GW2331 [Ligand Id: 2680] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL248906 (GW2331)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Inhibition of PPARalpha B 6.13 pIC50 740 nM IC50 Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645]
ChEMBL Inhibition of human Peroxisome proliferator activated receptor alpha B 6.27 pIC50 538 nM IC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Displacement of fluorescein labeled ligand from PPARalpha receptor by fluorescence polarization assay B 6.46 pIC50 348 nM IC50 Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL Agonist activity at PPARalpha receptor expressed in HEK293 cells by GAL4 transactivation assay F 7.15 pEC50 71 nM EC50 Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay F 7.35 pEC50 45 nM EC50 Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645]
ChEMBL Effective concentration against human Peroxisome proliferator activated receptor alpha B 7.7 pEC50 <20 nM EC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Displacement of fluorescein labeled ligand from PPARgamma receptor by fluorescence polarization assay B 6.17 pIC50 670 nM IC50 Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL Inhibition of PPARgamma B 6.22 pIC50 600 nM IC50 Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645]
ChEMBL Inhibition of human Peroxisome proliferator activated receptor gamma B 6.5 pIC50 316 nM IC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Effective concentration against human Peroxisome proliferator activated receptor gamma B 6.37 pEC50 425 nM EC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay F 6.6 pEC50 249 nM EC50 Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay F 6.61 pEC50 243 nM EC50 Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645]

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]