GW9508 [Ligand Id: 1050] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL207881 (GW9508) |
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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] |
| ChEMBL | Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interval for 90 secs by Calcium-3 dye based FLIPR assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127650-127650 [PMID:33127539] |
| GtoPdb | - | - | 7.3 | pEC50 | - | - | - | Br J Pharmacol (2006) 148: 619-28 [PMID:16702987] |
| ChEMBL | Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay | F | 7.3 | pEC50 | 50 | nM | EC50 | J Med Chem (2021) 64: 4130-4149 [PMID:33769827] |
| 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 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 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 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 | F | 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 | F | 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 human FFA4 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at every 1 secs for 60 secs by Calcium-3 dye based FLIPR assay | F | 5.5 | pEC50 | 3162.28 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127650-127650 [PMID:33127539] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
