289 articles for thisTarget
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Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.
Shandong University
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain.
Pfizer
Discovery of novel BRD4 inhibitors by high-throughput screening, crystallography, and cell-based assays.
Nanchang University
Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
University of Dundee
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Genentech
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Ludwig-Maximilians-Universit£T M£Nchen
Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.
Zhejiang University
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Boehringer Ingelheim Rcv
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.
China Pharmaceutical University
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Constellation Pharmaceuticals
4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).
Albert-Ludwigs-University of Freiburg
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Genentech
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
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.
University of Freiburg
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.
The University of Texas M.D. Anderson Cancer Center
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
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
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Glaxosmithkline
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.
University of Maryland
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
The University of Tokyo
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
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Glaxosmithkline
Biased multicomponent reactions to develop novel bromodomain inhibitors.
Dana-Farber Institute
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking.
University of Zurich
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Icahn School of Medicine At Mount Sinai
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, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
Constellation Pharmaceuticals
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.
Chinese Academy of Sciences
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
University of Oxford
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
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Pfizer
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
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
University of Oxford
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
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Genentech
Discovery and anti-tumor activity of 4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one (CG13250), a potent, selective and orally bioavailable BET bromodomain inhibitor.
University of Maryland
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.
University of Modena and Reggio Emilia
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
Constellation Pharmaceuticals
Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery.
China Pharmaceutical University
A comprehensive review of BET-targeting PROTACs for cancer therapy.
Xinxiang Medical University
Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.
China Pharmaceutical University
Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy.
Xinxiang Medical University
Design, synthesis, and biological evaluation of quinoxalinone derivatives as potent BRD4 inhibitors.
Lanzhou University
Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment.
Shandong First Medical University and Shandong Academy of Medical Sciences
Design, synthesis and anticancer evaluation of 3-methyl-1H-indazole derivatives as novel selective bromodomain-containing protein 4 inhibitors.
China Pharmaceutical University
Targeting MYC: From understanding its biology to drug discovery.
Institut De Recherches Cliniques De Montreal (IRCM)
A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.
University of Electronic Science and Technology of China
From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD).
University of S£O Paulo
Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs).
"Sapienza" University of Rome
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development.
West China Hospital of Sichuan University
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Gsk
Discovery of Novel BRD4 Ligand Scaffolds by Automated Navigation of the Fragment Chemical Space.
Universitat De Barcelona
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
Sun Yat-Sen University Cancer Center
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Newcastle University Centre For Cancer
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.
West China Hospital of Sichuan University
Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.
University of Chinese Academy of Sciences
Discovery of indol-6-yl-pyrrolo[2,3-c]pyridin-7-one derivatives as bromodomain-containing protein 4 (BRD4) inhibitors for the treatment of kidney fibrosis.
West China Hospital of Sichuan University
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Glaxosmithkline R&D
Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer.
Guangzhou Medical University
Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.
Southern Research
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
Hefei University of Technology
Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor.
Southwest Jiaotong University
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Constellation, A Morphosys
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.
West China Hospital
Discovery of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as novel and potent bromodomain and extra-terminal (BET) inhibitors with anticancer efficacy.
China Pharmaceutical University
Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer.
China Pharmaceutical University
Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential.
West China Hospital
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.
Shandong First Medical University & Shandong Academy of Medical Sciences
Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity.
University of Minnesota
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
Bristol Myers Squibb
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
Sichuan University
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
China Pharmaceutical University
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Current status in the discovery of dual BET/HDAC inhibitors.
The First Affiliated Hospital of Zhengzhou University
Medulloblastoma drugs in development: Current leads, trials and drawbacks.
University of Connecticut
Current status in the discovery of dual BET/HDAC inhibitors.
The First Affiliated Hospital of Zhengzhou University
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
Universit£T Leipzig
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy.
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.
China Pharmaceutical University
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Bristol Myers Squibb
CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
Cnrs
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Astrazeneca
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.
University of Minnesota
Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
Md Anderson Cancer Center
Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag.
Dana Farber Cancer Institute
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
Moffitt Cancer Center
Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype.
Bristol Myers Squibb Research and Development
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.
University of Oxford
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Glaxosmithkline
Novel Bromodomain Inhibitors for Treating Cancer, Fibrosis, and Inflammatory Disorders.
Smith, Gambrell & Russell
Identification of isoform/domain-selective fragments from the selection of DNA-encoded dynamic library.
The University of Hong Kong
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Glaxosmithkline
Toward the assembly and characterization of an encoded library hit confirmation platform: Bead-Assisted Ligand Isolation Mass Spectrometry (BALI-MS).
Pfizer
Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors.
Smith, Gambrell & Russell
New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
University of Minnesota
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.
Glaxosmithkline
Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
Glaxosmithkline R&D
Development of Dimethylisoxazole-Attached Imidazo[1,2-
University of Massachusetts Boston
Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.
China Pharmaceutical University
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
Southern Medical University
Development of BET inhibitors as potential treatments for cancer: A search for structural diversity.
Bristol Myers Squibb Research and Development
Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
Martin-Luther University of Halle-Wittenberg
Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).
Guangzhou Medical University
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
Shanghai Institute of Materia Medica
Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.
China Pharmaceutical University
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies.
Rwth Aachen University
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1
Chinese Academy of Sciences
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
Glaxosmithkline
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.
Shandong First Medical University & Shandong Academy of Medical Sciences
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model.
Kyorin Pharmaceutical
4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines.
Albert-Ludwigs-Universit£T Freiburg
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.
Constellation Pharmaceuticals
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.
Lanzhou University
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.
Chinese Academy of Sciences
Tumor-Targeted Bivalent Protein Degradation for Application in Cancer Therapy.
Usona Institute
Substituted 1-methyl-4-phenylpyrrolidin-2-ones - Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors.
Monash University (Parkville Campus)
Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors.
Southwest Jiaotong University
Design, synthesis and biological evaluation of imidazolopyridone derivatives as novel BRD4 inhibitors.
China Pharmaceutical University
Lead optimization and efficacy evaluation of quinazoline-based BET family inhibitors for potential treatment of cancer and inflammatory diseases.
National Institutes of Health
Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.
Glaxosmithkline R&D
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
University of Oxford
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
University of Oxford
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
University of Oxford
BET proteins: Investigating BRDT as a potential target for male contraception.
University of Minnesota
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
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
Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors.
China Pharmaceutical University
Substituted pteridinones as p90 ribosomal S6 protein kinase (RSK) inhibitors: A structure-activity study.
University of Colorado Anschutz Medical Campus
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Glaxosmithkline Medicines Research Centre
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
Glaxosmithkline R&D
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6
Harvard Medical School
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
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.
China Pharmaceutical University
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies.
China Pharmaceutical University
Pros and cons of virtual screening based on public "Big Data": In silico mining for new bromodomain inhibitors.
University of Strasbourg
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
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Genentech
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.
University of Chinese Academy of Sciences
Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains.
University of Minnesota
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
University of Texas Medical Branch
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Gsk
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.
The Institute of Cancer Research
Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.
Sichuan University
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
The Walter and Eliza Hall Institute For Medical Research
Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
Central South University
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
Southeast University
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
Systematically Mitigating the p38? Activity of Triazole-based BET Inhibitors.
University of Minnesota Twin Cities
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38? and BRD4.
Newcastle University
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.
University of Chinese Academy of Sciences
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
University of Strathclyde
Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains.
Moffitt Cancer Center
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
Sun Yat-Sen University
Novel phenanthridin-6(5H)-one derivatives as potent and selective BET bromodomain inhibitors: Rational design, synthesis and biological evaluation.
Henan University of Traditional Chinese Medicine
Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation.
Shaoxing University
Discovery of Thieno[2,3-
Sichuan University and Collaborative Innovation Center of Biotherapy
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
Arromax Pharmatech
Clinical candidates modulating protein-protein interactions: The fragment-based experience.
Taros Chemicals
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Gilead Sciences
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Chinese Academy of Sciences
Privileged Structures and Polypharmacology within and between Protein Families.
The Institute of Cancer Research
Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-
China Pharmaceutical University
Synthesis and elaboration of N-methylpyrrolidone as an acetamide fragment substitute in bromodomain inhibition.
Monash University (Parkville Campus)
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
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Genentech
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
University of Minnesota
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.
Dana Farber Cancer Institute
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
University of Oxford
[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
University of Oxford
Structure-based discovery of selective BRPF1 bromodomain inhibitors.
University of Zurich
Discovery and lead identification of quinazoline-based BRD4 inhibitors.
National Institutes of Health
Integrated Strategy for Lead Optimization Based on Fragment Growing: The Diversity-Oriented-Target-Focused-Synthesis Approach.
Aix-Marseille University
Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.
Guangzhou Medical University
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.
Glaxosmithkline
Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine.
Zenith Epigenetics
Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.
Celgene Quanticel Research
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.
University of Dundee
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
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.
University of Massachusetts-Boston
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.
Chinese Academy of Sciences
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Abbvie
Design and Optimization of Benzopiperazines as Potent Inhibitors of BET Bromodomains.
Forma Therapeutics
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
Characterization of a highly selective inhibitor of the Aurora kinases.
Harvard Medical School
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
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.
Hebei University
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
Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.
Guangzhou Medical University
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
Walter and Eliza Hall Institute of Medical Research
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.
Chinese Academy of Sciences
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
University of Oxford
Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.
Bienta/Enamine
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Genentech
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
Genentech
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
University College London
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Abbvie
Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment.
Korea Research Institute of Chemical Technology
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Sichuan University and Collaborative Innovation Center
Drug Discovery Targeting Bromodomain-Containing Protein 4.
University of Texas Medical Branch
Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors.
China Pharmaceutical University
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
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Genentech
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
Direct NMR Probing of Hydration Shells of Protein Ligand Interfaces and Its Application to Drug Design.
University of Vienna
BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.
University of Minnesota
Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities.
Pfizer