Azatadine

Summary

Azatadine (CHEMBL946) is an approved small-molecule H1-receptor antagonist (ATC R06AX09); indicated across 1 condition including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AX09
• Indications: 1 condition
• Chemistry: 290.4 Da · C20H22N2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL946
Name	Azatadine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	19861
ChEBI	CHEBI:2946
ATC	R06AX09
Molecular formula	C20H22N2
Molecular weight	290.4
InChIKey	SEBMTIQKRHYNIT-UHFFFAOYSA-N

SMILES: CN1CCC(=C2C3=CC=CC=C3CCC4=C2N=CC=C4)CC1

IUPAC name: 2-(1-methylpiperidin-4-ylidene)-4-azatricyclo[9.4.0.03,8]pentadeca-1(15),3(8),4,6,11,13-hexaene

ChEBI definition: A benzo[5,6]cyclohepta[1,2-b]pyridine having a 1-methylpiperidin-4-ylidene group at the 11-position.

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

Also known as: Azatadina, Azatadine, Trinalin, SID144206535, SID170464865, AZATADINE, azatadine

Parent form; salt/anhydrous children: CHEMBL3544908

Patent coverage: 2,560 distinct patent families (10,143 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 10,067 (99%) 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: 12 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C, Alpha-1A adrenergic receptor, Histamine H1 receptor, Kappa-type opioid receptor.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P31390	8.41	Ki	3.9	nM	CHEMBL_ACT_511685
HRH1	8.18	AC50	6.6	nM	CHEMBL_ACT_25212179
CHRM2	7.19	AC50	64	nM	CHEMBL_ACT_25195184
HRH1	7.18	AC50	66.5	nM	CHEMBL_ACT_25116927
CHRM2	7.1	AC50	80	nM	CHEMBL_ACT_25213427
CHRM1	6.96	AC50	110	nM	CHEMBL_ACT_25135119
HTR2A	6.84	AC50	143.8	nM	CHEMBL_ACT_25173497
HTR2A	6.47	AC50	340	nM	CHEMBL_ACT_25224871
HTR2B	5.8	AC50	1600	nM	CHEMBL_ACT_25227218
HTR2C	5.51	AC50	3100	nM	CHEMBL_ACT_25131488
HTR1A	5.25	AC50	5694	nM	CHEMBL_ACT_25164402
DRD2	5.14	AC50	7300	nM	CHEMBL_ACT_25140003
ADRA1A	5.06	AC50	8642	nM	CHEMBL_ACT_25137735
OPRK1	5.03	AC50	9376	nM	CHEMBL_ACT_25129132

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).