ChEMBL ligand: CHEMBL24038 (Ragaglitazar)
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-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	Binding affinity for human peroxisome proliferator activated receptor alpha	B	6.01	pKi	980	nM	Ki	J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
GtoPdb	-	-	6	pIC50	-	-	-	J Med Chem (2003) 46: 1306-17 [PMID:12672231]
ChEMBL	Receptor binding affinity to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand	B	6.01	pIC50	980	nM	IC50	J Med Chem (2003) 46: 1306-1317 [PMID:12672231]
ChEMBL	Transactivation of Homo sapiens (human) PPARalpha assessed as luciferase activity by reporter gene assay	B	5.49	pEC50	3235.94	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	5.49	pEC50	3235.94	nM	EC50	Med Chem Res (2013) 22: 287-302
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	5.49	pEC50	3210	nM	EC50	Med Chem Res (2013) 22: 287-302
ChEMBL	In vitro transactivation using receptor transactivation assay against hPPAR alpha	F	5.49	pEC50	3210	nM	EC50	J Med Chem (2002) 45: 789-804 [PMID:11831892]
ChEMBL	In vitro activation of human peroxisome proliferator activated receptor alpha	B	5.49	pEC50	3210	nM	EC50	Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434]
ChEMBL	Agonist activity at GAL4-fused PPARalpha assessed as transcriptional activity by cell based assay	F	5.49	pEC50	3200	nM	EC50	Bioorg Med Chem Lett (2012) 22: 7075-7079 [PMID:23084275]
ChEMBL	Agonistic activity for Peroxisome proliferator activated receptor alpha	F	5.49	pEC50	3200	nM	EC50	J Med Chem (2003) 46: 1306-1317 [PMID:12672231]
ChEMBL	Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay	B	5.49	pEC50	3200	nM	EC50	J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
ChEMBL	Agonist activity at GAL4 fused human PPARalpha LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay	B	5.55	pEC50	2800	nM	EC50	Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL	Binding affinity for human peroxisome proliferator activated receptor gamma	B	7.05	pKi	90	nM	Ki	J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
GtoPdb	-	-	7.03	pIC50	-	-	-	J Med Chem (2003) 46: 1306-17 [PMID:12672231]; Br J Pharmacol (2003) 140: 527-37 [PMID:12970088]; Br J Pharmacol (2005) 144: 308-16 [PMID:15655531]
ChEMBL	Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand	B	7.04	pIC50	92	nM	IC50	J Med Chem (2003) 46: 1306-1317 [PMID:12672231]
ChEMBL	Agonistic activity for human Peroxisome proliferator activated receptor gamma	F	6.22	pEC50	600	nM	EC50	J Med Chem (2003) 46: 1306-1317 [PMID:12672231]
ChEMBL	Agonist activity at GAL4-fused PPARgamma assessed as transcriptional activity by cell based assay	F	6.22	pEC50	600	nM	EC50	Bioorg Med Chem Lett (2012) 22: 7075-7079 [PMID:23084275]
ChEMBL	Transactivation of Homo sapiens (human) PPARgamma assessed as luciferase activity by reporter gene assay	B	6.24	pEC50	575.44	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	6.24	pEC50	575.44	nM	EC50	Med Chem Res (2013) 22: 287-302
ChEMBL	In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)	B	6.24	pEC50	570	nM	EC50	Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434]
ChEMBL	Agonist activity at GAL4 fused human PPARgamma LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay	B	6.24	pEC50	570	nM	EC50	Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218]
ChEMBL	In vitro transactivation using receptor transactivation assay against hPPAR gamma	F	6.24	pEC50	570	nM	EC50	J Med Chem (2002) 45: 789-804 [PMID:11831892]
ChEMBL	Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay	B	6.24	pEC50	570	nM	EC50	J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
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	6.24	pEC50	570	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]