GW0742X [Ligand Id: 2686] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL38508 (GW0742)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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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 Maximum transcriptional activation of human PPAR alpha receptor B 5.96 pEC50 1100 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]
ChEMBL Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay B 6.04 pEC50 920 nM EC50 J. Med. Chem. (2012) 55: 4978-4989 [PMID:22582973]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Activity against murine PPAR alpha receptor B 5.06 pEC50 8800 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Binding affinity to human PPARdelta (unknown origin) by competitive TR-FRET assay B 9.4 pKd 0.4 nM Kd J. Med. Chem. (2013) 56: 1535-1543 [PMID:23286787]
GtoPdb - - 9 pIC50 - - - Atherosclerosis (2005) 181: 29-37 [PMID:15939051];
Bioorg Med Chem Lett (2003) 13: 1517-21 [PMID:12699745]
ChEMBL Binding affinity for human PPAR delta receptor B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]
ChEMBL Agonist activity at human PPARdelta LBD by cell based luciferase reporter gene assay F 6.52 pEC50 300 nM EC50 J. Med. Chem. (2011) 54: 788-808 [PMID:21218783]
ChEMBL Activation of PPARbeta-LBD (unknown origin) assessed as fluorescein-labeled coactivator C33 recruitment by TR-FRET assay B 7.17 pEC50 67.11 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 3978-3983 [PMID:27450788]
ChEMBL Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay B 7.89 pEC50 13 nM EC50 Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay B 7.89 pEC50 13 nM EC50 Eur J Med Chem (2019) 164: 352-365 [PMID:30605833]
ChEMBL Agonist activity at PPARdelta (unknown origin) by Alpha Screen assay B 8.4 pEC50 4 nM EC50 MedChemComm (2019) 10: 1412-1419
ChEMBL Displacement of pan-PPAR fluormone from PPARdelta LBD by TR-FRET based LanthaScreen assay B 8.54 pEC50 2.9 nM EC50 J. Med. Chem. (2012) 55: 4978-4989 [PMID:22582973]
ChEMBL Agonist activity at human PPARdelta after 22 to 24 hrs by luciferase reporter gene assay B 8.7 pEC50 2 nM EC50 Bioorg Med Chem Lett (2018) 28: 2717-2722 [PMID:29628329]
ChEMBL Agonist activity at human PPARdelta expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 to 24 hrs by luciferase reporter gene assay B 8.72 pEC50 1.9 nM EC50 J Med Chem (2020) 63: 2854-2876 [PMID:32096640]
ChEMBL Agonist activity at PPARdelta (unknown origin) B 9 pEC50 1 nM EC50 Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL Maximum transcriptional activation of human PPAR delta receptor B 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Activity against murine PPAR delta receptor B 7.52 pEC50 30 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]
ChEMBL Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay F 8.24 pEC50 <=5.8 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 7239-7242 [PMID:21074432]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Maximum transcriptional activation of human PPAR gamma receptor B 5.7 pEC50 2000 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Activity against murine PPAR gamma receptor B 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1517-1521 [PMID:12699745]

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]