ChEMBL ligand: CHEMBL107367 (Farglitazar, G1-262570, Gi262570, GI-262570, GI-262570X, GI262570X)
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] Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] 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 to human Peroxisome proliferator activated receptor alpha using scintillation proximity assay	B	6.31	pKi	490	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854]
ChEMBL	Tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor alpha	B	6.31	pKi	489.78	nM	Ki	J Med Chem (1998) 41: 5037-5054 [PMID:9836621]
ChEMBL	The compound was tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor alpha	B	6.31	pKi	6.31	uM	Log Ki	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL	Displacement of fluorescein labeled ligand from PPARalpha receptor by fluorescence polarization assay	B	5.54	pIC50	2870	nM	IC50	Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL	Displacement of tritium labeled ligand from human PPARalpha by SPA assay	B	5.91	pIC50	1217	nM	IC50	Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL	Transactivation of Homo sapiens (human) PPARalpha assessed as luciferase activity by reporter gene assay	B	6.34	pEC50	457.09	nM	EC50	Med Chem Res (2012) 21: 2873-2884
ChEMBL	In vitro transactivation of Peroxisome proliferator activated receptor alpha.	F	6.34	pEC50	457.09	nM	EC50	J Med Chem (1998) 41: 5037-5054 [PMID:9836621]
ChEMBL	Compound was tested functionally in vitro for inducing 50% of the maximum alkaline phosphatase activity (Transactivation) against human Peroxisome proliferator activated receptor alpha using transfection assay in CV-1 cells	F	6.34	pEC50	457.09	nM	EC50	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL	Maximal reporter activity against human Peroxisome proliferator activated receptor alpha Gal4 chimeric in transiently transfected CV-1 cells by functional assay.	F	6.35	pEC50	450	nM	EC50	Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854]
ChEMBL	Agonist activity for Human PPAR alpha receptor in transcriptional activation assay	F	6.35	pEC50	450	nM	EC50	J Med Chem (2000) 43: 527-550 [PMID:10691680]
GtoPdb	-	-	6.35	pEC50	-	-	-	Pharmacology (2005) 73: 15-22 [PMID:15452359]; J Med Chem (2000) 43: 527-50 [PMID:10691680]
ChEMBL	Displacement of tritium labeled ligand from human PPARalpha by SPA assay	B	6.46	pEC50	345	nM	EC50	Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL	Agonist activity at PPARalpha receptor expressed in HEK293 cells by GAL4 transactivation assay	F	6.49	pEC50	321	nM	EC50	Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL	Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay	B	6.91	pEC50	122	nM	EC50	Eur J Med Chem (2017) 137: 310-326 [PMID:28609708]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL	Binding affinity to bind to human Peroxisome proliferator activated receptor delta using scintillation proximity assay	B	5.92	pKi	1200	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854]
ChEMBL	The compound was tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor delta	B	6.07	pKi	6.07	uM	Log Ki	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
GtoPdb	-	-	7.47	pKd	-	-	-	J Med Chem (1998) 41: 5020-36 [PMID:9836620]; Eur J Biochem (2004) 271: 386-97 [PMID:14717706]
ChEMBL	In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA)	B	8.94	pKi	1.15	nM	Ki	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL	Binding affinity against peroxisome proliferator activated receptor gamma (PPAR-gamma)	B	8.94	pKi	1.15	nM	Ki	J Med Chem (1998) 41: 5055-5069 [PMID:9836622]
ChEMBL	Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gamma	B	8.94	pKi	1.15	nM	Ki	J Med Chem (1998) 41: 5037-5054 [PMID:9836621]
ChEMBL	Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854]
ChEMBL	Displacement of fluorescein labeled ligand from PPARgamma receptor by fluorescence polarization assay	B	6.66	pIC50	217	nM	IC50	Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL	Displacement of tritium labeled ligand from human PPARgamma by SPA assay	B	7.6	pIC50	25	nM	IC50	Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL	Partial agonist activity at human PPARgamma LBD assessed as activation of Src-1 by HTRF assay	F	8.22	pEC50	6	nM	EC50	J Med Chem (2011) 54: 8541-8554 [PMID:22070604]
ChEMBL	Displacement of tritium labeled ligand from human PPARgamma by SPA assay	B	8.3	pEC50	5	nM	EC50	Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL	Partial agonist activity at human PPARgamma LBD assessed as activation of CBP1-453 by HTRF assay	F	8.3	pEC50	5	nM	EC50	J Med Chem (2011) 54: 8541-8554 [PMID:22070604]
ChEMBL	Partial agonist activity at human PPARgamma LBD assessed as activation of PGC1 by HTRF assay	F	8.4	pEC50	4	nM	EC50	J Med Chem (2011) 54: 8541-8554 [PMID:22070604]
ChEMBL	Partial agonist activity at human PPARgamma LBD assessed as activation of PBP by HTRF assay	F	8.52	pEC50	3	nM	EC50	J Med Chem (2011) 54: 8541-8554 [PMID:22070604]
ChEMBL	-log concentration required to induce 50% maximum lipogenic activity against Peroxisome proliferator activated receptor gamma	F	8.83	pEC50	1.48	nM	EC50	J Med Chem (1998) 41: 5055-5069 [PMID:9836622]
ChEMBL	Ability to promote differentiation of C3H10T1/2 stem cells to adipocytes using lipogenesis assay mediated through activation of Peroxisome proliferator activated receptor gamma	F	8.83	pEC50	1.48	nM	EC50	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL	Ability to promote differentiation of C3H10T1/2 stem cells to adipocytes using lipogenesis assay mediated through activation of Peroxisome proliferator activated receptor gamma	F	8.83	pEC50	1.48	nM	EC50	J Med Chem (1998) 41: 5037-5054 [PMID:9836621]
ChEMBL	Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay	B	8.85	pEC50	1.4	nM	EC50	Eur J Med Chem (2017) 137: 310-326 [PMID:28609708]
ChEMBL	Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay	F	9.22	pEC50	0.6	nM	EC50	Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606]
ChEMBL	Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.	F	9.47	pEC50	0.34	nM	EC50	Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854]
ChEMBL	Agonist activity for Human PPAR gamma receptor in transcriptional activation assay	F	9.47	pEC50	0.34	nM	EC50	J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL	Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells	F	9.47	pEC50	0.34	nM	EC50	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL	Transactivation of PPARgamma assessed as induction of alkaline phosphatase activity	B	9.47	pEC50	0.34	nM	EC50	Bioorg Med Chem Lett (2010) 20: 3344-3347 [PMID:20444603]
ChEMBL	in vitro agonist activity against peroxisome proliferator activated receptor-gamma (PPAR-gamma), using alkaline phosphatase activity transactivator assay	F	9.47	pEC50	0.34	nM	EC50	J Med Chem (1998) 41: 5055-5069 [PMID:9836622]
ChEMBL	Transactivation of Homo sapiens (human) PPARgamma assessed as luciferase activity by reporter gene assay	B	9.47	pEC50	0.34	nM	EC50	Med Chem Res (2012) 21: 2873-2884
ChEMBL	Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gamma	F	9.47	pEC50	0.34	nM	EC50	J Med Chem (1998) 41: 5037-5054 [PMID:9836621]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL	Compound was tested functionally in vitro for inducing 50% of the maximum alkaline phosphatase activity (Transactivation) against murine Peroxisome proliferator activated receptor gamma using transfection assay in CV-1 cells	F	9.45	pEC50	0.35	nM	EC50	J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL	Agonist activity for murine PPAR gamma receptor in transcriptional activation assay	F	9.46	pEC50	0.35	nM	EC50	J Med Chem (2000) 43: 527-550 [PMID:10691680]

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]