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

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ChEMBL ligand: CHEMBL981 (Supralip, LF-153, Fenocor-67, Fenofibric acid, NSC-281318, Lipanthyl, Fibricor, Fenofibrate related compound b, Fenogal, Fenofibrate free acid, Lipofen, Trilipix, Lofibra)
  • 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]