Protein / target

P2Y purinoceptor 12

P2RY12Q9H244Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
12
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

G protein-coupled purinergic nucleotide receptor activity

Strongest disease association

platelet-type bleeding disorder 8

Genetic evidence · score 0.85

Therapeutic maturity

Clinically validated target

12 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

12 approved · 3 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 ADP and ATP coupled to G proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation

Subcellular location

Cell membrane
Domains and Gene Ontology detail (31)

Gene Ontology

  • Ccell body membrane
  • Ccell projection membrane
  • Ccell surface
  • Cmembrane
  • Cplasma membrane
  • FG protein-coupled adenosine receptor activity
  • FG protein-coupled ADP receptor activity
  • FG protein-coupled purinergic nucleotide receptor activity
  • Fguanyl-nucleotide exchange factor activity
  • Padenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
  • Pcalcium-mediated signaling
  • Pcell projection organization

342 aa · 39 kDa

Biological roles

Reactome v97

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

HaemostasisUniProt · GOG protein-coupled signallingGOKinase signallingGOImmune signallingGOCell adhesionGO
View supporting evidence

Haemostasis

  • ·Receptor for ADP and ATP coupled to G proteins that inhibit the adenylyl cyclase second…
  • ·hemostasis
  • ·platelet activation
  • ·platelet aggregation

G protein-coupled signalling

  • ·G protein-coupled adenosine receptor activity
  • ·G protein-coupled ADP receptor activity
  • ·G protein-coupled purinergic nucleotide receptor activity
  • ·adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway

Kinase signalling

  • ·positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction

Immune signalling

  • ·substrate-dependent cell migration, cell extension

Cell adhesion

  • ·positive regulation of cell adhesion mediated by integrin
View underlying pathways (3)

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.

P2RX1P2RY1GNAI2GNAI1CYP2C19GNAI3P2RY13TREM2TMEM119GP6P2RY12

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.

Ticagrelor
Narrow target profileApprovedNegative allosteric modulator

Purinergic receptor P2Y12 negative allosteric modulator

Appears in clinical studies involving acute coronary syndrome, type 2 diabetes mellitus, coronary artery disorder, myocardial infarction

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

Prasugrel Hydrochloride
Narrow target profileApprovedAntagonist

Purinergic receptor P2Y12 antagonist

Appears in clinical studies involving myocardial infarction, myocardial ischemia, acute coronary syndrome, angina unstable

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.

platelet-type bleeding disorder 80.85

Genetic · overall 0.71

P2Y12 defect0.78

Genetic · overall 0.67

Highest-confidence therapeutic associations

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

acute coronary syndrome1.00

Clinical · overall 0.61

myocardial infarction1.00

Clinical · overall 0.62

Stroke0.98

Clinical · overall 0.61

peripheral vascular disease0.98

Clinical · overall 0.60

coronary artery disorder0.97

Clinical · overall 0.60

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

stroke disorder0.59

Clinical

peripheral arterial disease0.56

Clinical

angina unstable0.56

Clinical

Show all associations
platelet-type bleeding disorder 80.71
P2Y12 defect0.67
myocardial infarction0.62
acute coronary syndrome0.61
Stroke0.61
coronary artery disorder0.60
peripheral vascular disease0.60
stroke disorder0.59
peripheral arterial disease0.56
angina unstable0.56

Open Targets ranks 482 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 · 15 total

TICAGRELORApproval

acute coronary syndrome · type 2 diabetes mellitus · coronary artery disorder

ELINOGRELPhase 2

myocardial infarction

CANGRELOR TETRASODIUMApproval

myocardial infarction · Recurrent thrombophlebitis

PRASUGREL HYDROCHLORIDEApproval

myocardial infarction · myocardial ischemia · acute coronary syndrome

CLOPIDOGREL HYDROBROMIDEApproval

acute coronary syndrome · peripheral vascular disease · myocardial infarction

CANGRELORApproval

Recurrent thrombophlebitis · thrombotic disease · acute coronary syndrome

TICLOPIDINE HYDROCHLORIDEApproval

thrombotic disease · stroke disorder

SELATOGRELPhase 3

acute myocardial infarction · Non-ST Elevation Myocardial Infarction

TICLOPIDINEApproval

Recurrent thrombophlebitis · Stroke · angina pectoris

PRASUGRELApproval

Recurrent thrombophlebitis · acute coronary syndrome · myocardial infarction

Tractability

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

Safety liabilities

neurological events

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)

TERMINATED · via Ticagrelor · NCT01998399

UNKNOWN · via Ticagrelor · NCT02285751

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.

platelet-type bleeding disorder 8Well supported
0.85
agreement 0.730.97
Genetic100%Genetic literaturedup

Open Targets aggregate 0.71 · 1 independent evidence family · 1 not counted as duplicate

P2Y12 defectWell supported
0.78
agreement 0.660.90
Genetic100%Genetic literaturedup

Open Targets aggregate 0.67 · 1 independent evidence family · 1 not counted as duplicate

myocardial infarctionWell supported
0.77
agreement 0.610.92
Clinical91%Literature9%

Open Targets aggregate 0.62 · 2 independent evidence families

acute coronary syndromeWell supported
0.76
agreement 0.600.91
Clinical96%Literature4%

Open Targets aggregate 0.61 · 2 independent evidence families

StrokeWell supported
0.75
agreement 0.600.91
Clinical92%Literature8%

Open Targets aggregate 0.61 · 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 underlying per-type scores are shown above so the calculation can be checked.

What's happening now

6

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 publication2020-06-01
    Effect of Ticagrelor Monotherapy vs Ticagrelor With Aspirin on Major Bleeding and Cardiovascular Events in Patients With Acute Coronary Syndrome: The TICO Randomized Clinical Trial.

    JAMA · 2020 · 407 citations · Europe PMC · via Ticagrelor

  2. New publication2019-09-03
    A Genotype-Guided Strategy for Oral P2Y<sub>12</sub> Inhibitors in Primary PCI.

    The New England journal of medicine · 2019 · 462 citations · Europe PMC · via Prasugrel Hydrochloride

  3. New publication2019-09-01
    Ticagrelor or Prasugrel in Patients with Acute Coronary Syndromes.

    The New England journal of medicine · 2019 · 482 citations · Europe PMC · via Prasugrel Hydrochloride

  4. New publication2019-06-01
    Effect of 1-Month Dual Antiplatelet Therapy Followed by Clopidogrel vs 12-Month Dual Antiplatelet Therapy on Cardiovascular and Bleeding Events in Patients Receiving PCI: The STOPDAPT-2 Randomized Clinical Trial.

    JAMA · 2019 · 608 citations · Europe PMC · via Prasugrel Hydrochloride

  5. New publication2014-09-01
    Prehospital ticagrelor in ST-segment elevation myocardial infarction.

    The New England journal of medicine · 2014 · 438 citations · Europe PMC · via Ticagrelor

  6. Regulatory approval2010-12-03

    Approval: Brilique (EMA)

    ema · regulatory · ema · via Ticagrelor

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.