PMID

Data

Article Title

Organization

An Advanced Tool To Interrogate BRD9.

Moffitt Cancer Center

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.

Boehringer Ingelheim Rcv

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.

Glaxosmithkline

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Glaxosmithkline

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.

Icahn School of Medicine At Mount Sinai

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

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.

University of Minnesota

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

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

Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains.

Moffitt Cancer Center

Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.

Gilead Sciences

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

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

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

Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.

TBA

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

A Versatile Method to Determine the Cellular Bioavailability of Small-Molecule Inhibitors.

H. Lee Moffitt Cancer Center and Research Institute

Methylpyrrole inhibitors of BET bromodomains.

Abbvie

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