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 Agonist activity at human PPARalpha transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay B 5.6 pEC50 2500 nM EC50 J Med Chem (2021) 64: 6996-7032 [PMID:33988379]
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 PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay B 7.57 pEC50 26.9 nM EC50 J Med Chem (2021) 64: 6996-7032 [PMID:33988379]
ChEMBL Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay B 7.74 pEC50 18 nM EC50 Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359]
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 human PPARdelta measured by dual luciferase reporter gene assay B 7.89 pEC50 13 nM EC50 Eur J Med Chem (2022) 229: 114061-114061 [PMID:34954593]
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 Agonist activity at pBIND tagged human PPARdelta expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assay B 8 pEC50 10 nM EC50 Bioorg Med Chem (2022) 56: 116615-116615 [PMID:35051813]
ChEMBL Agonist activity at PPARdelta (unknown origin) by Alpha Screen assay B 8.4 pEC50 4 nM EC50 Medchemcomm (2019) 10: 1412-1419 [PMID:31673308]
ChEMBL Agonist activity at human PPAR-delta B 8.4 pEC50 4 nM EC50 J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL Agonist activity at human PPARdelta expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assay B 8.46 pEC50 3.5 nM EC50 J Med Chem (2022) 65: 1961-1978 [PMID:35089724]
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 Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay B 5.02 pEC50 9530 nM EC50 J Med Chem (2021) 64: 6996-7032 [PMID:33988379]
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 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]