Protein / target

Type-1 angiotensin II receptor

AGTR1P30556Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
22
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Angiotensin type II receptor activity

Primary system

Immune system

Strongest disease association

renal tubular dysgenesis of genetic origin

Genetic literature evidence · score 0.89

Therapeutic maturity

Clinically validated target

22 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

22 approved · 2 in clinical development

30 linked trials

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

Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator of blood pressure and sodium retention by the kidney (PubMed:15611106, PubMed:1567413, PubMed:25913193, PubMed:26420482, PubMed:30639100, PubMed:32079768, PubMed:8987975). The activated receptor in turn couples to G-alpha proteins G(q) (GNAQ, GNA11, GNA14 or GNA15) and thus activates phospholipase C and increases the cytosolic Ca(2+) concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C (PubMed:15611106)

Subcellular location

Cell membrane
Domains and Gene Ontology detail (33)

Gene Ontology

  • Cmembrane
  • Cplasma membrane
  • Fangiotensin type I receptor activity
  • Fangiotensin type II receptor activity
  • Fbradykinin receptor binding
  • Fprotein heterodimerization activity
  • Pangiotensin-activated signaling pathway
  • Pblood vessel diameter maintenance
  • Pcalcium-mediated signaling
  • Pcell chemotaxis
  • PG protein-coupled receptor signaling pathway
  • Pinflammatory response

359 aa · 41 kDa

Biological roles

Reactome v97

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

Immune signallingGOG protein-coupled signallingGOMetabolic enzyme activityGOKinase signallingUniProt
View supporting evidence

Immune signalling

  • ·inflammatory response
  • ·positive regulation of inflammatory response
  • ·regulation of inflammatory response
  • ·symbiont entry into host cell

G protein-coupled signalling

  • ·G protein-coupled receptor signaling pathway
  • ·phospholipase C-activating G protein-coupled receptor signaling pathway

Metabolic enzyme activity

  • ·positive regulation of cholesterol metabolic process
  • ·positive regulation of reactive oxygen species metabolic process

Kinase signalling

  • ·Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator o…
View underlying pathways (4)

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.

AGTGNAQACE2AGTRAPAGTR2BDKRB2ACERENKNG1ARRB2AGTR1

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.

Drugs targeting this protein

2

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

valsartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

Appears in clinical studies involving congestive heart failure, heart failure, myocardial infarction, hypertensive disorder

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

candesartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

Appears in clinical studies involving Hypertension, cardiovascular disorder, chronic kidney disease, hemorrhagic stroke

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

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

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Strongest genetic associations

Human genetic evidence — the most direct causal link between this target and a disease.

renal tubular dysgenesis of genetic origin0.89

Genetic literature · overall 0.72

renal tubular dysgenesis0.86

Genetic literature · overall 0.75

essential hypertension, genetic0.80

Genetic · overall 0.61

hypertensive disorder0.76

Genetic literature · overall 0.74

essential hypertension0.76

Genetic literature · overall 0.72

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

Hypertension1.00

Clinical · overall 0.63

myocardial infarction0.99

Clinical · overall 0.62

heart failure0.99

Clinical · overall 0.62

kidney disorder0.99

Clinical · overall 0.61

congestive heart failure0.98

Clinical · overall 0.61

Show all associations
renal tubular dysgenesis0.75
hypertensive disorder0.74
renal tubular dysgenesis of genetic origin0.72
essential hypertension0.72
Hypertension0.63
heart failure0.62
myocardial infarction0.62
essential hypertension, genetic0.61
congestive heart failure0.61
kidney disorder0.61

Open Targets ranks 1,493 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 24 total

ANGIOTENSIN IIApproval

cardiovascular disorder · Increased blood pressure · septic shock

SARALASINApproval

Hypertension

VALSARTANApproval

congestive heart failure · heart failure · myocardial infarction

FIMASARTANApproval

cardiovascular disorder · essential hypertension · Hypertension

AZILSARTAN KAMEDOXOMILApproval

hypertensive disorder · stroke disorder · Hypertension

TRV-120027Phase 2 3

COVID-19 · heart failure · heart failure

ANGIOTENSIN II ACETATEApproval

Shock · hypotensive disorder · septic shock

PRATOSARTANPhase 3

Hypertension

TELMISARTANApproval

hypertensive disorder · Hypertension · stroke disorder

SARALASIN ACETATEApproval

Hypertension

Tractability

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · Database UbiquitinationPR · Small Molecule BinderOC · Approved Drug

Safety liabilities

increased painreceptor bindingexcessive thirstrenal failuredry mouthhypotensionhypocalvariaslow or irregular heartbeatdecreased blood pressurecell proliferation and migrationoligoamniospersistent patent ductus arteriosus

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.

Show remaining trials (24)

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

hypertensive disorderWell supported
0.94
agreement 0.841.00
Clinical41%Genetic literature33%Animal model18%Literature7%

Open Targets aggregate 0.74 · 4 independent evidence families

essential hypertensionWell supported
0.93
agreement 0.821.00
Clinical40%Genetic literature35%Animal model19%Literature5%Geneticdup

Open Targets aggregate 0.72 · 4 independent evidence families · 1 not counted as duplicate

essential hypertension, geneticWell supported
0.87
agreement 0.750.99
Genetic71%Animal model29%Literature0%Genetic literaturedup

Open Targets aggregate 0.61 · 3 independent evidence families · 1 not counted as duplicate

renal tubular dysgenesis of genetic originWell supported
0.84
agreement 0.720.96
Genetic88%Animal model11%Literature1%Genetic literaturedup

Open Targets aggregate 0.72 · 3 independent evidence families · 1 not counted as duplicate

renal tubular dysgenesisWell supported
0.81
agreement 0.690.93
Genetic88%Animal model11%Literature1%Genetic literaturedup

Open Targets aggregate 0.75 · 3 independent evidence families · 1 not counted as duplicate

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 underlying per-type scores are shown above so the calculation can be checked.

What's happening now

7

Recent activity around this target, drawn from one canonical event stream. Every item is reached through 2 drugs that target this protein, so each event is news about that drug rather than about the protein directly.

  1. New publication2024-06-26
    Cardiovascular-kidney-metabolic overlap in heart failure with preserved ejection fraction: Cardiac structure and function, clinical outcomes, and response to sacubitril/valsartan in PARAGON-HF.

    European journal of heart failure · 2024 · 19 citations · Europe PMC · via valsartan

  2. 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 candesartan

  3. New publication2015-03-28
    Ambulatory 24-hour cardiac oxygen consumption and blood pressure-heart rate variability: effects of nebivolol and valsartan alone and in combination.

    Journal of the American Society of Hypertension : JASH · 2015 · 12 citations · Europe PMC · via valsartan

  4. New publication2014-08-30
    Angiotensin-neprilysin inhibition versus enalapril in heart failure.

    The New England journal of medicine · 2014 · 4,715 citations · Europe PMC · via valsartan

  5. New publication2013-05-01
    Efficacy and safety of valsartan in hypertensive children 6 months to 5 years of age.

    Journal of hypertension · 2013 · 10 citations · Europe PMC · via valsartan

  6. New publication2004-09-01
    Relation between renal dysfunction and cardiovascular outcomes after myocardial infarction.

    The New England journal of medicine · 2004 · 1,345 citations · Europe PMC · via valsartan

  7. New publication2003-11-10
    Valsartan, captopril, or both in myocardial infarction complicated by heart failure, left ventricular dysfunction, or both.

    The New England journal of medicine · 2003 · 1,589 citations · Europe PMC · via valsartan

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.