PMID

Data

Article Title

Organization

Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.

University of Dundee

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.

Genentech

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.

Ludwig-Maximilians-Universit£T M£Nchen

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Constellation Pharmaceuticals

The"Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.

University of Z£Rich

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.

Genentech

KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.

University of Freiburg

Discovery of CREBBP Bromodomain Inhibitors by High-Throughput Docking and Hit Optimization Guided by Molecular Dynamics.

University of Z£Rich

Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain.

University of Z£Rich

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.

Shandong University

Structure-Based Design of¿-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.

University of Michigan

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

Universit£

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Glaxosmithkline

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.

Icahn School of Medicine At Mount Sinai

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

University of Oxford

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Pfizer

Discovery and characterization of small molecule inhibitors of the BET family bromodomains.

Glaxosmithkline

Development of live-cell imaging probes for monitoring histone modifications.

Japan Science and Technology Agency

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.

University of Oxford

Rapid identification of improved protein ligands using peptoid microarrays.

University of Texas Southwestern Medical Center

Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy.

Gsk

Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.

Kochi Medical School

Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.

Hawaii Biotech