Back to discover

Protein / target

Beta-3 adrenergic receptor

Encoded byADRB3P13945Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
21
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Beta-3 adrenergic receptor binding

Strongest disease association

Myocardial Infarction

Via encoding gene ADRB3 · Clinical evidence · score 0.62

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, leading to either activation or inhibition of adenylate cyclase and cAMP-dependent pathway, respectively.

View complete UniProt function annotation

G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, leading to either activation or inhibition of adenylate cyclase and cAMP-dependent pathway, respectively (PubMed:10188996, PubMed:2570461, PubMed:8641219). The rank order of potency for physiological agonists is norepinephrine > epinephrine (PubMed:10188996, PubMed:2570461, PubMed:8641219). Involved in the regulation of thermogenesis and lipolysis in brown and white adipose tissue, after coupling to G(s) proteins and stimulation of the cAMP-PKA axis (By similarity). Also activates lipolytic process by coupling to G(i) proteins and consequent initiation of the ERK1/2 MAP kinase cascade (PubMed:10207024). Participates in relaxation of the blood vessels and the urinary bladder (PubMed:10188996). Also mediates negative inotropic effects in cardiomyocytes through activation of an NO synthase pathway and subsequent increase in cGMP levels, possibly involving G(i/o) protein-mediated coupling (PubMed:9769330)

Subcellular location

Cell membrane
Domains and Gene Ontology detail (25)

Gene Ontology

  • Cplasma membrane
  • Creceptor complex
  • Fbeta-3 adrenergic receptor binding
  • Fbeta-adrenergic receptor activity
  • Fbeta3-adrenergic receptor activity
  • Fepinephrine binding
  • FG protein activity
  • Fnorepinephrine binding
  • Fprotein homodimerization activity
  • Padenylate cyclase-activating adrenergic receptor signaling pathway
  • Padenylate cyclase-inhibiting adrenergic receptor signaling pathway
  • Padenylate cyclase-inhibiting G protein-coupled receptor signaling pathway

408 aa · 44 kDa

Biological roles

Reactome v97

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

G protein-coupled signallingUniProt · GOMetabolic enzyme activityGOMuscle contractionGO
View supporting evidence

G protein-coupled signalling

  • ·G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) protein…
  • ·adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
  • ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
  • ·G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messen…

Metabolic enzyme activity

  • ·carbohydrate metabolic process
  • ·energy reserve metabolic process

Muscle contraction

  • ·negative regulation of cardiac muscle contraction
  • ·negative regulation of smooth muscle contraction
View underlying pathways (2)

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.

UCP1GNASADRB2GNAI1GNAI3GNAI2ADRB1SRCLIPEFGF21ADRB3

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 · 18 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.

Angioedema1 medicine
Asthma1 medicine
Glaucoma1 medicine
Heart Arrest1 medicine
Heart Failure1 medicine
Hemorrhage1 medicine
Hypersensitivity1 medicine
Hypertension1 medicine
Lung Diseases, Obstructive1 medicine
Myocardial Infarction1 medicine
Shock, Septic1 medicine
Sinusitis1 medicine
Urinary Bladder, Overactive1 medicine
Urinary Incontinence1 medicine
Urinary Incontinence, Urge1 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.

21 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.

mirabegron
Narrow target profileApprovedAgonist

Beta-3 adrenergic receptor agonist

Indicated for Urinary Bladder, Overactive, Urinary Incontinence, Urinary Incontinence, Urge

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, ADRB2 · 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, ADRB2 +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 ADRB3

Gene-level evidence surfaced through the gene ADRB3 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.

Myocardial Infarction
0.77Well supported

Clinical evidence dominant · Open Targets 0.62

Hypertension
0.76Well supported

Clinical evidence dominant · Open Targets 0.61

Heart Failure
0.76Well supported

Clinical evidence dominant · Open Targets 0.61

Urinary Bladder, Overactive
0.75Well supported

Clinical evidence dominant · Open Targets 0.61

Asthma
0.73Moderately supported

Clinical evidence dominant · Open Targets 0.60

View evidence synthesis (5)
Myocardial InfarctionWell supported
0.77
agreement 0.610.92
Clinical89%Literature11%

Open Targets aggregate 0.62 · 2 independent evidence families

HypertensionWell supported
0.76
agreement 0.600.91
Clinical94%Literature6%

Open Targets aggregate 0.61 · 2 independent evidence families

Heart FailureWell supported
0.76
agreement 0.600.91
Clinical88%Literature12%

Open Targets aggregate 0.61 · 2 independent evidence families

Urinary Bladder, OveractiveWell supported
0.75
agreement 0.590.91
Clinical95%Literature5%

Open Targets aggregate 0.61 · 2 independent evidence families

AsthmaModerately supported
0.73
agreement 0.580.89
Clinical100%Literature1%

Open Targets aggregate 0.60 · 2 independent evidence families

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
Myocardial Infarction0.62
Hypertension0.61
Heart Failure0.61
Urinary Bladder, Overactive0.61
Asthma0.60
Cardiovascular Diseases0.58

Drug development

28 compounds recorded · 21 approved · 5 in clinical development · 2 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)
CARVEDILOL PHOSPHATEApproval
SOLABEGRONPhase 2
HYDROXYAMPHETAMINE HYDROBROMIDEApproval
ISOPROTERENOLApproval
EPHEDRINE HYDROCHLORIDEApproval
RAFABEGRONPhase 2
CARTEOLOL HYDROCHLORIDEApproval
CARVEDILOLApproval
EPINEPHRINE BITARTRATEApproval
MEPHENTERMINEApproval

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

Protein degradersEmerging

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

View underlying tractability evidence (8)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

receptor bindingToxCastweight gainClinPGx

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)

ACTIVE_NOT_RECRUITING · via mirabegron · NCT05604222

RECRUITING · via carvedilol · NCT05931276

NOT_YET_RECRUITING · via mirabegron · NCT07566208

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. Product recall2026-08-05

    Recall (Class II): MIRABEGRON

    fda · safety · fda · via mirabegron

  5. Regulatory approval2026-07-31

    Approval: EPINEPHRINE (ANDA217426)

    fda · regulatory · fda · via Epinephrine

  6. Label change2026-06-22

    Label change: EPINEPHRINE (NDA204640)

    fda · regulatory · fda · via Epinephrine

  7. Product recall2026-05-14

    Recall (Class III): EPINEPHRINE

    fda · safety · fda · via Epinephrine

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

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

  9. 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

  10. New publication2019-10-31
    The effect of topical epinephrine 1:1000 with and without infiltration of 1% lidocaine with epinephrine 1:100,000 on endoscopic surgical field visualization: a double-blind randomized controlled study.

    International forum of allergy & rhinology · 2020 · 6 citations · Europe PMC · via Epinephrine

  11. Safety communication2015-10-14

    Drug Safety Update: Mirabegron (Betmiga▼): risk of severe hypertension and associated cerebrovascular and cardiac events

    mhra · safety · mhra · via mirabegron

  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.