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 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]
