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 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]