GW9578 [Ligand Id: 2673] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL278590 (GSK9578, GW9578) |
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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]
