LY-510929 [Ligand Id: 2657] 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: CHEMBL77502
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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 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]