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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 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]