GW9508 [Ligand Id: 1050] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL207881 (GW9508)
  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
  • FFA1 receptor/Free fatty acid receptor 1 in Rat [ChEMBL: CHEMBL1795180] [GtoPdb: 225] [UniProtKB: Q8K3T4]
  • This target only has 1 pki data point
  • 0
1 CHEMBL207881_lig_chart_1 Free fatty acid receptor 1 HumanRat
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  • FFA2 receptor/Free fatty acid receptor 2 in Human [ChEMBL: CHEMBL5493] [GtoPdb: 226] [UniProtKB: O15552]
  • This target only has 0 pki data point
  • 0
2 CHEMBL207881_lig_chart_2 Free fatty acid receptor 2 Human
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  • FFA3 receptor/Free fatty acid receptor 3 in Human [ChEMBL: CHEMBL5201] [GtoPdb: 227] [UniProtKB: O14843]
  • This target only has 0 pki data point
  • 0
3 CHEMBL207881_lig_chart_3 Free fatty acid receptor 3 Human
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  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
  • This target only has 0 pki data point
  • 0
4 CHEMBL207881_lig_chart_4 G-protein coupled receptor 120 Human
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  • HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
  • This target only has 0 pki data point
  • 0
5 CHEMBL207881_lig_chart_5 Hydroxycarboxylic acid receptor 2 Human
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • This target only has 1 pki data point
  • 5.5
6 CHEMBL207881_lig_chart_6 Peroxisome proliferator-activated receptor alpha Human
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • This target only has 1 pki data point
  • 5.5
7 CHEMBL207881_lig_chart_7 Peroxisome proliferator-activated receptor delta Human
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • This target only has 1 pki data point
  • 5.5
8 CHEMBL207881_lig_chart_8 Peroxisome proliferator-activated receptor gamma Human
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  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
  • This target only has 1 pki data point
  • 5.8
9 CHEMBL207881_lig_chart_9 Prostanoid EP1 receptor Human
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
  • This target only has 1 pki data point
  • 6.4
10 CHEMBL207881_lig_chart_10 Prostanoid EP3 receptor Human
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
  • This target only has 1 pki data point
  • 5.5
11 CHEMBL207881_lig_chart_11 Prostanoid EP4 receptor Human
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  • S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
  • This target only has 0 pki data point
  • 0
12 CHEMBL207881_lig_chart_12 Sphingosine 1-phosphate receptor Edg-1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay B 6.66 pKi 218.78 nM Ki J. Med. Chem. (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL Agonist activity at human GPR40 H137A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium F 4.52 pEC50 >30000 nM EC50 J. Med. Chem. (2007) 50: 2981-2989 [PMID:17552505]
ChEMBL Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium F 4.75 pEC50 17800 nM EC50 J. Med. Chem. (2007) 50: 2981-2989 [PMID:17552505]
ChEMBL Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium F 5.17 pEC50 6800 nM EC50 J. Med. Chem. (2007) 50: 2981-2989 [PMID:17552505]
ChEMBL Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium F 5.66 pEC50 2200 nM EC50 J. Med. Chem. (2007) 50: 2981-2989 [PMID:17552505]
ChEMBL Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium F 5.92 pEC50 1200 nM EC50 J. Med. Chem. (2007) 50: 2981-2989 [PMID:17552505]
ChEMBL Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation B 6.5 pEC50 316.23 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 5330-5336 [PMID:25441945]
ChEMBL Agonist activity at human GPR40 expressed in HEK-EM 293 cells assessed as increase in intracellular calcium F 6.65 pEC50 223.87 nM EC50 J. Med. Chem. (2007) 50: 2981-2989 [PMID:17552505]
ChEMBL Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSA F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1298-1301 [PMID:20064714]
ChEMBL Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay F 7.06 pEC50 87.1 nM EC50 ACS Med. Chem. Lett. (2010) 1: 345-349 [PMID:24900217]
ChEMBL Agonist activity at GPR40 receptor F 7.1 pEC50 79.43 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
ChEMBL Agonist potency at human GPR40 expressed in CHO cells F 7.19 pEC50 64.57 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 1840-1845 [PMID:16439116]
GtoPdb - - 7.3 pEC50 - - - Br J Pharmacol (2006) 148: 619-28 [PMID:16702987]
ChEMBL Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay F 7.3 pEC50 50 nM EC50 ACS Med Chem Lett (2017) 8: 1336-1340 [PMID:29259758]
ChEMBL Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye based FLIPR assay F 7.32 pEC50 48 nM EC50 Bioorg Med Chem Lett (2018) 28: 2599-2604 [PMID:29980358]
ChEMBL Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay F 7.32 pEC50 47.86 nM EC50 J. Med. Chem. (2008) 51: 7061-7064 [PMID:18947221]
ChEMBL Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry F 7.32 pEC50 47.86 nM EC50 J. Med. Chem. (2011) 54: 6691-6703 [PMID:21854074]
ChEMBL Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay F 7.54 pEC50 28.84 nM EC50 ACS Med. Chem. Lett. (2010) 1: 345-349 [PMID:24900217]
ChEMBL 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 assay B 7.55 pEC50 28.18 nM EC50 J. Med. Chem. (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay F 7.55 pEC50 28.18 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
ChEMBL Agonist activity at human GPR40 expressed in CHO cells by calcium flux assay B 7.89 pEC50 13 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2949-2953 [PMID:24835985]
FFA1 receptor/Free fatty acid receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795180] [GtoPdb: 225] [UniProtKB: Q8K3T4]
ChEMBL Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assay B 7 pEC50 99 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2949-2953 [PMID:24835985]
FFA2 receptor/Free fatty acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5493] [GtoPdb: 226] [UniProtKB: O15552]
ChEMBL Activity at GPR43 receptor B 4.3 pEC50 <50118.72 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
FFA3 receptor/Free fatty acid receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5201] [GtoPdb: 227] [UniProtKB: O14843]
ChEMBL Activity at GPR41 receptor B 4.3 pEC50 <50118.72 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL Agonist activity at human GPR120 expressed in baculovirus infected sf9 cells assessed as increase in calcium flux measured every 1 sec for 60 secs by Calcium plus dye based FLIPR assay F 5.46 pEC50 3500 nM EC50 Bioorg Med Chem Lett (2018) 28: 2599-2604 [PMID:29980358]
GtoPdb - - 5.46 pEC50 - - EC50 Br J Pharmacol (2006) 148: 619-28 [PMID:16702987];
Biol Pharm Bull (2008) 31: 1847-51 [PMID:18827341]
ChEMBL Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay F 5.85 pEC50 1412.54 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
ChEMBL Activity at HM74A receptor B 5.2 pEC50 <6309.57 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Activity at PPARalpha receptor B 5.5 pKi <3162.28 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Activity at PPARdelta receptor B 5.5 pKi <3162.28 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Activity at PPARgamma receptor B 5.5 pKi <3162.28 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Activity at EP1 receptor B 5.8 pKi <1584.89 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Activity at EP3 receptor B 6.4 pKi 398.11 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Activity at EP4 receptor B 5.5 pKi <3162.28 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]
S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
ChEMBL Activity at S1P1 receptor B 4.5 pEC50 <31622.78 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 1584-1589 [PMID:17240142]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]