elafibranor [Ligand Id: 11135] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3707395 (Elafibranor, Gft505, GFT-505, GFT505)
  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
ChEMBL Inhibition of NLRP3 in mouse J774A.1 cells infected with FLA-ST assessed as inhibition of LPS- induced IL-1beta production by ELISA B 4.4 pIC50 39600 nM IC50 Eur J Med Chem (2021) 219: 113417-113417 [PMID:33845232]
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 (unknown origin) B 6.09 pEC50 820.3 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
ChEMBL Agonist activity at human Gal4 fused PPARalpha LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay B 6.12 pEC50 760 nM EC50 Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603]
ChEMBL Agonist activity at human PPARalpha transfected in human HepG2 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay B 6.43 pEC50 375 nM EC50 Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359]
ChEMBL Agonist activity at PPARalpha (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay B 6.65 pEC50 225 nM EC50 ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410]
ChEMBL Agonist activity at PPARalpha (unknown origin) B 8 pEC50 10 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
GtoPdb - - 8.22 pEC50 6 nM EC50 Expert Opin Pharmacother (2014) 15: 493-503 [PMID:24428677]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Agonist activity at PPARdelta (unknown origin) B 6.07 pEC50 842.9 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
ChEMBL Agonist activity at human Gal4 fused PPARdelta LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay B 6.14 pEC50 730 nM EC50 Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603]
ChEMBL Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay B 6.6 pEC50 249 nM EC50 Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359]
ChEMBL Agonist activity at PPARbeta (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay B 6.94 pEC50 115 nM EC50 ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410]
ChEMBL Agonist activity at PPARdelta (unknown origin) B 8 pEC50 10 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
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 human PPARgamma transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay B 5.4 pEC50 3962 nM EC50 Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359]
ChEMBL Agonist activity at human Gal4 fused PPARgamma LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay B 5.55 pEC50 2790 nM EC50 Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603]
ChEMBL Agonist activity at PPARgamma (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay B 5.67 pEC50 2116 nM EC50 ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410]
ChEMBL Agonist activity at PPARgamma (unknown origin) B 5.73 pEC50 1843.8 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
GtoPdb - - 7.33 pEC50 47 nM EC50 Expert Opin Pharmacother (2014) 15: 493-503 [PMID:24428677]

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]