Compound Detail
CHEMBL32479
BROTIZOLAM 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL32479 |
| Name | BROTIZOLAM |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | UMSGKTJDUHERQW-UHFFFAOYSA-N |
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
10
Publications
9
Known Names
6
Indications
Molecular Properties
393.7
MW (Da)
4.40
ALogP
5
HBA
0
HBD
43.1
PSA (Ų)
0.61
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1984 |
| Availability | Unknown |
| Chirality | Achiral |
Indications
Anxiety Dementia Depressive Disorder Schizophrenia Sleep Initiation and Maintenance Disorders Sleep Wake Disorders
ATC Classification
N05CD09
brotizolam
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Activity Summary
IC50 2 meas. best 8.59
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | IC50 | 8.59 | 8.59 | 2.6 | 1 |
| Platelet-activating factor receptor CHEMBL250 | IC50 | 6.52 | 6.52 | 300.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 2.0 | mL.min-1.kg-1 | Homo sapiens |
| F | 79.0 | % | Homo sapiens |
| Fu | 0.092 | - | Homo sapiens |
| MRT | 6.0 | hr | Homo sapiens |
| T1/2 | 4.8 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | IC50 | = | 2.6 | nM | 8.59 | Displacement of [3H]flunitrazepam from Benzodiazepine receptor in Sprague-Dawley... | 32492595 |
| Platelet-activating factor receptor | IC50 | = | 300.0 | nM | 6.52 | In vitro for platelet activating factor receptor antagonist activity in a bindin... | 2016721 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 18426954 | 10.1124/dmd.108.020479 | ADMET | 4 |
| 20014752 | 10.1021/tx900326k | Hepatotoxicity | 3 |
| 10891117 | 10.1021/jm0000564 | No relevant target | 2 |
| 10891117 | 10.1021/jm0000564 | ADMET | 2 |
| 2016721 | 10.1021/jm00108a031 | Cavia porcellus | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 2016721 | 10.1021/jm00108a031 | Platelet-activating factor receptor | 1 |
| 18426954 | 10.1124/dmd.108.020479 | NON-PROTEIN TARGET | 1 |
| - | 10.1007/s00044-012-9977-1 | Whole blood | 1 |
| 32492595 | 10.1016/j.ejmech.2020.112405 | Unchecked | 1 |
Data from ChEMBL 36 via Core Engine