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ChEMBL ligand: CHEMBL672 (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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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acetylcholinesterase (Yt 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 |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293-A cells membrane vesicles assessed inhibition of ABCG2-mediated urate transport activity by rapid filtration technique | B | 5.29 | pIC50 | 5100 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
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 at PPARalpha (unknown origin) | B | 4.52 | pEC50 | 30000 | nM | EC50 | Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855] |
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 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]