BRD4

Bromodomain-containing protein 4

Score: 0.453 Price: $0.45 Low Druggability Status: active Wiki: BRD4 (Bromodomain-Containing Protein 4)

HYPOTHESES

PAPERS

KG EDGES

DEBATES

3D Protein Structure

🧬 BRD4 — PDB 2OSS Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability

Low

Score: 0.40

Clinical Stage

Phase II

Target Class

Epigenetic Regulator

Safety

0.62

Druggability Analysis

Drug Development0.30

Structural Tractability0.70

Target Class0.70

Safety Profile0.62

Key Metrics

PDB Structures:

Known Drugs:

Approved:

In Clinical Trials:

Drug Pipeline (2 compounds)

Mechanism: BRD4 inhibition reduces neuroinflammatory super-enhancer activity while biased BRD4 modulators can selectively restore neuroprotective gene expression

Drug Pipeline (2 compounds)

Known Drugs:

JQ1 (Preclinical (tool compound))

OTX015 (Clinical (oncology))

Structural Data:

PDB (5) ✓AlphaFold ✓Cryo-EM —

2OSS 2YEL 3MUK 3P5O 4BJX

UniProt: O60885

🧬 3D Protein Structure

🧬 BRD4 — PDB 2OSS Click to expand interactive 3D viewer

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

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 (5)

Relevant trials from ClinicalTrials.gov

Active

Completed

Total Enrollment

213

By Phase

PHASE1: 4 · PHASE2: 1

A Dose-Finding Study of Birabresib (MK-8628), a Small Molecule Inhibitor of the Bromodomain and Extra-Terminal (BET) Pro Completed

PHASE1 NCT02259114 n=47

NUT Midline Carcinoma, Triple Negative Breast Cancer, Non-small Cell Lung Cancer With Rearrang

Interventions: Birabresib

Sponsor: Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, N | Started: 2014-10-23

A Dose-finding Study of the Bromodomain (Brd) Inhibitor OTX015/ Birabresib (MK-8628) in Hematologic Malignancies (MK-862 Completed

PHASE1 NCT01713582 n=141

Acute Myeloid Leukemia, Diffuse Large B-cell Lymphoma, Acute Lymphoblastic Leukemia

Interventions: OTX015/Birabresib

Sponsor: Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, N | Started: 2012-12-14

A Dose-finding Study of Birabresib (MK-8628) in Participants With Recurrent Glioblastoma Multiforme (MK-8628-002) Terminated

PHASE2 NCT02296476 n=12

Glioblastoma Multiforme

Interventions: Birabresib

Sponsor: Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, N | Started: 2014-10-29

A Dose Exploration Study With Birabresib (MK-8628) in Participants With Selected Advanced Solid Tumors (MK-8628-006) Terminated

PHASE1 NCT02698176 n=13

NUT Midline Carcinoma (NMC), Triple Negative Breast Cancer (TNBC), Non-small Cell Lung Cancer (NSCLC)

Interventions: Birabresib

Sponsor: Merck Sharp & Dohme LLC | Started: 2016-05-04

A Study Assessing tOTX015 in Combination With Azacitidine (AZA) or AZA Single Agent in Patients With Newly-diagnosed Acu Withdrawn

PHASE1 NCT02303782

Acute Myeloid Leukemia

Interventions: OTX015, Vidaza (azacitidine)

Sponsor: Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, N | Started: 2015-01

Linked Hypotheses (1)

Chromatin Accessibility Restoration via BRD4 Modulation0.768

Linked Experiments (0)

No linked experiments

Scoring Dimensions

Knowledge Graph (20)

activates (8)

GSDMD→BRD4NLRP3→BRD4SOX2→BRD4LIFR→BRD4LIF→BRD4

▸ Show 3 more

STAT3→BRD4EP300→BRD4SMAD3→BRD4

Debate History (1)

Should BRD4 (Bromodomain-containing protein 4) be prioritized as a therapeutic t2026-04-22

BRD4

3D Protein Structure

Druggability & Clinical Context

🧬 3D Protein Structure

3D Protein Structure

Clinical Trials (5)

Linked Hypotheses (1)

Linked Experiments (0)

Scoring Dimensions

Knowledge Graph (20)

activates (8)

associated with (4)

biomarker for (3)

inhibits (1)

interacts with (1)

modifies (1)

regulates (1)

therapeutic target (1)

Debate History (1)