LY-510929 [Ligand Id: 2657] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL77502 |
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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 | Agonist activity at PPARalpha | F | 7.35 | pIC50 | 44.98 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| GtoPdb | - | - | 7.55 | pIC50 | - | - | - | J Med Chem (2004) 47: 2422-5 [PMID:15115385] |
| ChEMBL | Displacement of PPAR-alpha/delta agonist from human Peroxisome proliferator activated receptor alpha | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2004) 47: 2422-2425 [PMID:15115385] |
| ChEMBL | Agonist activity at PPARalpha | F | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Transcriptional activation of reporter assay by human Peroxisome proliferator activated receptor alpha in CV-1 cells | B | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2004) 47: 2422-2425 [PMID:15115385] |
| ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 8.05 | pEC50 | 9 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
| ChEMBL | Transactivation of Homo sapiens (human) PPARalpha assessed as luciferase activity by reporter gene assay | B | 8.05 | pEC50 | 8.91 | nM | EC50 | Med Chem Res (2012) 21: 2873-2884 |
| ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 8.05 | pEC50 | 8.91 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Displacement of PPAR-alpha/delta agonist from human Peroxisome proliferator activated receptor delta | F | 5.28 | pIC50 | 5253 | nM | IC50 | J Med Chem (2004) 47: 2422-2425 [PMID:15115385] |
| ChEMBL | Agonist activity at PPARdelta | F | 5.28 | pIC50 | 5253 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Agonist activity at PPARdelta | F | 5.28 | pIC50 | 5248.07 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Agonist activity at PPARgamma | F | 7.62 | pIC50 | 23.99 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| GtoPdb | - | - | 8 | pIC50 | - | - | - |
Ann NY Acad Sci (1988) 547: 1-541 [PMID:3071214]; J Med Chem (2004) 47: 2422-5 [PMID:15115385] |
| ChEMBL | Displacement of PPARgamma agonist from human PPAR gamma receptor | F | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2004) 47: 2422-2425 [PMID:15115385] |
| ChEMBL | Agonist activity at PPARgamma | F | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Transcriptional activation of reporter assay by PPAR gamma receptor in CV-1 cells | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (2004) 47: 2422-2425 [PMID:15115385] |
| ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARgamma DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 8.4 | pEC50 | 4 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
| ChEMBL | Transactivation of Homo sapiens (human) PPARgamma assessed as luciferase activity by reporter gene assay | B | 8.4 | pEC50 | 3.98 | nM | EC50 | Med Chem Res (2012) 21: 2873-2884 |
| ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARgamma DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 8.4 | pEC50 | 3.98 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
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]
