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] There should be some charts here, you may need to enable JavaScript!
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
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) assessed as transcriptional activation	B	7.35	pEC50	45	nM	EC50	Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
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]
ChEMBL	Agonist activity at PPARgamma (unknown origin) assessed as transcriptional activation	B	6.76	pEC50	175	nM	EC50	Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
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 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]