GW9578 [Ligand Id: 2673] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL278590 (GSK9578, GW9578)
  • 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]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230]
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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 Inhibitory activity against human Peroxisome proliferator activated receptor alpha B 6.92 pIC50 120 nM IC50 J Med Chem (2003) 46: 5121-5124 [PMID:14613314]
ChEMBL Agonist activity at PPARalpha expressed in HEK293 cells by GAL4 transactivation assay F 6.35 pEC50 450 nM EC50 Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176]
ChEMBL Cotransfection activity of compound against human Peroxisome proliferator activated receptor alpha was determined F 6.47 pEC50 340 nM EC50 J Med Chem (2003) 46: 5121-5124 [PMID:14613314]
ChEMBL Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay B 6.6 pEC50 250 nM EC50 Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963]
ChEMBL Agonist activity at Gal4-fused human PPARalpha F 7 pEC50 100 nM EC50 Bioorg Med Chem Lett (2010) 20: 3376-3379 [PMID:20452212]
ChEMBL Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay F 7.11 pEC50 78 nM EC50 Bioorg Med Chem Lett (2007) 17: 937-941 [PMID:17157019]
GtoPdb - - 7.3 pEC50 - - - Diabetes (1999) 48: 1415-24 [PMID:10389847];
J Med Chem (1999) 42: 3785-8 [PMID:10508427];
Bioorg Med Chem Lett (2001) 11: 1225-7 [PMID:11354382]
ChEMBL Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells F 7.3 pEC50 50 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity for Human PPAR alpha receptor in transcriptional activation assay F 7.3 pEC50 50 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR alpha ligand binding domain B 7.3 pEC50 50 nM EC50 Bioorg Med Chem Lett (2001) 11: 1225-1227 [PMID:11354382]
ChEMBL Agonist activity at human PPARalpha F 8.22 pEC50 6 nM EC50 J Med Chem (2012) 55: 4027-4061 [PMID:22260081]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Agonist activity at Gal4-fused mouse PPARalpha F 8 pEC50 10 nM EC50 Bioorg Med Chem Lett (2010) 20: 3376-3379 [PMID:20452212]
ChEMBL Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells F 8.3 pEC50 5 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity for murine PPAR alpha receptor in transcriptional activation assay F 8.3 pEC50 5 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230]
ChEMBL Agonist activity at rat PPARalpha in rat H4IIE cells assessed as gene induction F 6.78 pEC50 166 nM EC50 Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Agonist activity at Gal4-fused human PPARdelta F 5.7 pEC50 2000 nM EC50 Bioorg Med Chem Lett (2010) 20: 3376-3379 [PMID:20452212]
ChEMBL Compound was tested for agonist activity on human Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells F 5.85 pEC50 1400 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity for Human PPAR delta receptor in transcriptional activation assay F 5.85 pEC50 1400 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR delta ligand binding domain B 5.85 pEC50 1400 nM EC50 Bioorg Med Chem Lett (2001) 11: 1225-1227 [PMID:11354382]
GtoPdb - - 5.9 pEC50 - - - Bioorg Med Chem Lett (2001) 11: 1225-7 [PMID:11354382]
ChEMBL Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay B 6 pEC50 1000 nM EC50 Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963]
ChEMBL Agonist activity at PPARdelta expressed in HEK293 cells by GAL4 transactivation assay F 6.82 pEC50 150 nM EC50 Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells F 5.59 pEC50 2600 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity for murine PPAR delta receptor in transcriptional activation assay F 5.59 pEC50 2600 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL Agonist activity at Gal4-fused mouse PPARdelta F 5.7 pEC50 2000 nM EC50 Bioorg Med Chem Lett (2010) 20: 3376-3379 [PMID:20452212]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Inhibitory activity of compound against the binding of human Peroxisome proliferator activated receptor gamma was determined B 6.26 pIC50 550 nM IC50 J Med Chem (2003) 46: 5121-5124 [PMID:14613314]
ChEMBL Cotransfection activity of compound against human Peroxisome proliferator activated receptor gamma was determined F 5.72 pEC50 1900 nM EC50 J Med Chem (2003) 46: 5121-5124 [PMID:14613314]
GtoPdb - - 6 pEC50 - - - Bioorg Med Chem Lett (2001) 11: 1225-7 [PMID:11354382]
ChEMBL Agonist activity for Human PPAR gamma receptor in transcriptional activation assay F 6 pEC50 1000 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR gamma ligand binding domain B 6 pEC50 1000 nM EC50 Bioorg Med Chem Lett (2001) 11: 1225-1227 [PMID:11354382]
ChEMBL Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells F 6 pEC50 1000 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity at Gal4-fused human PPARgamma F 6 pEC50 1000 nM EC50 Bioorg Med Chem Lett (2010) 20: 3376-3379 [PMID:20452212]
ChEMBL Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay F 6.3 pEC50 500 nM EC50 Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176]
ChEMBL Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay B 6.6 pEC50 250 nM EC50 Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Agonist activity at Gal4-fused mouse PPARgamma F 5.6 pEC50 2500 nM EC50 Bioorg Med Chem Lett (2010) 20: 3376-3379 [PMID:20452212]
ChEMBL Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells F 5.82 pEC50 1500 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity for murine PPAR gamma receptor in transcriptional activation assay F 5.82 pEC50 1500 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]

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]