fenofibric acid [Ligand Id: 2662] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL981 (Fenocor-67, Fenofibrate free acid, Fenofibrate related compound b, Fenofibric acid, Fenogal, Fibricor, LF-153, Lipanthyl, Lipofen, Lofibra, NSC-281318, Procetofenic acid, Supralip, Trilipix)
  • fatty acid binding protein 2/Fatty acid binding protein intestinal in Human [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
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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]
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  • Urate anion exchanger 1/Solute carrier family 22 member 12 in Human [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
fatty acid binding protein 2/Fatty acid binding protein intestinal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP B 6 pKi 1000 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 42 deg C by fluorimetric assay B 4.54 pKd 29000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 37 deg C by fluorimetric assay B 4.55 pKd 28000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 30 deg C by fluorimetric assay B 4.57 pKd 27000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 25 deg C by fluorimetric assay B 4.62 pKd 24000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 20 deg C by fluorimetric assay B 4.64 pKd 23000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 15 deg C by fluorimetric assay B 4.7 pKd 20000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 10 deg C by fluorimetric assay B 4.72 pKd 19000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 5 deg C by fluorimetric assay B 4.74 pKd 18000 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 37 deg C by fluorimetric assay B 6.38 pKd 420 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 30 deg C by fluorimetric assay B 6.44 pKd 360 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 25 deg C by fluorimetric assay B 6.47 pKd 340 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 20 deg C by fluorimetric assay B 6.66 pKd 220 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 15 deg C by fluorimetric assay B 6.8 pKd 160 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 10 deg C by fluorimetric assay B 7 pKd 100 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 5 deg C by fluorimetric assay B 7.03 pKd 94 nM Kd J Med Chem (2009) 52: 5344-5355 [PMID:19663428]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 4.56 pKi 27500 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 6.48 pKi 334 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
GtoPdb - - 6.48 pKi 334 nM Ki J Med Chem (2008) 51: 3755-64 [PMID:18533710]
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 towards peroxisome proliferator activated receptor alpha (PPAR alpha) B 4.46 pKi 35000 nM Ki Bioorg Med Chem Lett (2003) 13: 3185-3190 [PMID:12951090]
ChEMBL Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha) B 4.17 pIC50 68000 nM IC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
ChEMBL Inhibition of human Peroxisome proliferator activated receptor alpha binding B 4.46 pIC50 35000 nM IC50 J Med Chem (2005) 48: 2262-2265 [PMID:15801817]
ChEMBL Inhibitory activity against human Peroxisome proliferator activated receptor alpha B 4.62 pIC50 24000 nM IC50 J Med Chem (2003) 46: 5121-5124 [PMID:14613314]
ChEMBL Mean inhibitory concentration against human peroxisome proliferator activated receptor alpha B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2005) 15: 51-55 [PMID:15582409]
ChEMBL Inhibition of human Peroxisome proliferator activated receptor alpha B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Displacement of tritium labeled ligand from human PPARalpha by SPA assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from hPPARalpha B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2006) 16: 6328-6333 [PMID:17005394]
ChEMBL Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay F 4 pEC50 >100000 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
ChEMBL Agonist activity at human PPARalpha by luciferase reporter transactivation assay F 4.16 pEC50 69000 nM EC50 Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176]
ChEMBL In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha) B 4.49 pEC50 32050 nM EC50 J Med Chem (2003) 46: 4883-4894 [PMID:14584939]
ChEMBL Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells F 4.52 pEC50 30000 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
ChEMBL Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay F 4.52 pEC50 30000 nM EC50 Bioorg Med Chem Lett (2008) 18: 2128-2132 [PMID:18280733]
ChEMBL Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay B 4.52 pEC50 30000 nM EC50 J Med Chem (2009) 52: 6382-6393 [PMID:19775169]
ChEMBL Agonist activity at PPARalpha (unknown origin) B 4.52 pEC50 30000 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL Effective concentration against human Peroxisome proliferator activated receptor alpha in Gal4 transactivation assay B 4.82 pEC50 15000 nM EC50 J Med Chem (2005) 48: 2262-2265 [PMID:15801817]
ChEMBL Cotransfection activity of compound against human Peroxisome proliferator activated receptor alpha was determined F 4.89 pEC50 13000 nM EC50 J Med Chem (2003) 46: 5121-5124 [PMID:14613314]
ChEMBL Partial agonist activity at human PPARalpha expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay F 4.92 pEC50 12000 nM EC50 Bioorg Med Chem Lett (2011) 21: 1978-1982 [PMID:21377875]
ChEMBL Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay B 4.92 pEC50 12000 nM EC50 Bioorg Med Chem Lett (2011) 21: 220-224 [PMID:21130649]
ChEMBL Displacement of tritium labeled ligand from human PPARalpha by SPA assay B 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay B 5 pEC50 >10000 nM EC50 J Med Chem (2007) 50: 1495-1503 [PMID:17343371]
ChEMBL Mean effective concentration against human peroxisome proliferator activated receptor alpha B 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2005) 15: 51-55 [PMID:15582409]
ChEMBL Effective concentration against human Peroxisome proliferator activated receptor alpha B 5 pEC50 >10000 nM EC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Agonist activity at human recombinant PPARalpha by transactivation of TK-MH100x4-LUC reporter gene in HEK293 cells F 5.04 pEC50 9200 nM EC50 Bioorg Med Chem Lett (2006) 16: 3213-3218 [PMID:16617018]
ChEMBL Binding affinity to histidine-tagged human PPARalpha-LBD assessed as recruitment of co-activator peptide fluorescein-labeled PGC1alpha after 2 hrs by TR-FRET assay B 5.35 pEC50 4500 nM EC50 Bioorg Med Chem Lett (2011) 21: 5876-5880 [PMID:21855333]
ChEMBL Activity at human PPARalpha in CV1 cells B 5.58 pEC50 2646 nM EC50 Bioorg Med Chem Lett (2006) 16: 6328-6333 [PMID:17005394]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells F 4.74 pEC50 18000 nM EC50 J Med Chem (1999) 42: 3785-3788 [PMID:10508427]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay F 4 pEC50 >100000 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
ChEMBL Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactivation assay F 4 pEC50 >100000 nM EC50 Bioorg Med Chem Lett (2008) 18: 2128-2132 [PMID:18280733]
ChEMBL Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay B 5 pEC50 >10000 nM EC50 J Med Chem (2007) 50: 1495-1503 [PMID:17343371]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Inhibition of human Peroxisome proliferator activated receptor gamma binding B 4.3 pIC50 >50000 nM IC50 J Med Chem (2005) 48: 2262-2265 [PMID:15801817]
ChEMBL Inhibition of human Peroxisome proliferator activated receptor gamma B 4.6 pIC50 >25000 nM IC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Mean inhibitory concentration against human peroxisome proliferator-activated receptor gamma B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2005) 15: 51-55 [PMID:15582409]
ChEMBL Displacement of tritium labeled ligand from human PPARgamma by SPA assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393]
ChEMBL Displacement of [3H]2-methyl-2-(4-{3-propyl-(5-pyridin-2yl-thiophene-2-sulfonyl)-amino]-pro-pyl}-phenoxy)-propionic acid from human PPARgamma B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2006) 16: 6328-6333 [PMID:17005394]
ChEMBL Effective concentration against human Peroxisome proliferator activated receptor gamma in Gal4 transactivation assay B 4 pEC50 >100000 nM EC50 J Med Chem (2005) 48: 2262-2265 [PMID:15801817]
ChEMBL Effective concentration against human Peroxisome proliferator activated receptor gamma B 4 pEC50 >100000 nM EC50 J Med Chem (2005) 48: 2248-2250 [PMID:15771468]
ChEMBL Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay F 4 pEC50 100000 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
ChEMBL Agonist activity at human PPARgamma expressed in monkey CV1 cells by transactivation assay F 4 pEC50 >100000 nM EC50 Bioorg Med Chem Lett (2008) 18: 2128-2132 [PMID:18280733]
Urate anion exchanger 1/Solute carrier family 22 member 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
ChEMBL Inhibition of URAT1 (unknown origin) B 4.96 pIC50 11000 nM IC50 Medchemcomm (2016) 7: 1587-1595

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]