PMID

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Article Title

Organization

Non-kinase targets of protein kinase inhibitors.

The University Of Sydney

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

Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.

Zhejiang University

Discovery of a Series of 5,11-Dihydro-6

Dana-Farber Cancer Institute

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.

Boehringer Ingelheim Rcv

Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.

China Pharmaceutical University

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

Constellation Pharmaceuticals

4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).

Albert-Ludwigs-University Of Freiburg

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

Genentech

Dihydropteridinone Inhibitors of BRD4.

Dart Neuroscience

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.

Guangzhou Institutes Of Biomedicine And Health

KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.

University Of Freiburg

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

The University Of Texas M.D. Anderson Cancer Center

A phenotypic drug discovery study on thienodiazepine derivatives as inhibitors of T cell proliferation induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor.

Mitsubishi Tanabe Pharma

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.

Centre National de la Recherche Scientifique/INSERM/ULP

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.

University Of Dundee

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

University Of Z£Rich

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

Glaxosmithkline

BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.

University Of Maryland

Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.

The University Of Tokyo

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.

Glaxosmithkline

Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.

Amri

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.

Glaxosmithkline

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

University Of Michigan

Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization.

Shanghai Institute Of Materia Medica

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.

Glaxosmithkline

Biased multicomponent reactions to develop novel bromodomain inhibitors.

Dana-Farber Institute

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

Glaxosmithkline

Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking.

University Of Zurich

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

Icahn School Of Medicine At Mount Sinai

Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.

The Institute Of Cancer Research

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.

Glaxosmithkline

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

Constellation Pharmaceuticals

Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.

Chinese Academy Of Sciences

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

University Of Oxford

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

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

Pfizer

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.

University Of Oxford

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

Glaxosmithkline

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

Glaxosmithkline

Peptoid ligands that bind selectively to phosphoproteins.

The Scripps Research Institute

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

Glaxosmithkline

Bromodomains: are readers right for epigenetic therapy?

TBA

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

Japan Science And Technology Agency

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.

University Of Oxford

Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.

Glaxosmithkline

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

University Of Oxford

Discovery of thiophene inhibitors of polo-like kinase.

Gsk

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

Antibacterial agent discovery using thymidylate synthase biolibrary screening.

Unimore

Influence of side-chain structure of aliphatic amino acids on binding to isoleucyl-tRNA synthetase from Escherichia coli MRE 600.

Gesellschaft Fur Molekularbiolische Forschung Mbh

Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action.

Pharmacia

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase i

Bristol-Myers Squibb

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

Hawaii Biotech

Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives.

Biocryst Pharmaceuticals

Use of binding enthalpy to drive an allosteric transition.

University Of Maryland

DNA gyrase interaction with coumarin-based inhibitors: the role of the hydroxybenzoate isopentenyl moiety and the 5'-methyl group of the noviose.

Umr Cnrs 6032