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Protein / target

P2X purinoceptor 3

Encoded byP2RX3P56373Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
2
Approved medicines
Open Targets target-level
25
Clinical trials
Small-molecule tractable
Druggability
Advanced Clinical

Protein at a glance

Biological role

ATP-gated monoatomic cation channel

Strongest disease association

Venous Thrombosis

Via encoding gene P2RX3 · Genetic evidence · score 0.36

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

Extracellular ATP-activated non-selective cation channel.

View complete UniProt function annotation

Extracellular ATP-activated non-selective cation channel (PubMed:10440098, PubMed:27626375, PubMed:29674445, PubMed:31232692). Plays particularly important role in sensory neurons where its activation is critical for gustatory, nociceptive responses, visceral reflexes and sensory hypersensitization (By similarity)

Subcellular location

Cell membrane
Domains and Gene Ontology detail (18)

Gene Ontology

  • Caxon
  • Chippocampal mossy fiber to CA3 synapse
  • Cplasma membrane
  • Cpostsynapse
  • Creceptor complex
  • CSchaffer collateral - CA1 synapse
  • FATP binding
  • Fextracellularly ATP-gated monoatomic cation channel activity
  • Fmetal ion binding
  • Fpurinergic nucleotide receptor activity
  • Pcalcium ion transmembrane transport
  • Pcellular response to ATP

397 aa · 44 kDa

Biological roles

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

Synaptic signallingGOIon channel gatingGO
View supporting evidence

Synaptic signalling

  • ·hippocampal mossy fiber to CA3 synapse
  • ·postsynapse
  • ·Schaffer collateral - CA1 synapse
  • ·modulation of chemical synaptic transmission

Ion channel gating

  • ·extracellularly ATP-gated monoatomic cation channel activity
  • ·calcium ion transmembrane transport

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

Drugs targeting this protein

1

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.

Gefapixant
Narrow target profileApprovedAntagonist

P2X purinoceptor 3 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 P2RX3

Gene-level evidence surfaced through the gene P2RX3 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.

Venous Thrombosis
0.36Limited support

Genetic evidence dominant · Open Targets 0.22

Sleep Initiation and Maintenance Disorders
0.35Limited support

Genetic evidence dominant · Open Targets 0.21

Arrhythmias, Cardiac
0.21Preliminary

Genetic evidence dominant · Open Targets 0.13

Atrial Fibrillation
0.14Preliminary

Genetic evidence dominant · Open Targets 0.08

Blood Coagulation Disorders
0.14Preliminary

Genetic evidence dominant · Open Targets 0.08

View evidence synthesis (5)
Venous ThrombosisLimited support
0.36
agreement 0.240.48
Genetic100%

Open Targets aggregate 0.22 · 1 independent evidence family

Sleep Initiation and Maintenance DisordersLimited support
0.35
agreement 0.230.47
Genetic100%

Open Targets aggregate 0.21 · 1 independent evidence family

Arrhythmias, CardiacPreliminary
0.21
agreement 0.090.33
Genetic100%

Open Targets aggregate 0.13 · 1 independent evidence family

Atrial FibrillationPreliminary
0.14
agreement 0.000.28
Genetic96%Literature4%

Open Targets aggregate 0.08 · 2 independent evidence families

Blood Coagulation DisordersPreliminary
0.14
agreement 0.010.26
Genetic100%

Open Targets aggregate 0.08 · 1 independent evidence family

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
Venous Thrombosis0.22
Sleep Initiation and Maintenance Disorders0.21
Arrhythmias, Cardiac0.13
Endometriosis0.09
Atrial Fibrillation0.08
Blood Coagulation Disorders0.08
Atrial Flutter0.08

Drug development

3 compounds recorded · 2 approved · 1 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph: these count different sets and are not a subset relation.

View all recorded compounds (3)
GEFAPIXANT CITRATEApproval
CAMLIPIXANTPhase 3
GEFAPIXANTApproval

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

Advanced Clinical 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.

View underlying tractability evidence (9)
SM · Advanced ClinicalSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · Database UbiquitinationPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

increased urinary sodium excretionLynch et al. (2017)increased urine excretionLynch et al. (2017)decreased convulsionsLynch et al. (2017)decreased inflammationLynch et al. (2017)hemolysisLynch et al. (2017)increased painLynch et al. (2017)neurodegenerationLynch et al. (2017)decreased painLynch 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

25

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 (21)

ClinicalTrials.gov via the drug-target graph.

What's happening now

6

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets 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. New publication2024-12-01
    Gefapixant as a P2X3 receptor antagonist treatment for obstructive sleep apnea: a randomized controlled trial.

    Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine · 2024 · 3 citations · Europe PMC · via Gefapixant

  2. New publication2024-09-12
    Randomized, controlled, proof-of-concept trial of gefapixant for endometriosis-related pain.

    Fertility and sterility · 2025 · 6 citations · Europe PMC · via Gefapixant

  3. New publication2024-08-30
    Efficacy and safety of gefapixant in women with chronic cough and cough-induced stress urinary incontinence: a phase 3b, randomised, multicentre, double-blind, placebo-controlled trial.

    The Lancet. Respiratory medicine · 2024 · 2 citations · Europe PMC · via Gefapixant

  4. Regulatory approval2023-09-15

    Approval: Lyfnua (EMA)

    ema · regulatory · ema · via Gefapixant

  5. New publication2023-03-06
    The Efficacy and Safety of Gefapixant in a Phase 3b Trial of Patients with Recent-Onset Chronic Cough.

    Lung · 2023 · 25 citations · Europe PMC · via Gefapixant

  6. New publication2020-03-20
    Gefapixant in two randomised dose-escalation studies in chronic cough.

    The European respiratory journal · 2020 · 98 citations · Europe PMC · via Gefapixant

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.