Druggability & Clinical Context
Druggability
Low
Score: 0.38
Druggability Analysis
Structural Tractability0.30
Key Metrics
PDB Structures:
0
Known Drugs:
2
Approved:
1
In Clinical Trials:
0
Drug Pipeline (2 compounds)
1 Approved ยท 1 Preclinical
Therapeutic Areas:Metabolic Disease Oncology Rare Disease Respiratory
Druggability Rationale: This enzyme has moderate druggability. The active site may be partially accessible, or substrate mimicry approaches may face selectivity challenges against related family members. AlphaFold predicted structure available for computational screening. 1 approved drug(s) validate this target pharmacologically.
Mechanism: Small molecule inhibitors targeting the active site iron and substrate binding
Drug Pipeline (2 compounds)
1 Approved ยท 1 Preclinical
Known Drugs:Zileuton (approved) โ Asthma
PD146176 (preclinical) โ Inflammation
Structural Data:PDB โAlphaFold โCryo-EM โ
Binding Pocket Analysis:Catalytic residues, substrate-binding cleft
Clinical Trials (7)
Relevant trials from ClinicalTrials.gov
By Phase
PHASE1: 3 ยท PHASE2: 2 ยท PHASE4: 2
PHASE4
NCT01805687
n=25
Asthma
Interventions: Zileuton extended release
Sponsor: Cornerstone Therapeutics Inc. | Started: 2013-03
PHASE4
NCT00575861
n=19
Asthma
Interventions: zileuton
Sponsor: Gelb, Arthur F., M.D. | Started: 2005-09
PHASE2
NCT00723021
n=15
Asthma
Interventions: PF-04191834, PF-04191834, PF-04191834
Sponsor: Pfizer | Started: 2008-07
PHASE1
NCT00299065
n=60
Asthma
Interventions: Zileuton injection
Sponsor: Critical Therapeutics | Started: 2006-01
PHASE1
NCT01136941
n=9
Sickle Cell Disease
Interventions: Zileuton
Sponsor: Children's Hospital Medical Center, Cincinnati | Started: 2010-09
PHASE1
NCT01021215
n=84
Tobacco Use Disorder
Interventions: Zileuton, Celecoxib, laboratory biomarker analysis
Sponsor: National Cancer Institute (NCI) | Started: 2010-05
PHASE2
NCT00098358
n=90
Acne Vulgaris
Interventions: Zileuton
Sponsor: Critical Therapeutics | Started: 2004-11