Compound Detail
CHEMBL1623
MECLIZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1623 |
| Name | MECLIZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OCJYIGYOJCODJL-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
4
Known Names
5
Indications
Molecular Properties
391.0
MW (Da)
5.56
ALogP
2
HBA
0
HBD
6.5
PSA (Ų)
0.56
QED
1
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1957 |
| Availability | Prescription |
| Chirality | Racemic |
Indications
Hypersensitivity Vertigo Motion Sickness Smoking Cessation Carcinoma, Hepatocellular
ATC Classification
R06AE05
meclozine
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
R06AE55
meclozine, combinations
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
IC50 1 meas. best 5.7
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Serine protease hepsin CHEMBL2079849 | IC50 | 5.7 | 5.7 | 2020.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Serine protease hepsin | IC50 | = | 2020.0 | nM | 5.7 | High-Throughput Screening Assay: To identify novel inhibitors of hepsin, the Che... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 6 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 3 |
| 20014752 | 10.1021/tx900326k | Hepatotoxicity | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2A | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Cannabinoid receptor 1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Estrogen receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Adenosine receptor A3 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 2 |
| 22931300 | 10.1021/tx300075j | Liver microsomes | 2 |
| 22931300 | 10.1021/tx300075j | Cytochrome P450 3A4 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 2 |
Data from ChEMBL 36 via Core Engine