Carbinoxamine

Summary

Carbinoxamine (CHEMBL864) is an approved small-molecule H1-receptor antagonist (ATC R06AA08); indicated across 1 condition including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AA08
• Indications: 1 condition
• Chemistry: 290.79 Da · C16H19ClN2O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL864
Name	Carbinoxamine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2564
ChEBI	CHEBI:3398
ATC	R06AA08
Molecular formula	C16H19ClN2O
Molecular weight	290.79
InChIKey	OJFSXZCBGQGRNV-UHFFFAOYSA-N

SMILES: CN(C)CCOC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2

IUPAC name: 2-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-N,N-dimethylethanamine

ChEBI definition: An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson’s disease.

Pharmacological roles (ChEBI): H1-receptor antagonist, anti-allergic agent, muscarinic antagonist, antiparkinson drug.

Also known as: Carbinoxamina, Carbinoxamine, Palgic, carbinoxamine, SID29217899, CARBINOXAMINE

Parent form; salt/anhydrous children: CHEMBL1200974, CHEMBL1519829

Patent coverage: 2,063 distinct patent families (7,805 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 7,789 (100%) of the total. 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: 10 (assay-derived). Sample: Prelamin-A/C, Alpha-2B adrenergic receptor, Voltage-gated L-type calcium channel, Muscarinic acetylcholine receptor M2, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Histamine H1 receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, Histamine H3 receptor.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
HRH1	6.96	AC50	110	nM	CHEMBL_ACT_25212873
P22002	5.97	Ki	1080	nM	CHEMBL_ACT_2359823
KCNH2	5.89	AC50	1300	nM	CHEMBL_ACT_25118369
SLC6A4	5.52	AC50	3000	nM	CHEMBL_ACT_25150681
HRH3	5.46	AC50	3500	nM	CHEMBL_ACT_25200871
SLC6A3	5.28	AC50	5200	nM	CHEMBL_ACT_25124303

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).