GW9578 [Ligand Id: 2673] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL278590 (GSK9578, GW9578) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
