DRD2

Dopamine receptor D2

Score: 0.694 Price: $0.69 High Druggability Status: active Wiki: DRD2
🧠 Neurodegeneration
HYPOTHESES
1
PAPERS
18
KG EDGES
200
DEBATES
0

3D Protein Structure

🧬 DRD2 — PDB 6CM4 Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability
High
Score: 0.90
Clinical Stage
Approved
Target Class
Gpcr
Safety
0.60
Druggability Analysis
Drug Development1.00
Structural Tractability0.85
Target Class0.85
Safety Profile0.60
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 ✓
6CM46LUQ6VMS7DFP7JVR+5 more
UniProt: F8VUV1
Binding Pocket Analysis:

7TM binding cavity, extracellular loops

🧬 3D Protein Structure

🧬 DRD2 — PDB 6CM4 Click to expand interactive 3D viewer

Experimental structure from RCSB PDB | Powered by Mol* | Rotate: click+drag | Zoom: scroll

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.

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 (6)

Relevant trials from ClinicalTrials.gov

Active
2
Completed
2
Total Enrollment
4,629
By Phase
NA: 1 · PHASE1: 2 · PHASE2: 1 · Unknown: 2
A Pharmacodynamics and Safety Study of DSP-9632P in Patients With Levodopa-Induced Dyskinesia in Parkinson's Disease Completed
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
Use and Misuse of Domperidone in Parkinson's Disease in France - Observational Terminated
Unknown NCT04653584 n=1579
Parkinson Disease
Sponsor: Assistance Publique - Hôpitaux de Paris | Started: 2021-01-01
Domperidone as a Treatment for Dopamine Agonist-induced Peripheral Edema in Patients With Parkinson's Disease Terminated
PHASE2 NCT00305331 n=25
Parkinson's Disease, Peripheral Edema
Interventions: Domperidone (drug)
Sponsor: University Health Network, Toronto | Started: 2006-03
Use and Misuse of Domperidone in Parkinson's Disease in France - Dump Investigation Completed
Unknown NCT03837067 n=2300
Parkinson's Disease
Sponsor: Assistance Publique - Hôpitaux de Paris | Started: 2018-07-17
Efficacy of a Prediction Model-based Algorithm to PREVENT Drug-induced Impulse Control Disorders in Parkinson's Disease Not Yet Recruiting
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
Aerobic Exercise After Traumatic Brain Injury Enrolling By Invitation
PHASE1 NCT05786729 n=190
Traumatic Brain Injury
Interventions: Aerobic Exercise (AER), Rehabilitation
Sponsor: Centre for Neuro Skills | Started: 2022-01-18

Linked Hypotheses (0)

No linked hypotheses

Linked Experiments (0)

No linked experiments

Scoring Dimensions

Portfolio 0.71 (25%) Druggability 0.90 (20%) Evidence 0.58 (20%) Safety 0.60 (15%) Competitive 0.40 (10%) Connectivity 0.90 (10%) 0.694 composite

Knowledge Graph (20)

activates (1)

DRD2 JUN

associated with (8)

DRD2 neurodegeneration
DRD2 CYP3A4
DRD2 SNCA
DRD2 SLC6A2
DRD2 SLC6A3
...and 3 more

co discussed (9)

DRD2 CHR2
DRD2 CLOCK
DRD2 CRH
DRD2 BDNF
DRD2 SNCA
...and 4 more

interacts with (1)

DRD2 SNCA

participates in (1)

DRD2 dopaminergic_circuits

Debate History (0)

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