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78 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28650658 54 Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.EBI Shandong University
28375629 84 Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain.EBI Pfizer
28347667 35 Discovery of novel BRD4 inhibitors by high-throughput screening, crystallography, and cell-based assays.EBI Nanchang University
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University Of Sydney
27994766 28 Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.EBI University Of Dundee
27682507 167 Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.EBI Genentech
27673482 4 Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.EBI Ludwig-Maximilians-Universit£T M£Nchen
27266999 16 Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.EBI Zhejiang University
27774127 75 Discovery of a Series of 5,11-Dihydro-6EBI Dana-Farber Cancer Institute
26914985 124 Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.EBI Boehringer Ingelheim Rcv
27142751 22 Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.EBI China Pharmaceutical University
27190605 77 Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).EBI Constellation Pharmaceuticals
26731611 30 4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).EBI Albert-Ludwigs-University Of Freiburg
26572217 60 Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.EBI Genentech
26985285 4 Dihydropteridinone Inhibitors of BRD4.EBI Dart Neuroscience
26731490 99 Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.EBI Guangzhou Institutes Of Biomedicine And Health
26701186 50 KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.EBI University Of Freiburg
26061247 71 Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.EBI The University Of Texas M.D. Anderson Cancer Center
26869194 1 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.EBI Mitsubishi Tanabe Pharma
26735842 27 Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.EBI 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.EBI University Of Dundee
26043365 41 Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain.EBI University Of Z£Rich
25799074 65 Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.EBI Glaxosmithkline
26191363 29 BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.EBI University Of Maryland
25678016 15 Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.EBI The University Of Tokyo
26230603 176 Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.EBI Glaxosmithkline
26022843 39 Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.EBI Amri
26155854 125 Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.EBI Glaxosmithkline
26080064 141 Structure-Based Design of¿-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.EBI University Of Michigan
25559428 38 Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization.EBI Shanghai Institute Of Materia Medica
25408830 43 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.EBI Glaxosmithkline
25314271 44 Biased multicomponent reactions to develop novel bromodomain inhibitors.EBI Dana-Farber Institute
25249180 146 The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.EBI Glaxosmithkline
24767840 2 Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking.EBI University Of Zurich
24144283 100 Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.EBI Icahn School Of Medicine At Mount Sinai
24090311 12 Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.EBI 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.EBI Glaxosmithkline
24900758 44 Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.EBI Constellation Pharmaceuticals
23530754 25 Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.EBI Chinese Academy Of Sciences
23517011 29 Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.EBI University Of Oxford
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.EBI Cellzome
23095041 16 Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.EBI Pfizer
22924434 4 Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.EBI University Of Oxford
22437115 66 Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).EBI Glaxosmithkline
22136469 148 Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.EBI Glaxosmithkline
21742492 1 Peptoid ligands that bind selectively to phosphoproteins.EBI The Scripps Research Institute
21568322 16 Discovery and characterization of small molecule inhibitors of the BET family bromodomains.EBI Glaxosmithkline
24900532 1 Bromodomains: are readers right for epigenetic therapy?EBI TBA
22316554 22 Development of live-cell imaging probes for monitoring histone modifications.EBI Japan Science And Technology Agency
22137933 6 Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.EBI University Of Oxford
22136404 9 Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.EBI Glaxosmithkline
21851057 30 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.EBI University Of Oxford
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.EBI Abbvie
28910100 2 Direct NMR Probing of Hydration Shells of Protein Ligand Interfaces and Its Application to Drug Design.EBI University Of Vienna
28535045 64 BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.EBI University Of Minnesota
19117760 19 Structure-based virtual screening for novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase and their experimental evaluation.BDB Northern Kentucky University
19781947 5 Glucose-based spiro-isoxazolines: a new family of potent glycogen phosphorylase inhibitors.BDB Universite De Lyon
16028929 17 Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL.BDB Yale University
19097784 55 Discovery of thiophene inhibitors of polo-like kinase.BDB Gsk
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.BDB Gsk
17004711 85 Antibacterial agent discovery using thymidylate synthase biolibrary screening.BDB Unimore
782880 21 Influence of side-chain structure of aliphatic amino acids on binding to isoleucyl-tRNA synthetase from Escherichia coli MRE 600.BDB Gesellschaft Fur Molekularbiolische Forschung Mbh
11341829 9 Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action.BDB Pharmacia
17154512 78 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 iBDB Bristol-Myers Squibb
16386899 13 Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.BDB Hawaii Biotech
15055992 77 Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives.BDB Biocryst Pharmaceuticals
15723556 4 Use of binding enthalpy to drive an allosteric transition.BDB University Of Maryland
12044152 4 DNA gyrase interaction with coumarin-based inhibitors: the role of the hydroxybenzoate isopentenyl moiety and the 5'-methyl group of the noviose.BDB Umr Cnrs 6032