The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28650658 |
54 |
Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization. |
Shandong University |
28375629 |
84 |
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain. |
Pfizer |
28347667 |
35 |
Discovery of novel BRD4 inhibitors by high-throughput screening, crystallography, and cell-based assays. |
Nanchang University |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University Of Sydney |
27994766 |
28 |
Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening. |
University Of Dundee |
27682507 |
167 |
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. |
Genentech |
27673482 |
4 |
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. |
Ludwig-Maximilians-Universit£T M£Nchen |
27266999 |
16 |
Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. |
Zhejiang University |
27774127 |
75 |
Discovery of a Series of 5,11-Dihydro-6 |
Dana-Farber Cancer Institute |
26914985 |
124 |
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. |
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. |
China Pharmaceutical University |
27190605 |
77 |
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). |
Constellation Pharmaceuticals |
26731611 |
30 |
4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1). |
Albert-Ludwigs-University Of Freiburg |
26572217 |
60 |
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
Genentech |
26985285 |
4 |
Dihydropteridinone Inhibitors of BRD4. |
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. |
Guangzhou Institutes Of Biomedicine And Health |
26701186 |
50 |
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases. |
University Of Freiburg |
26061247 |
71 |
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. |
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. |
Mitsubishi Tanabe Pharma |
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 |
25799074 |
65 |
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. |
Glaxosmithkline |
26191363 |
29 |
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. |
University Of Maryland |
25678016 |
15 |
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors. |
The University Of Tokyo |
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 |
25408830 |
43 |
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. |
Glaxosmithkline |
25314271 |
44 |
Biased multicomponent reactions to develop novel bromodomain inhibitors. |
Dana-Farber Institute |
25249180 |
146 |
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. |
Glaxosmithkline |
24767840 |
2 |
Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking. |
University Of Zurich |
24144283 |
100 |
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. |
Icahn School Of Medicine At Mount Sinai |
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 |
24900758 |
44 |
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors. |
Constellation Pharmaceuticals |
23530754 |
25 |
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain. |
Chinese Academy Of Sciences |
23517011 |
29 |
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. |
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. |
Cellzome |
23095041 |
16 |
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. |
Pfizer |
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 |
21742492 |
1 |
Peptoid ligands that bind selectively to phosphoproteins. |
The Scripps Research Institute |
21568322 |
16 |
Discovery and characterization of small molecule inhibitors of the BET family bromodomains. |
Glaxosmithkline |
24900532 |
1 |
Bromodomains: are readers right for epigenetic therapy? |
TBA |
22316554 |
22 |
Development of live-cell imaging probes for monitoring histone modifications. |
Japan Science And Technology Agency |
22137933 |
6 |
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. |
University Of Oxford |
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 |
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 |
28910100 |
2 |
Direct NMR Probing of Hydration Shells of Protein Ligand Interfaces and Its Application to Drug Design. |
University Of Vienna |
28535045 |
64 |
BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. |
University Of Minnesota |
19117760 |
19 |
Structure-based virtual screening for novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase and their experimental evaluation. |
Northern Kentucky University |
19781947 |
5 |
Glucose-based spiro-isoxazolines: a new family of potent glycogen phosphorylase inhibitors. |
Universite De Lyon |
16028929 |
17 |
Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL. |
Yale University |
19097784 |
55 |
Discovery of thiophene inhibitors of polo-like kinase. |
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. |
Gsk |
17004711 |
85 |
Antibacterial agent discovery using thymidylate synthase biolibrary screening. |
Unimore |
782880 |
21 |
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 |
11341829 |
9 |
Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action. |
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 i |
Bristol-Myers Squibb |
16386899 |
13 |
Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors. |
Hawaii Biotech |
15055992 |
77 |
Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. |
Biocryst Pharmaceuticals |
15723556 |
4 |
Use of binding enthalpy to drive an allosteric transition. |
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. |
Umr Cnrs 6032 |