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Compound Detail

CHEMBL264374

BEZAFIBRATE
🧪 Phase III
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🧪 Phase III
CC(C)(Oc1ccc(CCNC(=O)c2ccc(Cl)cc2)cc1)C(=O)O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL264374
Name BEZAFIBRATE
Phase Phase III
Structure Type MOL
InChI Key IIBYAHWJQTYFKB-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Bezafibrate Bezafibrato Bezagen xl Bezalip Bezalip-mono Bezatol sr BM 15.075 BM-15.075 BM-15075 Fibrazate xl Liparol xl NSC-758174 +1 more
9
Targets
50
Activities
3
Assay Types
2
PK Parameters
20
Publications
13
Known Names
8
Indications
1
Mechanisms

Molecular Properties

361.8
MW (Da)
3.55
ALogP
3
HBA
2
HBD
75.6
PSA (Ų)
0.79
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product
USAN Stem -fibrate
USAN Year 1978

Extended Properties

Molecular Formula C19H20ClNO4
MW 361.83
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.78

Mechanism of Action

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

Indications

Cardiovascular Diseases Cholangitis, Sclerosing Hyperlipidemia, Familial Combined Liver Cirrhosis, Biliary Bipolar Disorder Diabetes Mellitus, Type 2 Mitochondrial Diseases Myelodysplastic Syndromes

ATC Classification

C10AB02
bezafibrate
Level 1: CARDIOVASCULAR SYSTEM
Level 2: LIPID MODIFYING AGENTS

Activity Summary

EC50 44 meas. best 8.22
IC50 4 meas. best 4.0
Ki 2 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
 EC50 8.22 7.1 6.0 2
Peroxisome proliferator-activated receptor
CHEMBL3559683
 EC50 5.98 5.98 1040.0 1
Peroxisome proliferator-activated receptor gamma
CHEMBL235
 EC50 5.52 4.4064 3000.0 11
Peroxisome proliferator-activated receptor alpha
CHEMBL239
 EC50 5.15 4.4446 7100.0 13
Peroxisome proliferator-activated receptor delta
CHEMBL3979
 EC50 4.72 4.5722 18900.0 9
Fatty acid-binding protein, intestinal
CHEMBL4879
 Ki 4.48 4.48 33000.0 1
Fatty acid-binding protein, liver
CHEMBL5738
 Ki 4.35 4.35 44400.0 1
Peroxisome proliferator-activated receptor gamma
CHEMBL2459
 EC50 4.26 4.26 55000.0 2
Peroxisome proliferator-activated receptor alpha
CHEMBL2128
 EC50 4.05 4.05 90000.0 2
Unchecked
CHEMBL612545
 IC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5.5 ng/g.hr Mus musculus
AUC 420.7 ng/g.hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 6.0 nM 8.22 Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incu... 33771587
Unchecked EC50 = 1050.0 nM 5.98 Transactivation of PPAR expressed in HepG2 cells after 20 hrs by luminescence as... 22381047
Peroxisome proliferator-activated receptor EC50 = 1040.0 nM 5.98 Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by lucifer... 23031596
Peroxisome proliferator-activated receptor gamma EC50 = 3000.0 nM 5.52 Agonist activity at human PPARgamma expressed in CV1 cells by transactivation as... 17964792
Peroxisome proliferator-activated receptor alpha EC50 = 7100.0 nM 5.15 Agonist activity at Gal4-tagged human PPARalpha ligand binding domain expressed ... -
Peroxisome proliferator-activated receptor gamma EC50 = 13200.0 nM 4.88 Agonist activity at human PPARgamma transfected in African green monkey COS-7 ce... 38522113
Peroxisome proliferator-activated receptor gamma EC50 = 15400.0 nM 4.81 Agonist activity at Gal4-tagged human PPARgamma ligand binding domain expressed ... -
Peroxisome proliferator-activated receptor delta EC50 = 18900.0 nM 4.72 Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with... 21215640
Peroxisome proliferator-activated receptor delta EC50 = 20000.0 nM 4.7 Compound was tested for agonist activity on human Peroxisome proliferator activa... 10508427
Peroxisome proliferator-activated receptor delta EC50 = 20000.0 nM 4.7 Agonist activity for Human PPAR delta receptor in transcriptional activation ass... 10691680
Peroxisome proliferator-activated receptor delta EC50 = 22600.0 nM 4.65 Agonist activity at Gal4-tagged human PPARdelta ligand binding domain expressed ... -
Peroxisome proliferator-activated receptor delta EC50 = 25900.0 nM 4.59 Agonist activity at human PPAR delta by luciferase reporter gene assay 38460271
Peroxisome proliferator-activated receptor delta EC50 = 30000.0 nM 4.52 Agonist activity at human PPARdelta expressed in CV1 cells by transactivation as... 17964792
Peroxisome proliferator-activated receptor alpha EC50 = 30000.0 nM 4.52 Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactiva... 18280733
Peroxisome proliferator-activated receptor delta EC50 = 30000.0 nM 4.52 Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactiva... 18280733
Peroxisome proliferator-activated receptor alpha EC50 = 30000.0 nM 4.52 Agonist activity at human PPARalpha expressed in CV1 cells by transactivation as... 17964792
Peroxisome proliferator-activated receptor alpha EC50 = 31700.0 nM 4.5 Agonist activity at GAL4-tagged PPARalpha-LBD (unknown origin) expressed in HEK2... 33142057
Fatty acid-binding protein, intestinal Ki = 33000.0 nM 4.48 Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP 18533710
Peroxisome proliferator-activated receptor alpha EC50 = 34300.0 nM 4.46 Agonist activity at human PPARalpha transfected in African green monkey COS-7 ce... 38522113
Peroxisome proliferator-activated receptor delta EC50 = 35740.0 nM 4.45 Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with... 23265844

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885881 Rattus norvegicus 1184
31158845 10.1038/s41586-019-1291-3 ADMET 103
- 10.5281/zenodo.13943903 ADMET 89
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
1995897 10.1021/jm00106a041 Hemoglobin HbA 8
6747995 10.1021/jm00374a006 ADMET 6
6094807 10.1021/jm00378a005 Unchecked 6
34547896 10.1021/acs.jmedchem.1c00823 Transthyretin 4
2795607 10.1021/jm00130a021 Hemoglobin HbA 4
2795607 10.1021/jm00130a021 Homo sapiens 4
12904063 10.1021/jm0205144 Rattus norvegicus 4
11831892 10.1021/jm010964g Rattus norvegicus 4
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 3
32787092 10.1021/acs.jmedchem.0c00868 ADMET 3
23265844 10.1016/j.bmc.2012.11.040 Peroxisome proliferator-activated receptor delta 3
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 3
20014752 10.1021/tx900326k Hepatotoxicity 3
10508427 10.1021/jm9903601 Peroxisome proliferator-activated receptor delta 2

Data from ChEMBL 36 via Core Engine