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 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]