Celiprolol

Summary

Celiprolol (CHEMBL27810) is an approved small molecule (ATC C07AB08); indicated across 2 conditions including cardiovascular disorder and ehlers-danlos syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C07AB08
• Indications: 2 conditions
• Clinical trials: 3
• Chemistry: 379.5 Da · C20H33N3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL27810
Name	Celiprolol
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2663
ATC	C07AB08
Molecular formula	C20H33N3O4
Molecular weight	379.5
InChIKey	JOATXPAWOHTVSZ-UHFFFAOYSA-N

SMILES: CCN(CC)C(=O)NC1=CC(=C(C=C1)OCC(CNC(C)(C)C)O)C(=O)C

IUPAC name: 3-[3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-1,1-diethylurea

Also known as: ACER-002 FREE BASE, ACER002 FREE BASE, Celiprolol, Celiprolol pch, CELIPROLOL, celiprolol, (-)-CELIPROLOL

Parent form; salt/anhydrous children: CHEMBL1742424

Patent coverage: 2,167 distinct patent families (9,169 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,153 (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: 4 (assay-derived). Sample: Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRB1	7.12	AC50	76	nM	CHEMBL_ACT_25122087
ADRB2	5.34	AC50	4600	nM	CHEMBL_ACT_25123128
P19327	5.05	Ki	8913	nM	CHEMBL_ACT_835267

Target pathways

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

Indications & clinical

Indications

2 indications (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
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
Ehlers-Danlos syndrome	3	MONDO:0020066	MONDO:0020066

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE4	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00190411	PHASE4	COMPLETED	Celiprolol in Patients With Ehlers-Danlos Syndrome, Vascular Type
NCT02380053	PHASE4	COMPLETED	Chronic Beta-blockade and Cardiopulmonary Exercise in COPD
NCT03752931	PHASE2	UNKNOWN	Celiprolol Versus Ditiazem for the Prevention of Postoperative Cardiac Arrythmias in Thoracic Surgery

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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