Compound Detail
CHEMBL1764
LEVOMEPROMAZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1764 |
| Name | LEVOMEPROMAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | VRQVVMDWGGWHTJ-CQSZACIVSA-N |
| Therapeutic | ✓ Yes |
2
Targets
3
Activities
2
Assay Types
7
PK Parameters
20
Publications
18
Known Names
5
Indications
1
Mechanisms
Molecular Properties
328.5
MW (Da)
4.50
ALogP
4
HBA
0
HBD
15.7
PSA (Ų)
0.80
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1982 |
| Availability | Discontinued |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| D2-like dopamine receptor antagonist | ANTAGONIST | D2-like dopamine receptor | ✓ | ✓ |
Indications
Psychotic Disorders Anxiety Dementia Depressive Disorder Schizophrenia
ATC Classification
N05AA02
levomepromazine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Activity Summary
IC50 2 meas. best 5.02
EC50 1 meas. best 5.6
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Middle East respiratory syndrome-related coronavirus CHEMBL4296578 | EC50 | 5.6 | 5.6 | 2500.0 | 1 |
| Pleiotropic ABC efflux transporter of multiple drugs CHEMBL1697658 | IC50 | 5.02 | 5.02 | 9600.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 5.9 | mL.min-1.kg-1 | Homo sapiens |
| CL | 9.9 | mL.min-1.kg-1 | Homo sapiens |
| CL | 9.9 | mL.min-1.kg-1 | Homo sapiens |
| F | 79.0 | % | Homo sapiens |
| Fu | 0.034 | - | Homo sapiens |
| MRT | 21.0 | hr | Homo sapiens |
| T1/2 | 30.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Middle East respiratory syndrome-related coronavirus | EC50 | = | 2500.0 | nM | 5.6 | Antiviral activity against MERS-CoV/KOR/KNIH/002_05_2015 infected in human Huh-7... | 32283298 |
| Pleiotropic ABC efflux transporter of multiple drugs | IC50 | = | 9600.0 | nM | 5.02 | Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae ... | 19188399 |
Literature References
Data from ChEMBL 36 via Core Engine