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Compound Detail

CHEMBL285674

ESTAZOLAM
💊 Approved Drug
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💊 Approved Drug
Clc1ccc2c(c1)C(c1ccccc1)=NCc1nncn1-2
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL285674
Name ESTAZOLAM
Phase Approved
Structure Type MOL
InChI Key CDCHDCWJMGXXRH-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

ABBOTT-47631 Estazolam Estazolam civ Eurodin NSC-290818 Prosom
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
20
Publications
6
Known Names
2
Indications
1
Mechanisms

Molecular Properties

294.8
MW (Da)
3.27
ALogP
4
HBA
0
HBD
43.1
PSA (Ų)
0.69
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1990
Availability Prescription
Chirality Achiral

Routes of Administration

Oral

Flags

Black Box Warning Natural Product
USAN Year 1990

Extended Properties

Molecular Formula C16H11ClN4
MW 294.75
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.04

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
GABA-A receptor; anion channel positive allosteric modulator POSITIVE ALLOSTERIC MODULATOR GABA-A receptor; anion channel ✓ ✓

Indications

Sleep Initiation and Maintenance Disorders Sleep Wake Disorders

ATC Classification

N05CD04
estazolam
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS

Drug Warnings

Black Box Warning
General Warning
Country: United States

Activity Summary

IC50 1 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
 IC50 7.33 7.33 46.6 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 10.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 46.6 nM 7.33 Displacement of [3H]flunitrazepam from GABAA benzodiazepine receptor in rat brai... 18829330

Literature References

PubMed DOI Target Context # Activities
16472241 10.2174/1570163043334794 Hepatotoxicity 18
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
7154007 10.1021/jm00354a015 Mus musculus 6
33450619 10.1016/j.ejmech.2020.113142 Mus musculus 4
20014752 10.1021/tx900326k Hepatotoxicity 3
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 3
592339 10.1021/jm00222a035 Mus musculus 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
26948801 10.1016/j.drudis.2016.02.015 Homo sapiens 2
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 2
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 2
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 2
22137933 10.1016/j.bmc.2011.10.080 Bromodomain-containing protein 4 2
22137933 10.1016/j.bmc.2011.10.080 Bromodomain-containing protein 3 2
22137933 10.1016/j.bmc.2011.10.080 Bromodomain-containing protein 2 2
22137933 10.1016/j.bmc.2011.10.080 Protein polybromo-1 1
22137933 10.1016/j.bmc.2011.10.080 Unchecked 1

Data from ChEMBL 36 via Core Engine