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Protein / target

Type-1 angiotensin II receptor

Encoded byAGTR1P30556Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
22
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Angiotensin type II receptor

Strongest disease association

Renal tubular dysgenesis of genetic origin

Via encoding gene AGTR1 · Genetic literature evidence · score 0.89

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

Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator of blood pressure and sodium retention by the kidney.

View complete UniProt function annotation

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.

Lipid & lipoprotein metabolismGOCell proliferation & survivalGOCell migrationGOImmune signallingGOG protein-coupled signallingGO
View supporting evidence

Lipid & lipoprotein metabolism

  • ·low-density lipoprotein particle remodeling
  • ·positive regulation of cholesterol metabolic process

Cell proliferation & survival

  • ·regulation of cell population proliferation

Cell migration

  • ·cell chemotaxis

Immune signalling

  • ·inflammatory response
  • ·positive regulation of inflammatory response
  • ·regulation of inflammatory response

G protein-coupled signalling

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

Approved medicines with mapped indications

4 medicines · 11 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.

Hypertension3 medicines
Diabetes Mellitus2 medicines
Myocardial Infarction2 medicines
Stroke2 medicines
Diabetes Mellitus, Type 21 medicine
Diabetic Nephropathies1 medicine
Glomerulonephritis, IGA1 medicine
Heart Failure1 medicine
Kidney Failure, Chronic1 medicine
Ventricular Dysfunction, Left1 medicine
Broader indication categories (1)
Cardiovascular Diseases3 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.

22 medicines meet Open Targets' target-level approved-medicine definition; the 4 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

6

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.

valsartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

Indicated for Diabetes Mellitus, Heart Failure, Hypertension, Myocardial Infarction

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

candesartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

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

telmisartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

Indicated for Diabetes Mellitus, Hypertension, Myocardial Infarction, Stroke

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

irbesartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

Indicated for Diabetes Mellitus, Type 2, Diabetic Nephropathies, Hypertension, Kidney Failure, Chronic

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

sparsentan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

Indicated for Glomerulonephritis, IGA

Direct interaction with this protein · 1 of 2 recorded protein targets — narrow recorded profile

azilsartan
Narrow target profileApprovedAntagonist

Type-1 angiotensin II receptor antagonist

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

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 AGTR1

Gene-level evidence surfaced through the gene AGTR1 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.

Hypertension
0.94Well supported

Clinical evidence dominant · Open Targets 0.74

Essential Hypertension
0.93Well supported

Clinical evidence dominant · Open Targets 0.72

Essential hypertension, genetic
0.87Well supported

Genetic evidence dominant · Open Targets 0.61

Renal tubular dysgenesis of genetic origin
0.84Well supported

Genetic evidence dominant · Open Targets 0.72

Renal tubular dysgenesis
0.81Well supported

Genetic evidence dominant · Open Targets 0.75

View evidence synthesis (5)
HypertensionWell 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 per-type scores above show the calculation.

Show all associations
Renal tubular dysgenesis0.75
Hypertension0.74
Renal tubular dysgenesis of genetic origin0.72
Essential Hypertension0.72
Heart Failure0.62
Myocardial Infarction0.62
Essential hypertension, genetic0.61
Kidney Diseases0.61

Drug development

24 compounds recorded · 22 approved · 2 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 6 drugs that target this protein in Forefront's canonical graph (4 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
ANGIOTENSIN IIApproval
SARALASINApproval
VALSARTANApproval
FIMASARTANApproval
AZILSARTAN KAMEDOXOMILApproval
TRV-120027Phase 2 3
ANGIOTENSIN II ACETATEApproval
PRATOSARTANPhase 3
TELMISARTANApproval
SARALASIN ACETATEApproval

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

Other modalitiesStrong

Approved Drug support this modality.

View underlying tractability evidence (10)
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

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

increased painLynch et al. (2017)receptor bindingToxCastexcessive thirstUrban et al. (2012)renal failureLynch et al. (2017)dry mouthUrban et al. (2012)hypotensionUrban et al. (2012)hypocalvariaLynch et al. (2017)slow or irregular heartbeatUrban et al. (2012)decreased blood pressureLynch et al. (2017)cell proliferation and migrationUrban et al. (2012)oligoamniosLynch et al. (2017)persistent patent ductus arteriosusLynch et al. (2017)

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)

UNKNOWN · via candesartan · NCT01629225

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 4 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 approval2026-08-11

    Approval: VALSARTAN (ANDA205357)

    fda · regulatory · fda · via valsartan

  2. Regulatory approval2026-08-04

    Approval: SACUBITRIL AND VALSARTAN (ANDA219946)

    fda · regulatory · fda · via valsartan

  3. Product recall2026-08-04

    Recall (Class II): VALSARTAN

    fda · safety · fda · via valsartan

  4. Label change2026-07-24

    Label change: IRBESARTAN (NDA020757)

    fda · regulatory · fda · via irbesartan

  5. Label change2026-07-13

    Label change: IRBESARTAN (ANDA077205)

    fda · regulatory · fda · via irbesartan

  6. Label change2025-08-01

    Label change: IRBESARTAN (NDA020757)

    fda · regulatory · fda · via irbesartan

  7. 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

  8. Regulatory approval2024-04-19

    Approval: Filspari (EMA)

    ema · regulatory · ema · via sparsentan

  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 candesartan

  10. 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

  11. New publication2008-11-11
    Irbesartan in patients with heart failure and preserved ejection fraction.

    The New England journal of medicine · 2008 · 1,406 citations · Europe PMC · via irbesartan

  12. Regulatory approval1997-08-26

    Approval: Aprovel (EMA)

    ema · regulatory · ema · via irbesartan

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.