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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 |
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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 GPR40 (unknown origin) | B | 7.32 | pEC50 | 48 | nM | EC50 | J Med Chem (2021) 64: 4312-4332 [PMID:33843223] |
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 | 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] |
ChEMBL | Agonist activity at GPR120 (unknown origin) | B | 5.46 | pEC50 | 3500 | nM | EC50 | J Med Chem (2021) 64: 4312-4332 [PMID:33843223] |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]