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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]