40 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Boehringer Ingelheim Rcv
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
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
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
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 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
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
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
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 and lead identification of quinazoline-based BRD4 inhibitors.
National Institutes Of Health
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.
University Of Michigan Comprehensive Cancer Center
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Abbvie
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
University Of Strathclyde
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Wuxi Apptec
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.
University Of Michigan
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
St. Jude Children'S Research Hospital
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
University Of Texas Medical Branch
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.
TBA
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
Walter And Eliza Hall Institute Of Medical Research
Drug Discovery Targeting Bromodomain-Containing Protein 4.
University Of Texas Medical Branch
Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer.
Sichuan University
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Abbvie
Multiple histamine receptors: properties and functional characteristics.
Queen'S Medical Centre
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