Compound Detail
CHEMBL646
TRIAZOLAM 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL646 |
| Name | TRIAZOLAM |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | JOFWLTCLBGQGBO-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
11
Targets
14
Activities
4
Assay Types
12
PK Parameters
20
Publications
7
Known Names
6
Indications
1
Mechanisms
Molecular Properties
343.2
MW (Da)
4.23
ALogP
4
HBA
0
HBD
43.1
PSA (Ų)
0.66
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1978 |
| Availability | Prescription |
| Chirality | Achiral |
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 Anxiety Dementia Depressive Disorder Schizophrenia Substance-Related Disorders
ATC Classification
N05CD05
triazolam
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Drug Warnings
Withdrawn
neurotoxicity
Psychiatric reaction and amnesia
Withdrawn
psychiatric toxicity
Psychiatric reaction and amnesia
Withdrawn
psychiatric toxicity
serious psychiatric adverse effects, including memory disturbances, anxiety, depression and agressivity
Withdrawn
psychiatric toxicity
serious psychiatric adverse effects, including memory disturbances, anxiety, depression and agressivity
Withdrawn
neurotoxicity
psychiatric adverse effects, particularly loss of memory and depression
Withdrawn
psychiatric toxicity
serious psychiatric adverse effects, including memory disturbances, anxiety, depression and agressivity
Withdrawn
psychiatric toxicity
psychiatric adverse effects, particularly loss of memory and depression
Withdrawn
General Warning
harmful
Withdrawn
psychiatric toxicity
serious psychiatric adverse effects, including memory disturbances, anxiety, depression and agressivity
Black Box Warning
General Warning
Activity Summary
Ki 6 meas. best 9.23
IC50 5 meas. best 8.81
Kd 2 meas. best 9.0
EC50 1 meas. best 7.66
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| GABA-A receptor; alpha-2/beta-3/gamma-2 CHEMBL2094130 | Ki | 9.23 | 9.23 | 0.6 | 1 |
| GABA-A receptor; anion channel CHEMBL1907607 | Ki | 9.1 | 7.39 | 0.8 | 2 |
| GABA-A receptor; alpha-1/beta-3/gamma-2 CHEMBL2094121 | Ki | 9.1 | 9.1 | 0.8 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 CHEMBL1962 | Kd | 9.0 | 9.0 | 1.0 | 1 |
| GABA-A receptor; alpha-3/beta-3/gamma-2 CHEMBL2094120 | Ki | 8.85 | 8.85 | 1.4 | 1 |
| GABA-A receptor; alpha-5/beta-3/gamma-2 CHEMBL2094122 | Ki | 8.81 | 8.81 | 1.5 | 1 |
| Unchecked CHEMBL612545 | IC50 | 8.81 | 8.81 | 1.5 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 CHEMBL5112 | Kd | 8.4 | 8.4 | 4.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 7.66 | 7.66 | 22.0 | 1 |
| Oryctolagus cuniculus CHEMBL374 | IC50 | 4.96 | 4.96 | 11100.0 | 2 |
| Platelet-activating factor receptor CHEMBL5136 | IC50 | 4.96 | 4.96 | 11100.0 | 1 |
| Cholecystokinin receptor type A CHEMBL2871 | IC50 | 4.41 | 4.41 | 39000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 3.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.9 | mL.min-1.kg-1 | Homo sapiens |
| CL | 3.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 3.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 150.0 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| F | 49.0 | % | Homo sapiens |
| F | 44.0 | % | Homo sapiens |
| Fu | 0.1 | - | Homo sapiens |
| Fu | 0.1 | - | Homo sapiens |
| Fu | 0.1 | - | Homo sapiens |
| MRT | 3.2 | hr | Homo sapiens |
| T1/2 | 2.7 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine