Azelnidipine

Summary

Azelnidipine (CHEMBL1275868) is a phase-3 clinical-stage small molecule.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Clinical trials: 2
• Chemistry: 582.6 Da · C33H34N4O6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1275868
Name	Azelnidipine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	65948
Molecular formula	C33H34N4O6
Molecular weight	582.6
InChIKey	ZKFQEACEUNWPMT-UHFFFAOYSA-N

SMILES: CC1=C(C(C(=C(N1)N)C(=O)OC2CN(C2)C(C3=CC=CC=C3)C4=CC=CC=C4)C5=CC(=CC=C5)[N+](=O)[O-])C(=O)OC(C)C

IUPAC name: 3-O-(1-benzhydrylazetidin-3-yl) 5-O-propan-2-yl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Also known as: Azelnidipine, Azelnidipino, Calblock, CS-905, CS905, SID50112690, SID144205993, SID170465756, SID174006618, AZELNIDIPINE, azelnidipine

Patent coverage: 1,077 distinct patent families (3,798 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,647 (96%) 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: 15 (assay-derived). Sample: Nuclear receptor ROR-gamma, 4’-phosphopantetheinyl transferase ffp, Alpha-2C adrenergic receptor, Menin/Histone-lysine N-methyltransferase MLL, Beta-1 adrenergic receptor, Motilin receptor, Sodium-dependent noradrenaline transporter, Type-1 angiotensin II receptor, Alpha-1A adrenergic receptor, Sodium-dependent dopamine transporter, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D, Nuclear receptor subfamily 1 group I member 2, Voltage-dependent L-type calcium channel subunit alpha-1C, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 16 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P22002	7.04	AC50	92	nM	CHEMBL_ACT_25119440
ADORA3	5.66	AC50	2200	nM	CHEMBL_ACT_25134015
NR1I2	5.43	AC50	3700	nM	CHEMBL_ACT_25188046
SLC6A2	5.24	AC50	5800	nM	CHEMBL_ACT_25144806
PDE4D	5.18	AC50	6600	nM	CHEMBL_ACT_25185126

Target pathways

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

Indications & clinical

Indications

0 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE4	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01819441	PHASE4	UNKNOWN	Stratification of Blood Pressure Control Against Progress of Cerebral Small Vessel Diseases in Poststroke Patients
NCT01028534	Not specified	COMPLETED	Effects of Antihypertensive Drugs in Patients With Hypertension and Obstructive Sleep Apnea (OSA)

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).