P2RX7

P2X purinoreceptor 7

Score: 0.682 Price: $0.68 High Druggability Status: active Wiki: P2RX7
🧠 Neurodegeneration
HYPOTHESES
1
PAPERS
29
KG EDGES
155
DEBATES
1

3D Protein Structure

🧬 P2RX7 — PDB 5U1L Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability
High
Score: 0.80
Clinical Stage
Phase II
Target Class
Ion Channel
Safety
0.60
Druggability Analysis
Drug Development0.30
Structural Tractability0.85
Target Class0.85
Safety Profile0.60
Key Metrics
PDB Structures:
24
Known Drugs:
2
Approved:
0
In Clinical Trials:
0
Drug Pipeline (2 compounds)
2 Preclinical
Druggability Rationale: P2X7 is highly druggable due to its well-characterized ATP-binding pocket, extensive structural data (24 PDB structures with sub-angstrom resolution), and proven clinical precedent with multiple selective antagonists in Phase 2 trials. The ion channel architecture provides a clearly defined ligand-binding site, and the high druggability score (0.80) reflects established chemical matter and successful target validation in inflammatory and neuropsychiatric indications.
Mechanism: Selective P2X7 receptor antagonists blocking ATP-gated ion channel
Drug Pipeline (2 compounds)
2 Preclinical
Known Drugs:
A-804598 (investigational) — inflammatory diseases
JNJ-54175446 (investigational) — depression
Structural Data:
PDB (24) ✓AlphaFold ✓Cryo-EM —
5U1L5U1U5U1V5U1W5U1X+19 more
UniProt: Q0IJ51

Selectivity & Safety Considerations

P2X7 selectivity over closely related P2X family members (P2X1-P2X6) is achievable but requires careful structural optimization, as antagonists may show cross-reactivity with other purinergic receptors. The unique C-terminal domain and specific ATP-binding pocket geometry of P2X7 provide selectivity advantages, though off-target effects on other ATP-sensing proteins should be monitored during development.

3D Protein Structure

PDB: Open in RCSB AlphaFold model

Interactive 3D viewer powered by RCSB PDB / Mol*. Use mouse to rotate, scroll to zoom.

Clinical Trials (8)

Relevant trials from ClinicalTrials.gov

Active
1
Completed
7
Total Enrollment
860
By Phase
NA: 5 · PHASE1: 1 · PHASE2: 1 · Unknown: 1
Anger Control Training for Youth With Tourette Syndrome Completed
NA NCT00486551 n=26
Tourette Syndrome, Chronic Tic Disorder, Oppositional Defiant Disorder
Interventions: Anger control training
Sponsor: Yale University | Started: 2001-08
Adaptive vs. Continuous Subthalamic Nucleus Deep Brain Stimulation in Parkinson's Disease Recruiting
NA NCT06909045 n=130
Deep Brain Stimulation, Parkinson Disease
Interventions: Adaptive DBS, Continue DBS
Sponsor: Academisch Medisch Centrum - Universiteit van Amsterdam (AMC | Started: 2026-01-27
Expiratory Muscle Training in Patients With Parkinson's Disease Completed
PHASE1 NCT00843739 n=90
Parkinson's Disease
Interventions: EMST - Active Treatment, sham EMST
Sponsor: University of Florida | Started: 2004-01
Study of the Follow-up of Stroke Treated With Anticoagulants Completed
Unknown NCT03292575 n=441
Stroke
Interventions: Anticoagulants
Sponsor: Centre Hospitalier Universitaire Dijon | Started: 2016-01
Early Detection and Prevention of Mild Cognitive Impairment Due to Cerebrovascular Disease Completed
NA NCT01924312 n=80
Cerebrovascular Disease, Mild Cognitive Impairment
Interventions: Heart Health Intervention
Sponsor: Gregory Jicha, 323-5550 | Started: 2013-05
Effects of Modern Board Games on Well Being in Older Adults Completed
NA NCT06306365 n=35
Executive Functions
Interventions: Modern board game-based learning
Sponsor: European University Miguel de Cervantes | Started: 2024-02-07
Treatment of Alzheimer's and Dementia With the Metabolism, Infections, Nutrition, Drug Elimination (MIND) Protocol Completed
NA NCT02260167 n=25
Alzheimer's Disease, Dementia
Interventions: A mix of natural treatments and medicati
Sponsor: Practitioners Alliance Network | Started: 2014-09
A Phase 2 Study to Evaluate Safety of Long-term AL001 Dosing in Frontotemporal Dementia (FTD) Patients (INFRONT-2) Completed
PHASE2 NCT03987295 n=33
Frontotemporal Dementia
Interventions: AL001
Sponsor: Alector Inc. | Started: 2019-09-27

Linked Hypotheses (1)

P2RX7-Mediated Exosome Secretion Blockade0.552

Linked Experiments (1)

P2RX7 variant rs1718119 association with glucose homeostasis in Botnia cohort0.900

Scoring Dimensions

Portfolio 0.70 (25%) Druggability 0.80 (20%) Evidence 0.56 (20%) Safety 0.60 (15%) Competitive 0.55 (10%) Connectivity 0.90 (10%) 0.682 composite

Knowledge Graph (20)

associated with (1)

P2RX7neurodegeneration

co discussed (17)

BMAL1P2RX7HK2P2RX7MIRO1P2RX7P2RY1P2RX7SOAT1P2RX7
▸ Show 12 more
KCNK2P2RX7TET2P2RX7PIEZO1P2RX7P2RX7DGAT1P2RX7C3NTN1P2RX7HSPG2P2RX7P2RY12P2RX7P2RX7AQP4P2RX7EPHB4P2RX7SMPD1P2RX7C1QA

interacts with (2)

P2RY1P2RX7P2RX7P2RY1

Debate History (1)

Should P2RX7 (P2X purinoreceptor 7) be prioritized as a therapeutic target for n2026-04-21