(CCc3ccccn3)c3nc(-c4ccccc4)cs3)cc2)cc1
CHEMBL3265146 ffar1_human Human No 7.7 EC50 = 19 nM Funct
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
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
CHEMBL2047167 ffar1_human Human No 7.7 EC50 = 19 nM Funct
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
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
CHEMBL2047161 ffar1_human Human No 7.7 EC50 = 19 nM Funct
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
501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
CHEMBL2079433 ffar1_human Human No 7.7 EC50 = 19 nM Funct
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
501 8 1 5 6.0 Cc1cc(OC2CCN(C)CC2)cc(C)c1-c1cccc(COc2ccc3c(c2)OC[C@H]3CC(=O)O)c1
CHEMBL4202612 ffar1_human Human No 7.7 EC50 = 19 nM Funct
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
542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1
CHEMBL3427713 ffar1_human Human No 7.7 EC50 = 19 nM Funct
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
394 7 1 3 5.3 CCO[C@@H](CC(=O)O)c1ccc(O[C@H]2CCc3c2cccc3C(F)(F)F)cc1
CHEMBL3604041 ffar1_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
334 8 1 3 4.5 CCOC(CC(=O)O)c1ccc(OCc2cccc(Cl)c2)cc1
CHEMBL4791842 ffar1_human Human Yes 7.7 EC50 = 19 nM Funct
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
493 8 1 3 6.3 CC#C[C@@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(CCc5ccccc54)CC3)cc2)cc1
CHEMBL4202612 ffar1_rat Rat No 7.7 EC50 = 19 nM Funct
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
542 7 1 5 7.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(Br)c(-c4ccccc4C)c3c2)cc1
CHEMBL4206640 ffar1_rat Rat No 7.7 EC50 = 19 nM Funct
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
554 11 3 8 5.1 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3scc(-c4ccc(OCC(O)CO)cc4C)c3c2)cc1
CHEMBL4206968 ffar1_rat Rat No 7.7 EC50 = 19 nM Funct
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
489 7 1 6 6.2 CC#C[C@@H](Cc1nnn[nH]1)c1ccc(OCc2ccc3sc(C#N)c(-c4ccccc4C)c3c2)cc1
CHEMBL4166943 ffar1_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assayAgonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay
429 7 1 4 5.8 COc1cc(-c2ccc(C3CCc4ccc([C@@H](CC(=O)O)C5CC5)cc4O3)cc2)ccn1
CHEMBL2381308 ffar1_human Human No 7.7 EC50 = 19.1 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
402 4 1 4 5.1 Cc1ccccc1-c1cccc([C@H]2COc3cc4c(cc3O2)OC[C@H]4CC(=O)O)c1
CHEMBL4438440 ffar1_human Human No 7.7 EC50 = 19.3 nM Funct
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
385 7 2 3 5.2 O=C(O)COc1ccc(NCc2cccc(-c3ccccc3Cl)c2)cc1F
CHEMBL2315528 ffar1_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1
CHEMBL2315528 ffar1_human Human No 7.7 EC50 = 20.0 nM Funct
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
289 4 1 2 3.2 N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1
CHEMBL3604064 ffar1_human Human No 6.7 EC50 = 190 nM Funct
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assayAgonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
356 8 1 4 4.3 CCO[C@@H](CC(=O)O)c1ccc(OC2CCc3c(OC)cccc32)cc1
CHEMBL4079421 ffar1_human Human No 6.7 EC50 = 190 nM Funct
Agonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assayAgonist activity at human GPR40 expressed in CHO-A12 cells assessed as increase in intracellular calcium flux measured for 100 secs by FLIPR assay
325 6 1 3 4.0 Cc1ccccc1COc1ccc(N2CCC[C@H]2CC(=O)O)cc1
CHEMBL4104467 ffar1_human Human No 6.7 EC50 = 190 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL4786299 ffar1_human Human No 6.7 EC50 = 190 nM Funct
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
509 8 1 3 6.5 CC#C[C@H](CC(=O)O)c1ccc(OCc2ccc(CN3CCC4(C=Cc5ccccc54)CC3)cc2)cc1F
CHEMBL3288360 ffar1_rat Rat No 6.7 EC50 = 190 nM Funct
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
389 6 1 4 5.0 Cc1cccc(C)c1-c1cccc(COc2cc3c(cn2)C(CC(=O)O)OC3)c1
CHEMBL3330548 ffar1_human Human No 6.7 EC50 = 190 nM Bind
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
484 7 1 5 6.4 COc1cccc(-c2ccc(Oc3ccc(N4N=C(C(F)(F)F)CC4CC(=O)O)cc3)c(C)c2)c1
CHEMBL3752557 ffar1_human Human No 6.7 EC50 = 190 nM Bind
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
477 8 1 3 7.0 O=C(O)CC(c1ccncc1)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1
CHEMBL3753088 ffar1_human Human No 6.7 EC50 = 190 nM Bind
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
482 8 1 3 7.6 O=C(O)CC(c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1)c1cccs1
CHEMBL2381288 ffar1_human Human No 6.7 EC50 = 190.5 nM Funct
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assayAgonist activity at human GPR40 transfected in CHO cells by calcium flux assay
380 3 1 4 4.5 O=C(O)C[C@@H]1COc2cc3c(cc21)OC[C@H](c1ccc(Cl)c(Cl)c1)O3
CHEMBL2315529 ffar1_human Human No 6.7 EC50 = 190.6 nM Funct
Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysisAgonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis
289 4 1 2 3.2 N#CCc1cccc(C#Cc2ccc(CCC(=O)O)cc2)c1
CHEMBL4210871 ffar1_human Human No 6.7 EC50 = 190.6 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
421 7 1 6 3.7 Cc1nc(-c2ccc(F)cc2)sc1COc1ccc(S(=O)(=O)CC(=O)O)cc1
CHEMBL2151291 ffar1_human Human No 5.7 EC50 = 1900 nM Funct
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
380 8 1 3 5.1 COc1ccc(F)c(-c2ccc(COc3ccc(CCC(=O)O)cc3)cc2)c1
CHEMBL2151298 ffar1_human Human No 5.7 EC50 = 1900 nM Funct
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
476 9 1 3 7.3 COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C(C)(C)C)c1
CHEMBL4071899 ffar1_mouse Mouse No 5.7 EC50 = 1900 nM Funct
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
433 7 1 3 5.8 COc1ccc(F)c(-c2ccc(Cc3ccc(N4CCC[C@H]4CC(=O)O)cc3)c(C)c2)c1
CHEMBL4095599 ffar1_mouse Mouse No 5.7 EC50 = 1900 nM Funct
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
323 5 1 2 4.3 Cc1ccccc1Cc1ccc(N2CC[C@H](C)[C@H]2CC(=O)O)cc1
CHEMBL255071 ffar1_human Human Yes 4.7 EC50 = 19000 nM Funct
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
313 5 1 5 2.8 O=C(O)CCCN1C(=O)/C(=C\c2cccs2)SC1=S
CHEMBL463785 ffar1_human Human Yes 4.7 EC50 = 19000 nM Funct
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
376 10 1 4 4.7 OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1
CHEMBL4068825 ffar1_mouse Mouse No 4.7 EC50 = 19000 nM Funct
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
368 5 1 5 4.0 N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1
CHEMBL4082057 ffar1_mouse Mouse No 4.7 EC50 = 19000 nM Funct
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
369 4 1 4 4.6 Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@H]4C(=O)O)cc3)ccc12
CHEMBL1688455 ffar1_human Human Yes 5.7 EC50 = 1905.5 nM Funct
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
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1
CHEMBL4213909 ffar1_human Human Yes 5.7 EC50 = 1905.5 nM Funct
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
332 7 1 2 5.0 O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1
CHEMBL4747554 ffar1_human Human No 4.7 EC50 = 19054.6 nM Bind
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
288 6 1 2 3.7 Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1
CHEMBL3797836 ffar1_human Human No 5.7 EC50 = 1930 nM Funct
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
370 7 1 5 4.1 Cc1noc(C)c1-c1ccnc(COc2ccc(CCC(=O)O)c(F)c2)c1
CHEMBL4078050 ffar1_human Human No 5.7 EC50 = 1930 nM Funct
Agonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assayAgonist activity at human GPR40 expressed in CHOA12 cells assessed as induction of Ca2+ mobilization by FLIPR assay
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
CHEMBL234057 ffar1_human Human No 6.7 EC50 = 195.0 nM Funct
Agonist activity at GPR40 receptorAgonist activity at GPR40 receptor
347 8 2 3 5.1 O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1
CHEMBL4206179 ffar1_human Human No 6.7 EC50 = 195.0 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
412 8 1 5 3.8 COc1ccccc1-c1cccc(COc2ccc(S(=O)(=O)CC(=O)O)cc2)c1
CHEMBL4214140 ffar1_human Human No 6.7 EC50 = 195.0 nM Funct
Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assayAgonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by Fluo 4AM dye-based FLIPR assay
378 7 1 3 5.7 Cc1cccc(C)c1-c1cccc(COc2ccc(SCC(=O)O)cc2)c1
CHEMBL2386367 ffar1_human Human No 5.7 EC50 = 1949.8 nM Funct
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
360 5 1 3 2.8 CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1
CHEMBL2164242 ffar1_human Human Yes 5.7 EC50 = 1949.8 nM Funct
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
499 12 2 5 5.2 OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C
CHEMBL3759866 ffar1_human Human No 4.7 EC50 = 19580 nM Funct
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
463 10 1 6 5.2 COc1cccc(O[C@@H](CCOc2ccc(CC3SC(=O)NC3=O)cc2)c2ccccc2)c1
CHEMBL4074009 ffar1_human Human No 4.7 EC50 = 19588 nM Funct </