Compound Detail
CHEMBL43064
CINNARIZINE 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL43064 |
| Name | CINNARIZINE |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | DERZBLKQOCDDDZ-JLHYYAGUSA-N |
| Therapeutic | ✓ Yes |
30
Targets
67
Activities
2
Assay Types
0
PK Parameters
20
Publications
30
Known Names
1
Indications
2
Mechanisms
Molecular Properties
368.5
MW (Da)
5.11
ALogP
2
HBA
0
HBD
6.5
PSA (Ų)
0.60
QED
1
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Voltage-gated L-type calcium channel blocker | BLOCKER | Voltage-gated L-type calcium channel | ✓ | ✓ |
| Histamine H1 receptor antagonist | ANTAGONIST | Histamine H1 receptor | ✓ | ✓ |
Indications
Vertigo
ATC Classification
N07CA02
cinnarizine
Level 1: NERVOUS SYSTEM
Level 2: OTHER NERVOUS SYSTEM DRUGS
N07CA52
cinnarizine, combinations
Level 1: NERVOUS SYSTEM
Level 2: OTHER NERVOUS SYSTEM DRUGS
Activity Summary
IC50 41 meas. best 7.4
Ki 26 meas. best 8.06
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL231 | Ki | 8.06 | 8.06 | 8.6 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 7.77 | 7.77 | 17.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 7.4 | 7.4 | 40.0 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.13 | 7.13 | 74.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 7.07 | 7.07 | 86.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.02 | 7.02 | 95.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 7.0 | 6.406 | 99.0 | 5 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 6.99 | 6.99 | 103.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 6.79 | 6.79 | 162.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.79 | 6.306 | 161.0 | 5 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 6.78 | 6.78 | 167.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 6.6 | 6.6 | 252.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | Ki | 6.59 | 6.59 | 259.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 6.44 | 6.44 | 360.0 | 1 |
| Sodium channel alpha subunits; brain (Types I, II, III) CHEMBL2096682 | IC50 | 6.36 | 6.36 | 440.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 6.35 | 6.35 | 444.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 6.33 | 6.33 | 465.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 6.3 | 6.3 | 502.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 6.29 | 6.29 | 510.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 6.26 | 6.26 | 545.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 6.24 | 6.24 | 573.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 6.24 | 6.24 | 579.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 6.22 | 6.22 | 605.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 6.21 | 6.21 | 619.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 6.19 | 6.19 | 652.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 6.14 | 6.14 | 731.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 6.12 | 6.12 | 759.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | IC50 | 6.12 | 6.12 | 762.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 6.11 | 6.11 | 777.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 6.11 | 6.11 | 776.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 6.04 | 6.04 | 906.0 | 1 |
| Mu-type opioid receptor CHEMBL233 | Ki | 6.04 | 6.04 | 922.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 5.99 | 5.99 | 1023.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 5.96 | 5.96 | 1083.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | IC50 | 5.96 | 5.96 | 1090.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 5.93 | 5.93 | 1167.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | Ki | 5.88 | 5.88 | 1304.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | IC50 | 5.79 | 5.79 | 1641.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 5.72 | 5.72 | 1919.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 5.65 | 5.65 | 2242.0 | 1 |
| Mu-type opioid receptor CHEMBL233 | IC50 | 5.64 | 5.64 | 2272.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 5.6 | 5.6 | 2513.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 5.55 | 5.55 | 2832.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 5.55 | 5.55 | 2808.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | IC50 | 5.44 | 5.44 | 3660.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 5.3 | 5.0833 | 5011.9 | 6 |
| A549 CHEMBL392 | IC50 | 5.01 | 5.01 | 9800.0 | 1 |
| LoVo CHEMBL614721 | IC50 | 4.98 | 4.98 | 10500.0 | 1 |
| MIA PaCa-2 CHEMBL614725 | IC50 | 4.96 | 4.96 | 11100.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 4.87 | 4.87 | 13500.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine