Druggability & Clinical Context
Druggability
High
Score: 0.90
Druggability Analysis
Structural Tractability0.85
Key Metrics
PDB Structures:
10
Known Drugs:
14
Approved:
14
In Clinical Trials:
0
Drug Pipeline (14 compounds)
14 Approved
Therapeutic Areas:CNS/Neuroscience Cardiovascular Pain Neurodegeneration
Druggability Rationale: DRD2 represents a high-druggability target with extensive structural characterization and multiple clinically approved small molecule modulators, indicating robust pharmaceutical tractability. The availability of high-resolution structural data (best resolution 2.19Å) and multiple existing antagonists/agonists like haloperidol and risperidone provide a strong foundation for targeted neurodegeneration drug discovery. The extensive clinical trial history and known pharmacological profiles suggest that DRD2-targeted interventions could be strategically valuable for neurodegenerative conditions with dopaminergic dysregulation.
Mechanism: Small molecule agonist or antagonist modulating dopamine signaling
Drug Pipeline (14 compounds)
14 Approved
Known Drugs:haloperidol (approved) — schizophrenia, Parkinson's disease
risperidone (approved) — schizophrenia, bipolar disorder
pramipexole (approved) — Parkinson's disease
ropinirole (approved) — Parkinson's disease
CHEMBL2359670 (approved)
CHEMBL3989478 (approved)
CHEMBL1200951 (approved)
CHEMBL567 (approved)
Structural Data:PDB (10) ✓AlphaFold ✓Cryo-EM ✓
Binding Pocket Analysis:7TM binding cavity, extracellular loops
Selectivity & Safety Considerations
GPCR selectivity should be assessed against related receptor subtypes. Off-target GPCR activity (especially at hERG, muscarinic, and adrenergic receptors) is a common source of clinical adverse effects.
Clinical Trials (6)
Relevant trials from ClinicalTrials.gov
By Phase
NA: 1 · PHASE1: 2 · PHASE2: 1 · Unknown: 2
PHASE1
NCT05435729
n=7
Levodopa-induced Dyskinesia, Parkinson's Disease
Interventions: DSP-9632P 27.5 mg, DSP-9632P 82.5 mg, Placebo
Sponsor: Sumitomo Pharma Co., Ltd. | Started: 2022-05-31
Unknown
NCT04653584
n=1579
Parkinson Disease
Sponsor: Assistance Publique - Hôpitaux de Paris | Started: 2021-01-01
PHASE2
NCT00305331
n=25
Parkinson's Disease, Peripheral Edema
Interventions: Domperidone (drug)
Sponsor: University Health Network, Toronto | Started: 2006-03
Unknown
NCT03837067
n=2300
Parkinson's Disease
Sponsor: Assistance Publique - Hôpitaux de Paris | Started: 2018-07-17
NA
NCT07505394
n=528
Parkinson Disease, Impulse Control Disorder
Interventions: Algorithm-guided group, Standard of Care (SoC) group
Sponsor: Assistance Publique - Hôpitaux de Paris | Started: 2026-06-01
PHASE1
NCT05786729
n=190
Traumatic Brain Injury
Interventions: Aerobic Exercise (AER), Rehabilitation
Sponsor: Centre for Neuro Skills | Started: 2022-01-18