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Compound Detail

CHEMBL542541

HYDRALAZINE HYDROCHLORIDE
💊 Approved Drug
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💊 Approved Drug
Cl.NNc1nncc2ccccc12
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL542541
Name HYDRALAZINE HYDROCHLORIDE
Phase Approved
Structure Type MOL
InChI Key ZUXNZUWOTSUBMN-UHFFFAOYSA-N
Therapeutic ✓ Yes
Parent Compound CHEMBL276832
Active Moiety CHEMBL276832

Known Names

Apresoline Apressinum Dralzine Hydralazine hcl Hydralazine hydrochloride Hydralazine hydrochloride component of -hydrochlorothiazide-reserpine Hydralazine hydrochloride component of apresazide Hydralazine hydrochloride component of apresoline-esidrix Hydralazine hydrochloride component of bidil Hydralazine hydrochloride component of cam-ap-es Hydralazine hydrochloride component of dralserp Hydralazine hydrochloride component of hydra-zide +9 more
4
Targets
9
Activities
4
Assay Types
0
PK Parameters
20
Publications
21
Known Names
6
Indications
1
Mechanisms

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
USAN Stem -dralazine; -lazine

Extended Properties

Molecular Formula C8H9ClN4
MW 196.64
Aromatic Rings 2
Heavy Atoms 12
NP-Likeness -1.58

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Unknown - - ✓ ✓

Indications

Hypertension Alzheimer Disease Cerebral Hemorrhage Heart Failure Heart Failure Macular Degeneration

Activity Summary

Ki 6 meas. best 5.72
EC50 1 meas. best 6.35
IC50 1 meas. best 4.58
Kd 1 meas. best 4.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor subfamily 1 group I member 2
CHEMBL2146315
 EC50 6.35 6.35 450.0 1
Cholinesterase
CHEMBL5763
 Ki 5.72 5.51 1900.0 2
Acetylcholinesterase
CHEMBL4078
 Ki 5.16 5.16 7000.0 1
Aspartate aminotransferase, cytoplasmic
CHEMBL2189139
 Ki 4.83 4.765 14740.0 2
Aspartate aminotransferase, cytoplasmic
CHEMBL2189139
 Kd 4.78 4.78 16540.0 1
Aspartate aminotransferase, cytoplasmic
CHEMBL2189139
 IC50 4.58 4.58 26620.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nuclear receptor subfamily 1 group I member 2 EC50 = 450.0 nM 6.35 Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase ... 20966043
Cholinesterase Ki = 1900.0 nM 5.72 Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed... -
Cholinesterase Ki = 5011.87 nM 5.3 Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed... -
Acetylcholinesterase Ki = 7000.0 nM 5.16 Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE... -
Aspartate aminotransferase, cytoplasmic Ki = 14740.0 nM 4.83 Noncompetitive inhibition of GOT1 (unknown origin) using aspartic acid as substr... 35820623
Aspartate aminotransferase, cytoplasmic Kd = 16540.0 nM 4.78 Binding affinity to GOT1 (unknown origin) assessed as dissociation constant by m... 35820623
Aspartate aminotransferase, cytoplasmic Ki = 20200.0 nM 4.7 Noncompetitive inhibition of GOT1 (unknown origin) using alpha-Ketoglutaric acid... 35820623
Aspartate aminotransferase, cytoplasmic IC50 = 26620.0 nM 4.58 Inhibition of GOT1 (unknown origin) 35820623

Literature References

PubMed DOI Target Context # Activities
3585901 10.1021/jm00389a012 Rattus norvegicus 21
35820623 10.1016/j.bmcl.2022.128883 Aspartate aminotransferase, cytoplasmic 8
6471067 10.1021/jm00375a007 Rattus norvegicus 6
3585901 10.1021/jm00389a012 Cavia porcellus 5
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 5
3585901 10.1021/jm00389a012 Homo sapiens 4
- 10.1007/s00044-005-0140-0 Cholinesterase 3
- 10.1007/s00044-005-0140-0 Acetylcholinesterase 3
6113284 10.1021/jm00137a020 GABA-A receptor; anion channel 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
17417631 10.1038/nchembio873 Unchecked 1
6113284 10.1021/jm00137a020 Rattus norvegicus 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B1 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B3 1
3585901 10.1021/jm00389a012 Mus musculus 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
3585901 10.1021/jm00389a012 Unchecked 1
35820623 10.1016/j.bmcl.2022.128883 Malate dehydrogenase, cytoplasmic 1

Data from ChEMBL 36 via Core Engine