Compound Detail
CHEMBL13209
NITRAZEPAM 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL13209 |
| Name | NITRAZEPAM |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | KJONHKAYOJNZEC-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
5
Activities
2
Assay Types
10
PK Parameters
20
Publications
16
Known Names
6
Indications
Molecular Properties
281.3
MW (Da)
2.38
ALogP
4
HBA
1
HBD
84.6
PSA (Ų)
0.68
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Indications
Anxiety Dementia Depressive Disorder Schizophrenia Sleep Wake Disorders Epilepsy
ATC Classification
N05CD02
nitrazepam
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Activity Summary
IC50 4 meas. best 7.42
Ki 1 meas. best 7.35
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| GABA-A receptor; anion channel CHEMBL2094107 | IC50 | 7.42 | 7.42 | 38.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 7.35 | 7.35 | 44.6 | 1 |
| Unchecked CHEMBL612545 | IC50 | 7.26 | 7.26 | 54.7 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 0.86 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.86 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.9 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.86 | mL.min-1.kg-1 | Homo sapiens |
| F | 79.0 | % | Homo sapiens |
| F | 78.0 | % | Homo sapiens |
| Fu | 0.13 | - | Homo sapiens |
| Fu | 0.13 | - | Homo sapiens |
| MRT | 33.0 | hr | Homo sapiens |
| T1/2 | 26.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| GABA-A receptor; anion channel | IC50 | = | 38.0 | nM | 7.42 | Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine recepto... | 2984422 |
| Unchecked | Ki | = | 44.6 | nM | 7.35 | DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flun... | - |
| Unchecked | IC50 | = | 54.7 | nM | 7.26 | DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flun... | - |
Literature References
Data from ChEMBL 36 via Core Engine