Compound Detail

CHEMBL672

FENOFIBRATE

💊 Approved Drug

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💊 Approved Drug

CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL672
Name	FENOFIBRATE
Phase	Approved
Structure Type	MOL
InChI Key	YMTINGFKWWXKFG-UHFFFAOYSA-N
Therapeutic	✓ Yes
Active Moiety	CHEMBL981

Known Names

Antara Antara (micronized) Fenofibrate Fenofibrate (micronized) Fenofibrate delayed release Fenofibrate micronized Fenofibrato Fenogal Fenoglide Lipantil Lipantil micro 200 Lipantil micro 267 +8 more

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

360.8

MW (Da)

4.68

ALogP

HBA

HBD

52.6

PSA (Å²)

0.55

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
First Approval	1993
Availability	Prescription
Chirality	Achiral

Routes of Administration

Oral

Flags

Natural Product Prodrug

USAN Stem

-fibrate

Extended Properties

Molecular Formula	C20H21ClO4
MW	360.84
Aromatic Rings	2
Heavy Atoms	25
NP-Likeness	-0.58

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Peroxisome proliferator-activated receptor alpha agonist	AGONIST	Peroxisome proliferator-activated receptor alpha	✓	✓

Indications

Cardiovascular Diseases Diabetes Mellitus Diabetes Mellitus, Type 2 Dyslipidemias Hypercholesterolemia Hypothyroidism Atherosclerosis Coronary Disease Diabetic Retinopathy Hyperlipidemia, Familial Combined Hyperlipidemias Hyperlipoproteinemia Type III Hyperlipoproteinemias Hypertension Hypertriglyceridemia Lipid Metabolism Disorders Lipodystrophy Liver Cirrhosis, Biliary Metabolic Diseases Alcoholism

ATC Classification

C10AB05

fenofibrate

Level 1: CARDIOVASCULAR SYSTEM

Level 2: LIPID MODIFYING AGENTS

Activity Summary

IC50 29 meas. best 6.0

EC50 21 meas. best 6.24

Kd 15 meas. best 7.75

Ki 12 meas. best 7.62

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Fatty acid-binding protein, liver CHEMBL5738	Kd	7.75	7.0667	18.0	15
Fatty acid-binding protein, liver CHEMBL5738	Ki	7.62	7.005	24.0	2
Peroxisome proliferator-activated receptor gamma CHEMBL235	EC50	6.24	5.315	570.0	2
5-hydroxytryptamine receptor 2A CHEMBL224	Ki	6.22	6.22	605.0	1
Peroxisome proliferator-activated receptor alpha CHEMBL239	IC50	6.0	6.0	1000.0	1
5-hydroxytryptamine receptor 2C CHEMBL225	Ki	5.91	5.91	1242.0	1
Peroxisome proliferator-activated receptor alpha CHEMBL239	EC50	5.7	4.6477	2000.0	13
5-hydroxytryptamine receptor 2A CHEMBL224	IC50	5.67	5.67	2118.0	1
5-hydroxytryptamine receptor 2C CHEMBL225	IC50	5.62	5.62	2371.0	1
Adenosine receptor A3 CHEMBL256	Ki	5.49	5.49	3222.0	1
Broad substrate specificity ATP-binding cassette transporter ABCG2 CHEMBL5393	IC50	5.29	5.29	5100.0	1
Adenosine receptor A3 CHEMBL256	IC50	5.24	5.24	5701.0	1
Sodium-dependent dopamine transporter CHEMBL238	Ki	5.16	5.16	6859.0	1
Plasmodium falciparum CHEMBL364	IC50	5.1	4.9429	7943.3	7
MIA PaCa-2 CHEMBL614725	IC50	5.08	5.08	8400.0	1
Sodium-dependent dopamine transporter CHEMBL238	IC50	5.06	5.06	8633.0	1
Unchecked CHEMBL612545	Ki	4.95	4.8233	11361.0	3
LoVo CHEMBL614721	IC50	4.88	4.88	13200.0	1
Bile salt export pump CHEMBL6020	IC50	4.82	4.6767	15300.0	3
Acetylcholinesterase CHEMBL220	IC50	4.81	4.81	15551.0	1
A549 CHEMBL392	IC50	4.8	4.8	15900.0	1
Unchecked CHEMBL612545	IC50	4.75	4.7367	17672.0	3
PC-3 CHEMBL390	IC50	4.75	4.75	18000.0	1
Peroxisome proliferator-activated receptor alpha CHEMBL2128	EC50	4.75	4.75	18000.0	1
Sodium-dependent noradrenaline transporter CHEMBL222	Ki	4.67	4.67	21231.0	1
Sodium-dependent noradrenaline transporter CHEMBL222	IC50	4.67	4.67	21408.0	1
D(3) dopamine receptor CHEMBL234	Ki	4.33	4.33	46709.0	1
Peroxisome proliferator-activated receptor alpha CHEMBL2129	EC50	4.31	4.31	49000.0	1
Cruzipain CHEMBL3563	IC50	4.21	4.21	61000.0	1
NON-PROTEIN TARGET CHEMBL3879801	IC50	4.13	4.13	74500.0	1
Beta-3 adrenergic receptor CHEMBL246	Ki	4.03	4.03	92959.0	1

Pharmacokinetic Data

Parameter	Value	Units	Species
AUC	2014208.88	ng.hr.mL-1	Rattus norvegicus
AUC	649512.0	ng.hr.mL-1	Mesocricetus auratus
AUC	42218.28	ng.hr.mL-1	Canis lupus familiaris
AUC	2020704.0	ng.hr.mL-1	Rattus norvegicus
AUC	128884.83	ng.hr.mL-1	Homo sapiens
CL	54.0	uL.min-1.(10^6cells)-1	Rattus norvegicus
Cmax	15000.0	nM	Canis lupus familiaris
Cmax	12139.0	nM	Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Fatty acid-binding protein, liver	Kd	=	18.0	nM	7.75	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Kd	=	23.0	nM	7.64	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Kd	=	24.0	nM	7.62	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Ki	=	24.0	nM	7.62	Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FAB...	18533710
Fatty acid-binding protein, liver	Kd	=	27.0	nM	7.57	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Kd	=	32.0	nM	7.5	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Kd	=	41.0	nM	7.39	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Kd	=	62.0	nM	7.21	Binding affinity to rat recombinant L-FABP high affinity site expressed in Esche...	19663428
Fatty acid-binding protein, liver	Kd	=	130.0	nM	6.89	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	150.0	nM	6.82	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	160.0	nM	6.8	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	200.0	nM	6.7	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	250.0	nM	6.6	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	270.0	nM	6.57	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	320.0	nM	6.5	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Kd	=	360.0	nM	6.44	Binding affinity to rat recombinant L-FABP low affinity site expressed in Escher...	19663428
Fatty acid-binding protein, liver	Ki	=	405.0	nM	6.39	Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FAB...	18533710
Peroxisome proliferator-activated receptor gamma	EC50	=	570.0	nM	6.24	In vitro activation of human peroxisome proliferator activated receptor gamma (P...	12482434
5-hydroxytryptamine receptor 2A	Ki	=	605.0	nM	6.22	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: ...	-
Peroxisome proliferator-activated receptor alpha	IC50	=	1000.0	nM	6.0	Inhibition of human PPARalpha receptor by scintillation proximity assay	19530681

Literature References

PubMed	DOI	Target Context	# Activities
-	10.6019/CHEMBL3885881	Rattus norvegicus	2119
-	10.6019/CHEMBL3885861	Rattus norvegicus	1391
-	10.5281/zenodo.13943903	ADMET	88
31158845	10.1038/s41586-019-1291-3	ADMET	51
22339404	10.1021/jm201697v	Rattus norvegicus	23
32791402	10.1016/j.ejmech.2020.112649	Unchecked	20
22524508	10.1021/jm201107g	Syrian golden hamster	18
19663428	10.1021/jm801349e	Fatty acid-binding protein, liver	18
30337230	10.1016/j.bmcl.2018.10.003	Mus musculus	15
22194678	10.1371/journal.pcbi.1002310	Hepatotoxicity	14
32791402	10.1016/j.ejmech.2020.112649	Mus musculus	14
15646539	10.1016/s0399-8320(04)95062-2	Unchecked	11
23707917	10.1016/j.ejmech.2013.04.020	Rattus norvegicus	10
33684440	10.1016/j.bmcl.2021.127898	Mus musculus	9
21515043	10.1016/j.bmcl.2011.03.057	Syrian golden hamster	9
20416984	10.1016/j.ejmech.2010.03.043	Rattus norvegicus	8
29153558	10.1016/j.ejmech.2017.10.034	Syrian golden hamster	8
15646539	10.1016/s0399-8320(04)95062-2	NON-PROTEIN TARGET	8
26707395	10.1016/j.bmcl.2015.12.037	Rattus norvegicus	8
37269672	10.1016/j.ejmech.2023.115510	Mus musculus	8

Data from ChEMBL 36 via Core Engine