Back to discover

Protein / target

Beta-2 adrenergic receptor

Encoded byADRB2P07550Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
75
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Potassium channel regulator

Strongest disease association

Stroke

Via encoding gene ADRB2 · Genetic evidence · score 0.34

Therapeutic position

Established drug target

Small molecules

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways.

View complete UniProt function annotation

G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways (PubMed:2831218, PubMed:7915137). ADRB2 binds epinephrine (Epi) with an approximately 30-fold greater affinity than norepinephrine (NE) (PubMed:2831218, PubMed:33093660, PubMed:7915137). In the heart, Epi- and NE-activated ADRB2 induces rapid and slow cardiomyocyte contraction rate, respectively (By similarity). Both NE and Epi promote coupling to G(s)/PKA pathway to regulate myocyte contraction rate (By similarity). Epi also promotes ADRB2 coupling to G(i) proteins to exert cardioprotective effects especially in the conditions of hypoxia and oxidative stress through the G(i)/PI3K/Akt signaling pathway (By similarity). ADRB2-G(s) signaling delivers proapoptotic signals in cardiomyocytes although G(i)-mediated survival effect appears to predominate (By similarity). ADRB2 also transduces signals independently of PKA to regulate cellular pH by modulating Na(+)/H(+) exchanger SLC9A3 function (PubMed:9560162)

Subcellular location

Cell membraneGolgi apparatus
Domains and Gene Ontology detail (41)

Gene Ontology

  • Capical plasma membrane
  • Cclathrin-coated endocytic vesicle membrane
  • Cendosome
  • Cendosome membrane
  • CGolgi apparatus
  • Clysosome
  • Cmembrane
  • Cneuronal dense core vesicle
  • Cnucleus
  • Cplasma membrane
  • Creceptor complex
  • Fadenylate cyclase binding

413 aa · 46 kDa

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Excitatory neurotransmissionGOCell proliferation & survivalUniProtG protein-coupled signallingUniProt · GOApoptosis & cell deathGO
View supporting evidence

Excitatory neurotransmission

  • ·positive regulation of mini excitatory postsynaptic potential

Cell proliferation & survival

  • ·G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) protein…

G protein-coupled signalling

  • ·G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) protein…
  • ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
  • ·negative regulation of G protein-coupled receptor signaling pathway

Apoptosis & cell death

  • ·negative regulation of cardiac muscle cell apoptotic process
  • ·positive regulation of cardiac muscle cell apoptotic process
View underlying pathways (5)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

ARRB2ARRB1SLC9A3…GNASSAGGRK2AKAP12SNX27ADRB1SRCADRB2

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Approved medicines with mapped indications

3 medicines · 16 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Lung Diseases, Obstructive2 medicines
Angioedema1 medicine
Asthma1 medicine
Glaucoma1 medicine
Heart Arrest1 medicine
Heart Failure1 medicine
Hemorrhage1 medicine
Hypersensitivity1 medicine
Hypertension1 medicine
Myocardial Infarction1 medicine
Pulmonary Disease, Chronic Obstructive1 medicine
Shock, Septic1 medicine
Sinusitis1 medicine
Urticaria1 medicine
Ventricular Dysfunction, Left1 medicine
Broader indication categories (1)
Cardiovascular Diseases2 medicines

Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.

75 medicines meet Open Targets' target-level approved-medicine definition; the 3 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

3

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

albuterol
Narrow target profileApprovedAgonist

Beta-2 adrenergic receptor agonist

Indicated for Lung Diseases, Obstructive, Pulmonary Disease, Chronic Obstructive

Direct interaction with this protein · Only this protein recorded as a target

carvedilol
ApprovedAntagonist

Adrenergic receptor beta antagonist

Indicated for Heart Failure, Hypertension, Myocardial Infarction, Ventricular Dysfunction, Left

Acts on a complex — shared with ADRB1, ADRB3 · 1 of 6 recorded protein targets

Epinephrine
ApprovedAgonist

Adrenergic receptor agonist

Indicated for Angioedema, Asthma, Glaucoma, Heart Arrest

Acts on a complex — shared with ADRA1A, ADRA2A, ADRA1D +5 more · 1 of 9 recorded protein targets — broad pharmacology

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene ADRB2

Gene-level evidence surfaced through the gene ADRB2 that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Glaucoma, Open-Angle
0.81Well supported

Clinical evidence dominant · Open Targets 0.62

Stroke
0.80Well supported

Clinical evidence dominant · Open Targets 0.60

Glaucoma
0.79Well supported

Clinical evidence dominant · Open Targets 0.62

Asthma
0.78Well supported

Clinical evidence dominant · Open Targets 0.63

Pulmonary Disease, Chronic Obstructive
0.78Well supported

Clinical evidence dominant · Open Targets 0.63

View evidence synthesis (5)
Glaucoma, Open-AngleWell supported
0.81
agreement 0.680.93
Clinical76%Animal model21%Literature3%

Open Targets aggregate 0.62 · 3 independent evidence families

StrokeWell supported
0.80
agreement 0.700.91
Clinical60%Genetic31%Literature9%

Open Targets aggregate 0.60 · 3 independent evidence families

GlaucomaWell supported
0.79
agreement 0.660.92
Clinical79%Animal model17%Literature4%

Open Targets aggregate 0.62 · 3 independent evidence families

AsthmaWell supported
0.78
agreement 0.650.92
Clinical85%Literature15%RNA expression0%

Open Targets aggregate 0.63 · 3 independent evidence families

Pulmonary Disease, Chronic ObstructiveWell supported
0.78
agreement 0.630.94
Clinical86%Literature14%

Open Targets aggregate 0.63 · 2 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Asthma0.63
Pulmonary Disease, Chronic Obstructive0.63
Glaucoma, Open-Angle0.62
Hypertension0.62
Glaucoma0.62
Myocardial Infarction0.61
Ocular Hypertension0.61
Heart Failure0.60
Migraine Disorders0.60
Stroke0.60

Drug development

96 compounds recorded · 75 approved · 17 in clinical development · 4 earlier-stage

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 3 drugs that target this protein in Forefront's canonical graph (3 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
NADOLOLApproval
TERBUTALINEApproval
METIPRANOLOLApproval
LEVALBUTEROL TARTRATEPhase 3
EPHEDRINE SULFATEApproval
BEDORADRINEPhase 2
PROPRANOLOLApproval
MILVETEROLPhase 2
ARFORMOTEROL TARTRATEApproval
LEVOBUNOLOLApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (uniprot ubiquitination and small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (11)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMAB · Human Protein Atlas locPR · UniProt UbiquitinationPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

hypertriglyceridemiaClinPGxbronchospasmLynch et al. (2017)increased blood glucoseLynch et al. (2017)sexual adverse eventsClinPGxdecreased blood potassiumLynch et al. (2017)bronchodilationBowes et al. (2012)increased blood pressureLynch et al. (2017)increased heart rateBowes et al. (2012)Promotion, mesovarian leiomyomasAOP-Wikireceptor bindingToxCastcardiovascular performanceUrban et al. (2012)hypotensionClinPGx

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

RECRUITING · via carvedilol · NCT05931276

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 3 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Regulatory approval2026-09-14

    Approval: EPINEPHRINE (ANDA219832)

    fda · regulatory · fda · via Epinephrine

  2. Trial status changed2026-08-28

    Effect of Adding a Low-Dose Epinephrine Bolus Prior to Infusion on Maternal Hemodynamic Stability During Cesarean Section Under Spinal Anesthesia: A Randomized Clinical Trial

    Status changed to Completed · ClinicalTrials.gov · via Epinephrine

  3. Supplemental approval2026-08-27

    Supplemental approval: CARVEDILOL (ANDA078786)

    fda · regulatory · fda · via carvedilol

  4. Regulatory approval2026-07-31

    Approval: EPINEPHRINE (ANDA217426)

    fda · regulatory · fda · via Epinephrine

  5. Label change2026-06-22

    Label change: EPINEPHRINE (NDA204640)

    fda · regulatory · fda · via Epinephrine

  6. Product recall2026-05-14

    Recall (Class III): EPINEPHRINE

    fda · safety · fda · via Epinephrine

  7. Supplemental approval2024-10-09

    Supplemental approval: CARVEDILOL (ANDA078786)

    fda · regulatory · fda · via carvedilol

  8. Regulatory approval2024-08-22

    Approval: Eurneffy (EMA)

    ema · regulatory · ema · via Epinephrine

  9. New publication2023-11-07
    Impact of norepinephrine on immunity and oxidative metabolism in sepsis.

    Frontiers in immunology · 2023 · 33 citations · Europe PMC · via Epinephrine

  10. New publication2023-09-25
    Multicenter, Prospective, Randomized Controlled Trial of High-Sensitivity Cardiac Troponin I-Guided Combination Angiotensin Receptor Blockade and Beta-Blocker Therapy to Prevent Anthracycline Cardiotoxicity: The Cardiac CARE Trial.

    Circulation · 2023 · 53 citations · Europe PMC · via carvedilol

  11. New publication2013-03-04
    Beclometasone-formoterol as maintenance and reliever treatment in patients with asthma: a double-blind, randomised controlled trial.

    The Lancet. Respiratory medicine · 2013 · 107 citations · Europe PMC · via albuterol

  12. New publication1996-05-01
    The effect of carvedilol on morbidity and mortality in patients with chronic heart failure. U.S. Carvedilol Heart Failure Study Group.

    The New England journal of medicine · 1996 · 2,888 citations · Europe PMC · via carvedilol

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.