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 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]
