Druggability & Clinical Context
Druggability
Low
Score: 0.42
Druggability Analysis
Structural Tractability0.85
Key Metrics
PDB Structures:
17
Known Drugs:
1
Approved:
0
In Clinical Trials:
0
Drug Pipeline (1 compounds)
Druggability Rationale: PIEZO1 demonstrates moderate druggability (0.55 score) supported by extensive structural data (17 PDB structures, cryo-EM, 3.1Å resolution) and proof-of-concept with Yoda1 tool compound, though the large transmembrane architecture and mechanosensitive nature present challenges for small molecule modulation. The ion channel class typically exhibits lower success rates in drug development, but PIEZO1's well-characterized structural features and established modulatory pathways support continued therapeutic development.
Mechanism: Small molecule modulator of mechanosensitive ion channel activity
Drug Pipeline (1 compounds)
Known Drugs:Yoda1 (tool_compound) — research
Structural Data:PDB (17) ✓AlphaFold ✓Cryo-EM ✓
Selectivity & Safety Considerations
PIEZO1 selectivity versus PIEZO2 (the primary isoform concern) will be critical given their overlapping tissue expression and mechanosensing functions; achieving isoform-selective modulation is challenging due to high sequence homology. Off-target effects on other ion channels and mechanotransduction pathways require careful profiling given PIEZO1's broad physiological roles in multiple tissue types.
Clinical Trials (5)
Relevant trials from ClinicalTrials.gov
By Phase
NA: 3 · Unknown: 2
NA
NCT06892171
n=20
Xerocytosis, Phenotype, Genotype
Interventions: Blood sample
Sponsor: Centre Hospitalier Universitaire, Amiens | Started: 2025-03-01
NA
NCT06459778
n=147
Infertility, Female, Intracytoplasmic Sperm Injections
Interventions: Piezo-ICSI
Sponsor: The Affiliated Nanjing Drum Tower Hospital of Nanjing Univer | Started: 2023-11-20
Unknown
NCT07236541
n=20
Lung Fibrosis
Interventions: No intervention; observational biospecim
Sponsor: Ming Zhong | Started: 2025-10-30
Unknown
NCT05253924
n=76
Preterm Birth, Parent-Child Relations, Epigenetics
Interventions: DNA methylation of target genes, EEG acquisition
Sponsor: IRCCS Eugenio Medea | Started: 2021-07-13
NA
NCT07477899
n=352
Adverse Childhood Experiences, Developmental Risk, Psychomotor Development Disorders
Interventions: Home visiting programme
Sponsor: IRCCS Eugenio Medea | Started: 2024-06-26