Buclizine

Summary

Buclizine (CHEMBL1201271) is an approved small-molecule cholinergic antagonist (ATC R06AE51); indicated across 1 condition including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AE51 (+1 more)
• Indications: 1 condition
• Chemistry: 433 Da · C28H33ClN2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201271
Name	Buclizine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	6729
ChEBI	CHEBI:3205
ATC	R06AE51, R06AE01
Molecular formula	C28H33ClN2
Molecular weight	433
InChIKey	MOYGZHXDRJNJEP-UHFFFAOYSA-N

SMILES: CC(C)(C)C1=CC=C(C=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl

IUPAC name: 1-[(4-tert-butylphenyl)methyl]-4-[(4-chlorophenyl)-phenylmethyl]piperazine

ChEBI definition: An N-alkylpiperazine carrying (4-chlorophenyl)(phenyl)methyl and 4-tert-butylbenzyl groups.

Pharmacological roles (ChEBI): antiemetic, cholinergic antagonist, histamine antagonist, local anaesthetic, central nervous system depressant.

Also known as: Buclizina, Buclizine, BUCLIZINE, buclizine

Parent form; salt/anhydrous children: CHEMBL1200403, CHEMBL2360580

Patent coverage: 1,400 distinct patent families (5,799 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

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Cannabinoid receptor 1, Histamine H1 receptor, Kappa-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D, Nuclear receptor subfamily 1 group I member 2, Growth hormone secretagogue receptor type 1.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KCNH2	5.92	AC50	1200	nM	CHEMBL_ACT_25118264
CNR1	5.75	AC50	1800	nM	CHEMBL_ACT_25181790
HRH1	5.68	AC50	2100	nM	CHEMBL_ACT_25212795
OPRK1	5.1	AC50	7900	nM	CHEMBL_ACT_25129686

Target pathways

No target-pathway data for this drug (no mapped target genes).

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: 0.

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).