Compound Detail
CHEMBL648
CYCLIZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL648 |
| Name | CYCLIZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | UVKZSORBKUEBAZ-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
17
Targets
38
Activities
3
Assay Types
0
PK Parameters
20
Publications
3
Known Names
1
Indications
Molecular Properties
266.4
MW (Da)
3.02
ALogP
2
HBA
0
HBD
6.5
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1982 |
| Availability | Discontinued |
| Chirality | Achiral |
Indications
Hypersensitivity
ATC Classification
R06AE03
cyclizine
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
R06AE53
cyclizine, combinations
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
IC50 19 meas. best 7.42
Ki 18 meas. best 8.35
EC50 1 meas. best 5.94
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL231 | Ki | 8.35 | 8.35 | 4.4 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.42 | 7.42 | 38.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 7.19 | 7.19 | 64.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 6.92 | 6.92 | 119.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 6.8 | 6.8 | 159.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 6.79 | 6.79 | 163.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 6.65 | 6.65 | 225.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 6.62 | 6.62 | 238.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 6.43 | 6.43 | 373.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | Ki | 6.38 | 6.38 | 412.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 6.34 | 6.34 | 455.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 6.27 | 6.27 | 535.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 6.24 | 6.24 | 582.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | Ki | 6.22 | 6.22 | 606.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 6.22 | 6.22 | 597.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 6.2 | 6.2 | 633.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 6.17 | 6.17 | 675.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | IC50 | 6.13 | 6.13 | 748.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | IC50 | 6.12 | 6.12 | 763.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | IC50 | 6.07 | 6.07 | 852.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 5.99 | 5.99 | 1021.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 5.99 | 5.99 | 1016.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | IC50 | 5.94 | 5.94 | 1158.0 | 1 |
| Hepatitis C virus CHEMBL379 | EC50 | 5.94 | 5.94 | 1140.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 5.92 | 5.92 | 1215.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 5.86 | 5.86 | 1379.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 5.81 | 5.81 | 1551.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 5.68 | 5.555 | 2088.0 | 4 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 5.6 | 5.6 | 2492.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 5.6 | 5.485 | 2518.0 | 4 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 5.52 | 5.52 | 2992.0 | 1 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 5.21 | 5.21 | 6217.5 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine