farglitazar [Ligand Id: 2672] activity data from GtoPdb and ChEMBL

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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]
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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]
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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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 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]