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Compound Detail

CHEMBL276832

HYDRALAZINE
💊 Approved Drug
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💊 Approved Drug
NNc1nncc2ccccc12
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL276832
Name HYDRALAZINE
Phase Approved
Structure Type MOL
InChI Key RPTUSVTUFVMDQK-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Hidralazina Hydralazine Hydralazine polistirex NSC-126699
7
Targets
12
Activities
2
Assay Types
7
PK Parameters
20
Publications
4
Known Names
20
Indications

Molecular Properties

160.2
MW (Da)
0.92
ALogP
4
HBA
2
HBD
63.8
PSA (Ų)
0.48
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1953
Availability Prescription
Chirality Achiral

Routes of Administration

Oral Parenteral

Flags

Natural Product
USAN Stem -dralazine; -lazine

Extended Properties

Molecular Formula C8H8N4
MW 160.18
Aromatic Rings 2
Heavy Atoms 12
NP-Likeness -1.58

Indications

Hypertension Atherosclerosis Coronary Disease Diabetes Mellitus, Type 2 Hypercholesterolemia Ovarian Neoplasms Uterine Cervical Neoplasms Breast Neoplasms Cardiovascular Diseases Cerebral Hemorrhage Heart Diseases Heart Failure Heart Failure Neoplasms Pre-Eclampsia Stroke Vascular Diseases Lung Neoplasms Rectal Neoplasms Polycystic Kidney Diseases

ATC Classification

C02DB02
hydralazine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: ANTIHYPERTENSIVES

Activity Summary

IC50 10 meas. best 6.38
EC50 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisomal acyl-coenzyme A oxidase 1
CHEMBL4105748
 IC50 6.38 6.38 420.0 1
Myeloperoxidase
CHEMBL2439
 IC50 6.05 5.945 900.0 4
Lactoperoxidase
CHEMBL2295561
 IC50 5.92 5.92 1200.0 1
Polyunsaturated fatty acid lipoxygenase ALOX15
CHEMBL4358
 IC50 5.44 5.44 3649.0 1
Aldehyde oxidase
CHEMBL3257
 IC50 5.41 5.41 3930.0 1
Unchecked
CHEMBL612545
 IC50 5.09 5.09 8150.0 1
Aspartate aminotransferase, cytoplasmic
CHEMBL2189139
 IC50 4.58 4.58 26620.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 85.0 mL.min-1.kg-1 Homo sapiens
CL 85.0 mL.min-1.kg-1 Homo sapiens
Cmax 2500.0 nM Homo sapiens
F 20.0 % Homo sapiens
Fu 0.12 - Homo sapiens
MRT 0.29 hr Homo sapiens
T1/2 0.96 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Peroxisomal acyl-coenzyme A oxidase 1 IC50 = 420.0 nM 6.38 Inhibition of human recombinant AOX in presence of NAD+ and NADPH 37197460
Myeloperoxidase IC50 = 900.0 nM 6.05 Irreversible inhibition of MPO (unknown origin) 28197313
Myeloperoxidase IC50 = 900.0 nM 6.05 Inhibition of human MPO 28197313
Myeloperoxidase IC50 = 900.0 nM 6.05 Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine ... 28671460
Lactoperoxidase IC50 = 1200.0 nM 5.92 Inhibition of bovine milk LPO assessed as reduction in NaOSCN production in pres... 28671460
Myeloperoxidase IC50 = 2360.0 nM 5.63 Inhibition of recombinant MPO (unknown origin) assessed as reduction in LDL oxid... 28671460
Polyunsaturated fatty acid lipoxygenase ALOX15 IC50 = 3649.0 nM 5.44 DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) -
Aldehyde oxidase IC50 = 3930.0 nM 5.41 Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-ni... -
Unchecked IC50 = 8150.0 nM 5.09 Inhibition of aldehyde oxidase in Sprague-Dawley rat liver cytosolic fraction us... -
Aspartate aminotransferase, cytoplasmic IC50 = 26620.0 nM 4.58 Inhibition of GOT1 (unknown origin) using aspartic acid and alpha-ketoglutaric a... 35820623

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885881 Rattus norvegicus 405
458822 10.1021/jm00192a012 Rattus norvegicus 24
691003 10.1021/jm00206a011 Canis familiaris 20
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
7452697 10.1021/jm00186a024 Rattus norvegicus 14
6747991 10.1021/jm00374a024 Canis familiaris 14
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
7265125 10.1021/jm00136a006 Rattus norvegicus 11
6125596 10.1021/jm00349a010 Rattus norvegicus 10
3361579 10.1021/jm00400a004 Rattus norvegicus 10
3361578 10.1021/jm00400a003 Rattus norvegicus 10
28671460 10.1021/acs.jmedchem.7b00285 Myeloperoxidase 9
6827558 10.1021/jm00357a015 Rattus norvegicus 8
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
28197313 10.1021/acsmedchemlett.6b00417 Myeloperoxidase 6
19628 10.1021/jm00218a007 Rattus norvegicus 6
42797 10.1021/jm00197a002 Rattus norvegicus 6
7310823 10.1021/jm00144a017 Rattus norvegicus 6
691003 10.1021/jm00206a011 Rattus norvegicus 5
37337 10.1021/jm00192a015 Canis familiaris 5

Data from ChEMBL 36 via Core Engine