Atenolol

Summary

Atenolol (CHEMBL24) is an approved small-molecule β-adrenergic antagonist (ATC C07AB03) targeting ADRB1 and ADRB2; indicated across 21 conditions including hypertensive disorder and myocardial infarction.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C07AB03
• Targets: 2 (ADRB1, ADRB2)
• Indications: 21 conditions
• Clinical trials: 81
• Chemistry: 266.34 Da · C14H22N2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL24
Name	Atenolol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2249
ChEBI	CHEBI:2904
ATC	C07AB03
Molecular formula	C14H22N2O3
Molecular weight	266.34
InChIKey	METKIMKYRPQLGS-UHFFFAOYSA-N

SMILES: CC(C)NCC(COC1=CC=C(C=C1)CC(=O)N)O

IUPAC name: 2-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide

ChEBI definition: An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.

Pharmacological roles (ChEBI): β-adrenergic antagonist, anti-arrhythmia drug, antihypertensive agent, sympatholytic agent.

Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.

Also known as: Antipressan, Atenamin, Atenix-100, Atenix-25, Atenix-50, Atenolol, Atenolol component of polycap, Atenolol component of tenoretic, Atenololum, Betacard, C07AB03, Corotenol

Patent coverage: 12,471 distinct patent families (48,715 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 48,714 (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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
ADRB1	β1-adrenoceptor	Antagonist	7.6	0%	P08588
ADRB2	β2-adrenoceptor	Antagonist	6	0.4%	P07550

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Prelamin-A/C, Adrenergic receptor alpha-1, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, Cannabinoid receptor 1, 5-hydroxytryptamine receptor 1A, Urease, Beta-2 adrenergic receptor.

Bioactivity

ChEMBL activities: 28 potent at pChembl ≥ 5 of 31 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRB1	8.75	IC50	1.77	nM	CHEMBL_ACT_1611105
LMNA	8.3	Potency	5	nM	CHEMBL_ACT_3654571
TDP1	7.15	Potency	70.8	nM	CHEMBL_ACT_3926612
ADRB1	6.82	Ki	150	nM	CHEMBL_ACT_13342047
ADRB1	6.8	Ki	160	nM	CHEMBL_ACT_26333270
ADRB1	6.77	Ki	170	nM	CHEMBL_ACT_6317037
ADRB1	6.68	IC50	210	nM	CHEMBL_ACT_16501839
ADRB1	6.68	IC50	210	nM	CHEMBL_ACT_16838403
ADRA1D	6.64	IC50	230	nM	CHEMBL_ACT_13336215
ADRB1	6.58	IC50	260	nM	CHEMBL_ACT_13342119
ADRB2	6.58	Kd	260	nM	CHEMBL_ACT_19403984
ADRB1	6.55	IC50	280	nM	CHEMBL_ACT_26333216
ADRB1	6.37	Ki	430	nM	CHEMBL_ACT_2401822
ADRB1	6.22	IC50	600	nM	CHEMBL_ACT_2401816
ADRB1	6.17	AC50	677.1	nM	CHEMBL_ACT_25121441
ADRB1	6.12	Ki	758	nM	CHEMBL_ACT_7603222
Q8K4Z4	5.93	Kd	1175	nM	CHEMBL_ACT_1027114
Q8K4Z4	5.93	Kd	1175	nM	CHEMBL_ACT_539540
ADRB2	5.92	Kd	1200	nM	CHEMBL_ACT_19403973
Q8K4Z4	5.9	Kd	1259	nM	CHEMBL_ACT_14606289
ADRB1	5.88	IC50	1313	nM	CHEMBL_ACT_7603221
ADRB1	5.82	Ki	1514	nM	CHEMBL_ACT_18377917
ADRB1	5.79	IC50	1640	nM	CHEMBL_ACT_5165962
ADRB1	5.76	IC50	1740	nM	CHEMBL_ACT_2573318
ADRB2	5.3	AC50	4987	nM	CHEMBL_ACT_25122609
ADRB2	5.02	Ki	9550	nM	CHEMBL_ACT_18377938
ADRB2	5	Ki	10060	nM	CHEMBL_ACT_7603224
P19327	5	Ki	10000	nM	CHEMBL_ACT_857539

Target pathways

Aggregated over 2 target gene(s): ADRB1, ADRB2.

Top Reactome pathways

16 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	2	ADRB1, ADRB2
Signaling by GPCR	2	ADRB1, ADRB2
Class A/1 (Rhodopsin-like receptors)	2	ADRB1, ADRB2
Amine ligand-binding receptors	2	ADRB1, ADRB2
GPCR downstream signalling	2	ADRB1, ADRB2
Adrenoceptors	2	ADRB1, ADRB2
G alpha (s) signalling events	2	ADRB1, ADRB2
GPCR ligand binding	2	ADRB1, ADRB2
Membrane Trafficking	1	ADRB2
Metabolism of proteins	1	ADRB2
Vesicle-mediated transport	1	ADRB2
Deubiquitination	1	ADRB2
Ub-specific processing proteases	1	ADRB2
Post-translational protein modification	1	ADRB2
Cargo recognition for clathrin-mediated endocytosis	1	ADRB2
Clathrin-mediated endocytosis	1	ADRB2

Dominant GO biological processes

GO term	Targets
diet induced thermogenesis	2
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	2
adenylate cyclase-activating G protein-coupled receptor signaling pathway	2
response to cold	2
positive regulation of cardiac muscle cell apoptotic process	2
heat generation	2
negative regulation of multicellular organism growth	2
positive regulation of MAPK cascade	2
brown fat cell differentiation	2
adenylate cyclase-activating adrenergic receptor signaling pathway	2
positive regulation of cold-induced thermogenesis	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
positive regulation of heart rate by epinephrine-norepinephrine	1
positive regulation of the force of heart contraction by epinephrine-norepinephrine	1

Indications & clinical

Indications

21 indications (7 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
hypertensive disorder	4	MONDO:0005044	EFO:0000537
myocardial infarction	4	MONDO:0005068	EFO:0000612
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
diabetes mellitus	4	MONDO:0005015	EFO:0000400
stroke disorder	4	MONDO:0005098	EFO:0000712
coronary artery disorder	4	MONDO:0005010	MONDO:0021661
heart disorder	3	MONDO:0005267	EFO:0003777
hemangioma	3	MONDO:0006500	EFO:1000635
atrial fibrillation	3	MONDO:0004981	EFO:0000275
heart failure	3	MONDO:0005252	EFO:0003144
cerebrovascular disorder	3	MONDO:0011057	EFO:0003763
mitral valve stenosis	3	MONDO:0005852	EFO:0007372
myocardial ischemia	3	MONDO:0024644	EFO:1001375
essential hypertension	3	MONDO:0001134	MONDO:0001134
Marfan syndrome	3	MONDO:0007947	MONDO:0007947
vascular disorder	3	MONDO:0005385	EFO:0004264
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358
postural orthostatic tachycardia syndrome	1	MONDO:0011479	EFO:1000645
osteoporosis	0	MONDO:0005298	EFO:0003882

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 81.

Phase distribution

Phase	Trials
PHASE4	33
PHASE3	17
Not specified	14
PHASE2	7
PHASE1	4
EARLY_PHASE1	3
PHASE2/PHASE3	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00133692	PHASE4	COMPLETED	INVEST: INternational VErapamil SR Trandolapril STudy
NCT00171132	PHASE4	COMPLETED	VALENCE: Valsartan Versus Atenolol on Exercise Capacity in Hypertensive Overweight Postmenopausal Women
NCT00171756	PHASE4	COMPLETED	Study to Compare the Effect of Valsartan vs Atenolol on Pro-thrombotic State in Hypertensive Patients.
NCT00185094	PHASE4	COMPLETED	A Comparison of the Effect of Olmesartan Medoxomil, Losartan Potassium, and Atenolol on the Ability of Overweight Patients With High Blood Pressure to Respond to Insulin
NCT00202358	PHASE4	UNKNOWN	Perioperative Effect of Atenolol on Cytokine Profiles
NCT00232882	PHASE4	COMPLETED	Pharmacodynamic Influences of Candesartan, Atenolol, Hydrochlorothiazide and Drug Combinations in Hypertensive Patients.
NCT00246519	PHASE4	COMPLETED	Pharmacogenomic Evaluation of Antihypertensive Responses
NCT00263393	PHASE4	COMPLETED	Rural Andhra Pradesh Cardiovascular Prevention Study (RAPCAPS)
NCT00295542	PHASE4	COMPLETED	Ambulatory Blood Pressure Monitoring in the Prediction of Cardiovascular Events and Effects of Chronotherapy
NCT00507663	PHASE4	COMPLETED	Elder Surgery - Functional Recovery Following Beta Blockade
NCT00529750	PHASE4	COMPLETED	Effect of the Angiotensin II Receptor Antagonist Irbesartan on Biochemical and Functional Markers of Endothelial Dysfunction in Patients With Hypertension
NCT00535925	PHASE4	COMPLETED	Nephropathy In Type 2 Diabetes and Cardio-renal Events
NCT00661895	PHASE4	COMPLETED	Black Education and Treatment of Hypertension (BEAT HTN)
NCT00669279	PHASE4	COMPLETED	Effect of Carvedilol Controlled-Release (CR) and Atenolol on Central Blood Pressure
NCT00772499	PHASE4	COMPLETED	Vascular Improvement With Olmesartan Medoxomil Study
NCT00925119	PHASE4	TERMINATED	Examining Genetic Influence on Response to Beta-Blocker Medications in People With Type 2 Diabetes
NCT01030016	PHASE4	COMPLETED	Study of Atenolol Influence on Blood Pressure During Resistance Exercise
NCT01079962	PHASE4	COMPLETED	An Active-controlled, Clinical Trial to Assess Central Hemodynamic Effects of Bisoprolol in Hypertensive Patients (Central Hemodynamic Assessment Measured in Patient With HypertensION [CHAMPION])
NCT01132768	PHASE4	TERMINATED	The Confirmatory Olmesartan Plaque Regression Study
NCT01230892	PHASE4	COMPLETED	Evaluation of The Effects of Nebivolol in Comparison to Atenolol on Wall Shear Stress and Rupture Prone Coronary Plaques
NCT01251146	PHASE4	COMPLETED	A Randomized Controlled Study to Assess the Effects of Bisoprolol and Atenolol on Resting Heart Rate and Sympathetic Nervous System’s Activity in Subjects With Essential Hypertension
NCT01295047	PHASE4	COMPLETED	Comparison of Medical Therapies in Marfan Syndrome.
NCT01397994	PHASE4	UNKNOWN	Study to Assess Efficacy of Nicorandil+Atenolol vs Atenolol in Treatment of Chronic Stable Angina.
NCT01445964	PHASE4	COMPLETED	Effect of SLCO2B1 Genotype and Apple Juice on Pharmacokinetics of Atenolol After Oral Administration in Healthy Male Korean
NCT01736488	PHASE4	COMPLETED	Clinical Study to Evaluate the Antihypertensive Efficacy and Changes of Neurohormonal Markers of Fimasartan and Atenolol With Exaggerated Blood Pressure Response During Exercise in Essential Hypertensive Patients
NCT01762436	PHASE4	COMPLETED	Effects of Bisoprolol and Atenolol on Sympathetic Nervous Activity and Central Aortic Pressure in Patients With Essential Hypertension
NCT01939509	PHASE4	COMPLETED	Hemodynamic Changes of Patients Receiving Atenolol/Bisoprolol
NCT02403349	PHASE4	UNKNOWN	Comparison of Peripheral and Cerebral Arterial Flow in Acute Ischemic Stroke: Fimasartan vs. Valsartan vs. Atenolol
NCT02441842	PHASE4	COMPLETED	Evaluation of Periop Biochemical Stress Factors in Craniotomy Neurosurgical Procedure With Respect to Preop Hypertension
NCT02547597	PHASE4	COMPLETED	Comparison of Carvedilol and Atenolol on Anti-anginal and Metabolic Effects in Patients With Stable Angina Pectoris
NCT03245996	PHASE4	COMPLETED	The Impact of Heart Rate on Central Blood Pressure in Sick Sinus Syndrome Patients With a Permanent Cardiac Pacemaker
NCT04931108	PHASE4	UNKNOWN	The Effect of Nitrendipine/Atenolol Combination on Blood Pressure Variability.
NCT05106179	PHASE4	UNKNOWN	The Efficacy and Safety of Beta-blockers Drugs in Adults With Spinal Hemangioma
NCT07268170	PHASE2/PHASE3	ENROLLING_BY_INVITATION	Heart Rate Control Before Cardiac Computed Tomography in Adults for the Evaluation of Coronary Artery Disease
NCT00000478	PHASE3	COMPLETED	Asymptomatic Cardiac Ischemia Pilot (ACIP) Study
NCT00000513	PHASE3	COMPLETED	Trial of Antihypertensive Intervention Management
NCT00000514	PHASE3	COMPLETED	Systolic Hypertension in the Elderly Program (SHEP)
NCT00108082	PHASE3	COMPLETED	The CLEVER Study - Coreg And Left Ventricular Mass Regression
NCT00145210	PHASE3	COMPLETED	Safety and Efficacy of Nebivolol in the Treatment of Hypertension in African Americans
NCT00185185	PHASE3	COMPLETED	Olmesartan Medoxomil in Atherosclerosis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for atenolol and CYP2D6	DPWG	CYP2D6
Annotation of CPIC Guideline for acebutolol, atenolol, betaxolol, biso	CPIC	ADRA2C;ADRB1;GRK4;GRK5

PharmGKB also curates 44 clinical and 118 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

238 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Desloratadine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
ACEBUTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ALBUTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BETAXOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BISOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARTEOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CELIPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DARIFENACIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOBUTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOMPERIDONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ESMOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
INDACATEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
METOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NADOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NEBIVOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
OXPRENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRENYLAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRIMAQUINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RANOLAZINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAMPIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAXIMIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RITODRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SOTALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TAMOXIFEN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2