The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
| 26914985 |
124 |
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. |
Boehringer Ingelheim Rcv |
| 26735842 |
27 |
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 |
| 26367539 |
22 |
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 |
| 26043365 |
41 |
Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain. |
University of Z£Rich |
| 26230603 |
176 |
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. |
Glaxosmithkline |
| 26022843 |
39 |
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design. |
Amri |
| 26155854 |
125 |
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors. |
Glaxosmithkline |
| 26080064 |
141 |
Structure-Based Design of¿-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
University of Michigan |
| 25559428 |
38 |
Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization. |
Shanghai Institute of Materia Medica |
| 25249180 |
146 |
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. |
Glaxosmithkline |
| 24090311 |
12 |
Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening. |
The Institute of Cancer Research |
| 24015967 |
71 |
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. |
Glaxosmithkline |
| 22726925 |
216 |
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 |
| 22924434 |
4 |
Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. |
University of Oxford |
| 22437115 |
66 |
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). |
Glaxosmithkline |
| 22136469 |
148 |
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides. |
Glaxosmithkline |
| 21568322 |
16 |
Discovery and characterization of small molecule inhibitors of the BET family bromodomains. |
Glaxosmithkline |
| 22316554 |
22 |
Development of live-cell imaging probes for monitoring histone modifications. |
Japan Science and Technology Agency |
| 22136404 |
9 |
Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery. |
Glaxosmithkline |
| 21851057 |
30 |
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. |
University of Oxford |
| 27757418 |
27 |
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. |
University of Oxford |
| 32787145 |
72 |
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype. |
Gsk |
| 32702236 |
120 |
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor. |
Glaxosmithkline |
| 32453591 |
70 |
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
University of Illinois At Chicago |
| 27528113 |
117 |
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153). |
Astrazeneca |
| 32255647 |
73 |
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. |
University of Texas Medical Branch |
| 32208600 |
102 |
Discovery of 8-Methyl-pyrrolo[1,2- |
Chinese Academy of Sciences |
| 30019901 |
62 |
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. |
TBA |
| 31461688 |
108 |
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins. |
University of Chinese Academy of Sciences |
| 31789032 |
106 |
Discovery of Benzo[ |
China Pharmaceutical University |
| 32324999 |
110 |
Discovery of |
Abbvie |
| 32153186 |
118 |
Discovery of Thieno[2,3- |
Sichuan University and Collaborative Innovation Center of Biotherapy |
| 30606676 |
83 |
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor. |
Gilead Sciences |
| 31398032 |
113 |
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification. |
Cellzome |
| 30253095 |
82 |
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
University of Minnesota |
| 30268702 |
66 |
Discovery and lead identification of quinazoline-based BRD4 inhibitors. |
National Institutes of Health |
| 28339196 |
48 |
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 |
| 29678460 |
71 |
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors. |
Abbvie |
| 29656650 |
151 |
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. |
University of Strathclyde |
| 29169673 |
115 |
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. |
Wuxi Apptec |
| 28463487 |
185 |
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 |
| 29170024 |
45 |
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. |
St. Jude Children'S Research Hospital |
| 29649741 |
56 |
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. |
University of Texas Medical Branch |
| 30015487 |
96 |
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor. |
TBA |
| 29259751 |
142 |
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. |
Walter and Eliza Hall Institute of Medical Research |
| 28195723 |
94 |
Drug Discovery Targeting Bromodomain-Containing Protein 4. |
University of Texas Medical Branch |
| 28268136 |
130 |
Methylpyrrole inhibitors of BET bromodomains. |
Abbvie |
| 29172540 |
65 |
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 |
| 28949521 |
88 |
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 |
| 1321744 |
14 |
Multiple histamine receptors: properties and functional characteristics. |
Queen'S Medical Centre |
| 19138846 |
23 |
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 |
| 16386899 |
13 |
Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors. |
Hawaii Biotech |
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