GW7845 [Ligand Id: 2704] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL106666 (GW7845) |
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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 | Binding affinity to human Peroxisome proliferator activated receptor alpha using scintillation proximity assay | B | 5.96 | pKi | 1100 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Maximal reporter activity against human Peroxisome proliferator activated receptor alpha Gal4 chimeric in transiently transfected CV-1 cells by functional assay. | F | 5.46 | pEC50 | 3500 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Agonist activity for Human PPAR alpha receptor in transcriptional activation assay | F | 5.46 | pEC50 | 3500 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Transactivation of Homo sapiens (human) PPARalpha assessed as luciferase activity by reporter gene assay | B | 5.46 | pEC50 | 3467.37 | nM | EC50 | Med Chem Res (2012) 21: 2873-2884 |
| 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 bind to human Peroxisome proliferator activated receptor delta using scintillation proximity assay | B | 5.92 | pKi | 1200 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| GtoPdb | - | - | 8.43 | pKi | - | - | - |
J Med Chem (1998) 41: 5020-36 [PMID:9836620]; J Med Chem (1998) 41: 5055-69 [PMID:9836622] |
| ChEMBL | Binding affinity against peroxisome proliferator activated receptor gamma (PPAR-gamma) | B | 8.43 | pKi | 3.71 | nM | Ki | J Med Chem (1998) 41: 5055-5069 [PMID:9836622] |
| ChEMBL | Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Inhibition of BRL-49653 stimulated human PPARgamma transactivation in CV-1 cells by GAL4 reporter assay | B | 5 | pIC50 | <10000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3916-3920 [PMID:17533125] |
| ChEMBL | Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay. | F | 9.15 | pEC50 | 0.71 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Agonist activity for Human PPAR gamma receptor in transcriptional activation assay | F | 9.15 | pEC50 | 0.71 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | in vitro agonist activity against peroxisome proliferator activated receptor-gamma (PPAR-gamma), using alkaline phosphatase activity transactivator assay | F | 9.15 | pEC50 | 0.71 | nM | EC50 | J Med Chem (1998) 41: 5055-5069 [PMID:9836622] |
| ChEMBL | Transactivation of Homo sapiens (human) PPARgamma assessed as luciferase activity by reporter gene assay | B | 9.15 | pEC50 | 0.71 | nM | EC50 | Med Chem Res (2012) 21: 2873-2884 |
| ChEMBL | Transactivation of human PPARgamma in CV-1 cells by GAL4 reporter assay | B | 9.2 | pEC50 | 0.63 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 3916-3920 [PMID:17533125] |
| ChEMBL | -log concentration required to induce 50% maximum lipogenic activity against Peroxisome proliferator activated receptor gamma | F | 9.21 | pEC50 | 0.62 | nM | EC50 | J Med Chem (1998) 41: 5055-5069 [PMID:9836622] |
| 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 for murine PPAR gamma receptor in transcriptional activation assay | F | 8.92 | pEC50 | 1.2 | 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]
