original ) (raw )Discovery and characterization of bromodomain 2–specific inhibitors of BRDT
Sureshbabu Nagarajan
Proceedings of the National Academy of Sciences, 2021
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Preclinical characterization of BET family bromodomain inhibitor ABBV-075 suggests combination therapeutic strategies
Mai Bùi
Cancer research, 2017
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The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development
Chao-yie Yang
Journal of Medicinal Chemistry, 2013
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AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies
Michael Waring
Molecular cancer therapeutics, 2016
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Potent and selective bivalent inhibitors of BET bromodomains
Michael Waring
Nature Chemical Biology, 2016
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LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor
Lucas Vieira
Angewandte Chemie, 2015
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Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement
Huarui Cui
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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia
Mai Bùi
Molecular Cancer Therapeutics, 2021
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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)
David Lugo
Bioorganic & medicinal chemistry letters, 2012
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Selective inhibition of BET bromodomains
Amanda Christie
2010
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Rational design and development of selective BRD7 bromodomain inhibitors and their activity in prostate cancer
Sandra Alcala Ordóñez
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Design and characterization of bivalent BET inhibitors
Amanda Souza
Nature chemical biology, 2016
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Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies
Anne Cheasty
Journal of medicinal chemistry, 2017
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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
Mai Bùi
Journal of Medicinal Chemistry, 2017
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BET Bromodomain Inhibitors With One-step Synthesis Discovered from Virtual Screen
Norbert Berndt
Journal of medicinal chemistry, 2017
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Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes
Xavier Lucas , Stefan Gerhardt
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The Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
Anne-Marie Michon
Journal of medicinal chemistry, 2015
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A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification
Anne-Marie Michon
Journal of Medicinal Chemistry, 2019
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Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains
Guangtao Zhang
Journal of Medicinal Chemistry, 2013
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Targeting the BET family for the treatment of leukemia
Xavier Lucas
Epigenomics, 2014
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CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation
Sebastien Combes
Journal of Medicinal Chemistry, 2022
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Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)
James Audia
ACS Medicinal Chemistry Letters, 2016
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Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability
Alessandra Pasquo
PLOS ONE, 2016
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The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
Anne-Marie Michon
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Clinical trials for BET inhibitors run ahead of the science
G. Is
Drug Discovery Today: Technologies, 2016
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Biased multicomponent reactions to develop novel bromodomain inhibitors
Asha kadam
Journal of medicinal chemistry, 2014
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Pyronaridine as a Bromodomain-Containing Protein 4-N-Terminal Bromodomain (BRD4-BD1) Inhibitor: In Silico Database Mining, Molecular Docking, and Molecular Dynamics Simulation
Alaa Abdelrahman
Molecules, 2023
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IDENTIFICATION OF POTENT BROMODOMAIN4 (BRD4) INHIBITORS BY ENERGY-PHARMACOPHORE BASED VIRTUAL SCREENING TO TARGET BRD4-NUT MIDLINE CARCINOMA
International Journal of Pharmacy and Pharmaceutical Sciences (IJPPS)
International Journal of Pharmacy and Pharmaceutical Sciences, 2015
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Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor
Huarui Cui
Journal of Medicinal Chemistry
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Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor
Mary Do
Journal of Medicinal Chemistry, 2016
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Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition
Ola Epemolu
Chemical Science, 2018
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Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
Ildiko Felletar
Journal of Medicinal Chemistry, 2013
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First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours
John Aspegren
British Journal of Cancer
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The BET Bromodomain inhibitor OTX015 affects pathogenetic pathways in pre-clinical B-cell tumor models and synergizes with targeted drugs
Esteban Cvitkovic
Clinical Cancer Research, 2015
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