Cyclizine
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Also known as CiclizinaNSC-26608SID11112316SID26747952SID124882239
Summary
Cyclizine (CHEMBL648) is an approved small-molecule cholinergic antagonist (ATC R06AE53) targeting HRH1; indicated across 1 condition including allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AE53 (+1 more)
- Targets: 1 (HRH1)
- Indications: 1 condition
- Clinical trials: 1
- Chemistry: 266.4 Da · C18H22N2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL648 |
| Name | Cyclizine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 6726 |
| ChEBI | CHEBI:3994 |
| ATC | R06AE53, R06AE03 |
| Molecular formula | C18H22N2 |
| Molecular weight | 266.4 |
| InChIKey | UVKZSORBKUEBAZ-UHFFFAOYSA-N |
SMILES: CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3
IUPAC name: 1-benzhydryl-4-methylpiperazine
ChEBI definition: An N-alkylpiperazine in which one nitrogen of the piperazine ring is substituted by a methyl group, while the other is substituted by a diphenylmethyl group.
Pharmacological roles (ChEBI): antiemetic, cholinergic antagonist, central nervous system depressant, local anaesthetic, H1-receptor antagonist.
Also known as: Ciclizina, Cyclizine, NSC-26608, SID11112316, SID26747952, cyclizine, SID124882239, CYCLIZINE
Parent form; salt/anhydrous children: CHEMBL1200497, CHEMBL1324714, CHEMBL3189137
Patent coverage: 3,306 distinct patent families (13,632 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| HRH1 | H1 receptor | Antagonist | 8.35 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 20 (assay-derived). Sample: Nuclear receptor ROR-gamma, Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Muscarinic acetylcholine receptor M5, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Alpha-1D adrenergic receptor, 5-hydroxytryptamine receptor 2A.
Bioactivity
ChEMBL activities: 38 potent at pChembl ≥ 5 of 41 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 8.35 | Ki | 4.44 | nM | CHEMBL_ACT_7693455 |
| HRH1 | 7.42 | IC50 | 38 | nM | CHEMBL_ACT_7693454 |
| HTR2A | 7.19 | Ki | 64 | nM | CHEMBL_ACT_7693565 |
| CHRM4 | 6.92 | Ki | 119 | nM | CHEMBL_ACT_7693489 |
| CHRM3 | 6.8 | Ki | 159 | nM | CHEMBL_ACT_7693487 |
| CHRM1 | 6.79 | Ki | 163 | nM | CHEMBL_ACT_7693483 |
| HTR2A | 6.65 | IC50 | 225 | nM | CHEMBL_ACT_7693564 |
| HTR2B | 6.62 | Ki | 238 | nM | CHEMBL_ACT_7693567 |
| CHRM2 | 6.48 | AC50 | 334.2 | nM | CHEMBL_ACT_25196089 |
| HTR2B | 6.43 | IC50 | 373 | nM | CHEMBL_ACT_7693566 |
| CHRM2 | 6.38 | Ki | 412 | nM | CHEMBL_ACT_7693485 |
| CHRM5 | 6.34 | Ki | 455 | nM | CHEMBL_ACT_7693491 |
| HTR2C | 6.27 | Ki | 535 | nM | CHEMBL_ACT_7693569 |
| ADRA2A | 6.24 | Ki | 582 | nM | CHEMBL_ACT_7691339 |
| ADRA1D | 6.22 | Ki | 597 | nM | CHEMBL_ACT_7691337 |
| SLC6A3 | 6.22 | Ki | 606 | nM | CHEMBL_ACT_7691415 |
| CHRM5 | 6.2 | IC50 | 633 | nM | CHEMBL_ACT_7693490 |
| CHRM1 | 6.17 | IC50 | 675 | nM | CHEMBL_ACT_7693482 |
| CHRM3 | 6.13 | IC50 | 748 | nM | CHEMBL_ACT_7693486 |
| SLC6A3 | 6.12 | IC50 | 763 | nM | CHEMBL_ACT_7691414 |
| CHRM4 | 6.07 | IC50 | 852 | nM | CHEMBL_ACT_7693488 |
| DRD3 | 5.99 | Ki | 1016 | nM | CHEMBL_ACT_7691411 |
| HTR2C | 5.99 | IC50 | 1021 | nM | CHEMBL_ACT_7693568 |
| CHRM2 | 5.94 | IC50 | 1158 | nM | CHEMBL_ACT_7693484 |
| ADRA1D | 5.92 | IC50 | 1215 | nM | CHEMBL_ACT_7691336 |
| P15823 | 5.86 | Ki | 1379 | nM | CHEMBL_ACT_7691335 |
| ADRA2A | 5.81 | IC50 | 1551 | nM | CHEMBL_ACT_7691338 |
| SLC6A3 | 5.7 | AC50 | 1982 | nM | CHEMBL_ACT_25125312 |
| DRD3 | 5.66 | AC50 | 2209 | nM | CHEMBL_ACT_25194865 |
| CHRM1 | 5.62 | AC50 | 2408 | nM | CHEMBL_ACT_25210513 |
Target pathways
Aggregated over 1 target gene(s): HRH1.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Histamine receptors | 1 | HRH1 |
| G alpha (q) signalling events | 1 | HRH1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| inflammatory response | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| chemical synaptic transmission | 1 |
| memory | 1 |
| visual learning | 1 |
| regulation of vascular permeability | 1 |
| positive regulation of vasoconstriction | 1 |
| regulation of synaptic plasticity | 1 |
| cellular response to histamine | 1 |
| signal transduction | 1 |
| phospholipase C-activating serotonin receptor signaling pathway | 1 |
Indications & clinical
Indications
1 indication (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
Clinical trials
Total trials: 1.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06789614 | Not specified | NOT_YET_RECRUITING | Comparison of the Effect of Cyclizine Versus Metoclopramide on Gastric Residual Volume in Patients Undergoing Bariatric Surgery: A Randomized Double-blinded Clinical Trial |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
295 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACLIDINIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | HRH1 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ACRIVASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMISULPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMSACRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ANTAZOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ATOMOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZATADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | HRH1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | HRH1 |
| BETAMETHASONE PHOSPHORIC ACID | ChEMBL | Phase 4 (approved) | HRH1 |
| BIPERIDEN | ChEMBL | Phase 4 (approved) | HRH1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUPROPION | ChEMBL | Phase 4 (approved) | HRH1 |
| BUSPIRONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUTRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CAPTOPRIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CARBINOXAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORDIAZEPOXIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENTERMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | HRH1 |
| CINACALCET | ChEMBL | Phase 4 (approved) | HRH1 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOFAZIMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DESIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DEXBROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1
- Diseases: allergic disease
- Drugs: Aclidinium Bromide, Desloratadine, Dihydroergotamine, Paliperidone, Pramipexole, Abemaciclib, Acetophenazine, Acrivastine, Amiodarone, Amisulpride, Amitriptyline, Amoxapine, Amsacrine, Antazoline, Apomorphine, Aripiprazole, Asenapine, Astemizole, Atomoxetine, Azatadine, Azelastine, Benfluorex, Benperidol, Benzbromarone, Benztropine, Bepridil, Betamethasone Phosphoric Acid, Biperiden, Brexpiprazole, Bromperidol, Brompheniramine, Buclizine, Bupropion, Buspirone, Butriptyline, Cabergoline, Candesartan Cilexetil, Captopril, Carbinoxamine, Cariprazine, Cetirizine, Chlordiazepoxide, Chlorpheniramine, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clotrimazole, Clozapine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine, Dexbrompheniramine