NR3C1

Glucocorticoid receptor

Score: 0.659 Price: $0.66 Medium Druggability Status: active Wiki: NR3C1

🧠 Neurodegeneration

HYPOTHESES

PAPERS

KG EDGES

202

DEBATES

3D Protein Structure

🧬 NR3C1 — PDB 1M2Z Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability

Medium

Score: 0.53

Clinical Stage

Approved

Target Class

Transcription Factor

Safety

0.40

Druggability Analysis

Drug Development1.00

Structural Tractability0.95

Target Class0.50

Safety Profile0.40

Key Metrics

PDB Structures:

Known Drugs:

Approved:

In Clinical Trials:

Drug Pipeline (13 compounds)

13 Approved

Therapeutic Areas:

Oncology Immunology Rare Disease

Druggability Rationale: NR3C1 (glucocorticoid receptor) demonstrates high druggability due to its well-characterized structural binding pocket and extensive crystallographic data, with 63 PDB structures enabling precise molecular targeting. The existing portfolio of selective glucocorticoid receptor modulators and antagonists like mifepristone and dexamethasone provides a strong translational framework for neurodegeneration drug discovery, particularly given the receptor's role in neuroinflammatory and stress response pathways.

Mechanism: Selective glucocorticoid receptor modulators (SRMs) or antagonists

Drug Pipeline (13 compounds)

13 Approved

Known Drugs:

Dexamethasone (approved) — inflammation, autoimmune diseases

Prednisolone (approved) — inflammation, autoimmune diseases

Mifepristone (approved) — Cushing's syndrome, abortion

CHEMBL635 (approved)

CHEMBL1200845 (approved)

CHEMBL1201173 (approved)

CHEMBL1201749 (approved)

CHEMBL632 (approved)

Structural Data:

PDB (63) ✓AlphaFold ✓Cryo-EM ✓

1LAT 3BQD 3CLD 3E7C 3FYL+58 more

UniProt: F1D8N4

Binding Pocket Analysis:

DNA-binding domain, dimerization interface

🧬 3D Protein Structure

🧬 NR3C1 — PDB 1M2Z Click to expand interactive 3D viewer

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

Selectivity & Safety Considerations

Selectivity among transcription factor family members is challenging but critical, as broad transcriptional disruption can cause widespread toxicity.

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

Completed

Total Enrollment

1,468

By Phase

PHASE1: 1 · PHASE2: 2 · PHASE3: 2 · PHASE4: 3

Ixazomib Plus Lenalidomide Plus Dexamethasone for Newly Diagnosed Myeloma Patients Active Not Recruiting

PHASE2 NCT03376672 n=120

Multiple Myeloma

Interventions: Ixazomib, Lenalidomide, Dexamethasone

Sponsor: Raija Silvennoinen | Started: 2018-05-31

Abraxane® With or Without Mifepristone for Advanced, Glucocorticoid Receptor-Positive, Triple-Negative Breast Cancer Active Not Recruiting

PHASE2 NCT02788981 n=29

Breast Cancer

Interventions: Mifepristone, Placebo, Nab-Paclitaxel

Sponsor: University of Chicago | Started: 2017-03-28

Rituximab + High-Dose Methylprednisolone Debulking Prior to Venetoclax for CLL & SLL Patients Active Not Recruiting

PHASE1 NCT04981912 n=4

Chronic Lymphocytic Leukemia or Small Ly

Interventions: HDMP + rituximab as a means of debulking

Sponsor: University of California, San Diego | Started: 2021-09-02

Evaluation of the Efficacy of Topical Ophthalmic Steroids in a Modified Conjunctival Allergen Challenge (CAC) Model Completed

PHASE4 NCT01534195 n=11

Allergic Conjunctivitis

Interventions: Prednisolone Sodium Phosphate Ophthalmic, Tears Naturale II Ophthalmic Solution

Sponsor: ORA, Inc. | Started: 2012-01

A Study of Sodium Carboxymethylcellulose for Post Cataract Surgery Dry Eye Symptoms Completed

PHASE4 NCT02028754 n=180

Dry Eye Syndromes, Cataract

Interventions: Sodium Carboxymethylcellulose, Levofloxacin, Prednisolone

Sponsor: Allergan | Started: 2011-07

A Pilot of an Outpatient Regimen of Medical Abortion With Mifepristone and Sublingual Misoprostol in the 11 and 12 Weeks Completed

PHASE4 NCT02720991 n=50

Abortion, 3 Months

Interventions: Mifepristone, Sublingual misoprostol

Sponsor: Gynuity Health Projects | Started: 2014-07

An Efficacy and Safety Study for Yondelis (Trabectedin) in Patients With Advanced Relapsed Ovarian Cancer Completed

PHASE3 NCT00113607 n=672

Ovarian Cancer

Interventions: Trabectedin, DOXIL, Dexamethasone

Sponsor: Johnson & Johnson Pharmaceutical Research & Development, L.L | Started: 2005-04

Bortezomib, Selinexor, and Dexamethasone in Patients With Multiple Myeloma Completed

PHASE3 NCT03110562 n=402

Multiple Myeloma

Interventions: Selinexor, Bortezomib, Dexamethasone

Sponsor: Karyopharm Therapeutics Inc | Started: 2017-05-24

Linked Hypotheses (0)

No linked hypotheses

Linked Experiments (0)

No linked experiments

Scoring Dimensions

Knowledge Graph (20)

...and 5 more

expressed in (3)

NR3C1 → ESR1

NR3C1 → TNF

NR3C1 → ESR2

inhibits (1)

NR3C1 → BDNF

interacts with (2)

NR3C1 → CRH

NR3C1 → TNFA

Debate History (0)

No debates yet

NR3C1

3D Protein Structure

Druggability & Clinical Context

🧬 3D Protein Structure

Selectivity & Safety Considerations

3D Protein Structure

Clinical Trials (8)

Linked Hypotheses (0)

Linked Experiments (0)

Scoring Dimensions

Knowledge Graph (20)

activates (1)

associated with (3)

co discussed (10)

expressed in (3)

inhibits (1)

interacts with (2)

Debate History (0)