Compound Detail
CHEMBL1521
ZALEPLON 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1521 |
| Name | ZALEPLON |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | HUNXMJYCHXQEGX-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
4
Targets
6
Activities
3
Assay Types
23
PK Parameters
20
Publications
14
Known Names
6
Indications
1
Mechanisms
Molecular Properties
305.3
MW (Da)
2.64
ALogP
5
HBA
0
HBD
74.3
PSA (Ų)
0.75
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1999 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator | POSITIVE ALLOSTERIC MODULATOR | GABA A receptor alpha-1/beta-1/gamma-2 | ✓ | ✓ |
Indications
Sleep Initiation and Maintenance Disorders Anxiety Dementia Depressive Disorder Schizophrenia Sleep Wake Disorders
ATC Classification
N05CF03
zaleplon
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Drug Warnings
Black Box Warning
misuse
Black Box Warning
General Warning
Activity Summary
EC50 2 meas. best 6.54
IC50 2 meas. best 6.78
Ki 2 meas. best 6.47
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | IC50 | 6.78 | 6.58 | 167.0 | 2 |
| GABA-A receptor; alpha-1/beta-2/gamma-2 CHEMBL2095172 | EC50 | 6.54 | 6.54 | 290.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 6.47 | 6.47 | 336.0 | 1 |
| GABA-A receptor; alpha-2/beta-3/gamma-2 CHEMBL2094130 | EC50 | 5.79 | 5.79 | 1630.0 | 1 |
| Aldehyde oxidase CHEMBL3257 | Ki | 4.08 | 4.08 | 83000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 90.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 15.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 4.3 | mL.min-1.kg-1 | Homo sapiens |
| CL | 48.1 | mL.min-1.kg-1 | Mus musculus |
| CL | 2.3 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| F | 30.0 | % | Homo sapiens |
| F | 30.0 | % | Homo sapiens |
| Fu | 0.4 | - | Homo sapiens |
| Fu | 0.4 | - | Homo sapiens |
| Fu | 0.49 | - | Homo sapiens |
| Fu | 0.4 | - | Homo sapiens |
| MRT | 1.4 | hr | Homo sapiens |
| T1/2 | 1.1 | hr | Homo sapiens |
| T1/2 | 1.072 | hr | Homo sapiens |
| T1/2 | 0.7 | hr | Mus musculus |
| T1/2 | 1.1 | hr | Homo sapiens |
| T1/2 | 1.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | IC50 | = | 167.0 | nM | 6.78 | Inhibition of GABA receptor BZ domain (unknown origin) | 36439976 |
| GABA-A receptor; alpha-1/beta-2/gamma-2 | EC50 | = | 290.0 | nM | 6.54 | Modulation of human GABA-A alpha1beta2gamma2 expressed in xenopus oocytes assess... | 23121096 |
| Unchecked | Ki | = | 336.0 | nM | 6.47 | DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flun... | - |
| Unchecked | IC50 | = | 412.0 | nM | 6.38 | DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flun... | - |
| GABA-A receptor; alpha-2/beta-3/gamma-2 | EC50 | = | 1630.0 | nM | 5.79 | Modulation of human GABAA alpha2beta3gamma2 expressed in xenopus oocytes assesse... | 23121096 |
| Aldehyde oxidase | Ki | = | 83000.0 | nM | 4.08 | Inhibition of aldehyde oxidase in human liver cytosol assessed as production of ... | 22522748 |
Literature References
Data from ChEMBL 36 via Core Engine