fenofibrate [Ligand Id: 7186] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL672 (Antara, Antara (micronized), Fenofibrate, Fenofibrate delayed release, Fenofibrate micronized, Fenofibrate (micronized), Fenogal, Fenoglide, Lipantil, Lipantil micro 200, Lipantil micro 267, Lipantil micro 67, Lipidil, Lipofen, NSC-281319, Supralip 160, Tricor, Tricor (micronized), Triglide)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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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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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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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]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230]
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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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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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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
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) B 4.81 pIC50 15551 nM IC50 DrugMatrix in vitro pharmacology data
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.49 pKi 3222 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.24 pIC50 5701 nM IC50 DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.03 pKi 92959 nM Ki DrugMatrix in vitro pharmacology data
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 B 4.21 pIC50 61000 nM IC50 J Med Chem (2010) 53: 4259-4265 [PMID:20426472]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 4.33 pKi 46709 nM Ki DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.16 pKi 6859 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.06 pIC50 8633 nM IC50 DrugMatrix in vitro pharmacology data
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 6.44 pKd 360 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 6.49 pKd 320 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 6.57 pKd 270 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 6.6 pKd 250 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 6.7 pKd 200 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 6.8 pKd 160 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 6.82 pKd 150 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 6.89 pKd 130 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 7.21 pKd 62 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 7.39 pKd 41 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 7.49 pKd 32 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 7.57 pKd 27 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 7.62 pKd 24 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 7.64 pKd 23 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 7.74 pKd 18 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 6.39 pKi 405 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 7.62 pKi 24 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
GtoPdb - - 7.62 pKi 24 nM Ki J Med Chem (2008) 51: 3755-64 [PMID:18533710]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.67 pKi 21231 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.67 pIC50 21408 nM IC50 DrugMatrix in vitro pharmacology data
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Inhibition of human PPARalpha receptor by scintillation proximity assay B 6 pIC50 1000 nM IC50 J Med Chem (2009) 52: 4443-4453 [PMID:19530681]
ChEMBL Transactivation of human GAL4-fused PPARalpha LBD expressed in human HepG2 cells after 24 hrs by renilla luciferase reporter gene assay B 4.3 pEC50 50000 nM EC50 Bioorg Med Chem Lett (2019) 29: 2124-2128 [PMID:31320147]
ChEMBL In vitro effective concentration for agonist activity on dog Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CHO-K1 cells F 4.3 pEC50 50000 nM EC50 J Med Chem (2003) 46: 3581-3599 [PMID:12904063]
ChEMBL In vitro effective concentration for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected KRP-297 cells F 4.39 pEC50 41000 nM EC50 J Med Chem (2003) 46: 3581-3599 [PMID:12904063]
ChEMBL Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay B 4.47 pEC50 33510 nM EC50 Bioorg Med Chem (2013) 21: 766-778 [PMID:23265844]
ChEMBL Agonist activity at human PPARalpha assessed as luciferase activity by transactivation assay F 4.47 pEC50 33500 nM EC50 J Med Chem (2009) 52: 6835-6850 [PMID:19807106]
GtoPdb In a cell based hPPAR-GAL4 transactivation assay. - 4.52 pEC50 30000 nM EC50 J Med Chem (2004) 47: 4118-27 [PMID:15293980]
ChEMBL Agonist activity for Human PPAR alpha receptor in transcriptional activation assay F 4.52 pEC50 30000 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay B 4.52 pEC50 30000 nM EC50 J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
ChEMBL Agonist activity at GAL4-fused PPARalpha LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation after 18 hrs by dual luciferase reporter gene assay B 4.52 pEC50 30000 nM EC50 Eur J Med Chem (2017) 138: 212-220 [PMID:28667876]
ChEMBL Agonist activity at PPARalpha (unknown origin) B 4.52 pEC50 30000 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL Agonist activity at PPARalpha F 4.7 pEC50 20000 nM EC50 J Med Chem (2008) 51: 6318-6333 [PMID:18826205]
ChEMBL In vitro activation of human peroxisome proliferator activated receptor alpha B 5.49 pEC50 3210 nM EC50 Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434]
ChEMBL Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay F 5.7 pEC50 2000 nM EC50 J Med Chem (2009) 52: 4443-4453 [PMID:19530681]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Agonist activity for murine PPAR alpha receptor in transcriptional activation assay F 4.74 pEC50 18000 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230]
ChEMBL In vitro effective concentration for agonist activity on rat Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CHO-K1 cells F 4.31 pEC50 49000 nM EC50 J Med Chem (2003) 46: 3581-3599 [PMID:12904063]
ChEMBL Agonist activity at rat PPARalpha in rat H4IIE cells assessed as gene induction F 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176]
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 PPARgamma receptor by scintillation proximity assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2009) 52: 4443-4453 [PMID:19530681]
ChEMBL Binding affinity at PPARgamma B 4.39 pEC50 41000 nM EC50 Bioorg Med Chem (2008) 16: 2489-2498 [PMID:18083521]
ChEMBL Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay F 5.3 pEC50 >5000 nM EC50 J Med Chem (2009) 52: 4443-4453 [PMID:19530681]
ChEMBL In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma) B 6.24 pEC50 570 nM EC50 Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.22 pKi 605 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.67 pIC50 2118 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.91 pKi 1242 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.63 pIC50 2371 nM IC50 DrugMatrix in vitro pharmacology data
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 4.12 pIC50 >75000 nM IC50 Medchemcomm (2016) 7: 1587-1595

ChEMBL data shown on this page come from version 32:

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]