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ChEMBL ligand: CHEMBL107367 (Farglitazar, G1-262570, Gi262570, GI-262570, GI-262570X, GI262570X) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]