List of works - Chun-Wa Chung

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

scientific article

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

scientific article

A Chemical Probe for the ATAD2 Bromodomain

scientific article

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

scientific article published on 15 May 2020

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

scientific article

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives

scientific article

Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ

scientific article published on 03 June 2020

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

scientific article published on 23 March 2015

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe

scientific article published on 21 December 2016

Enabling lead discovery for histone lysine demethylases by high-throughput RapidFire mass spectrometry

scientific article published on 21 August 2011

Exploring the SAR of the β-Ketoacyl-ACP Synthase Inhibitor GSK3011724A and Optimization around a Genotoxic Metabolite

scientific article published on 20 March 2020

Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides ⬇️

scientific article published on January 11, 2012

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

scientific article published on 9 May 2016

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

scientific article published on 21 July 2020

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

scientific article published on 06 July 2020

Getting the chemistry right: protonation, tautomers and the importance of H atoms in biological chemistry.

scientific article

Identification of KasA as the cellular target of an anti-tubercular scaffold

scientific article

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

scientific article published on 26 January 2015

New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold

scientific article published on 8 February 2016

Novel insight into the reaction of nitro, nitroso and hydroxylamino benzothiazinones and of benzoxacinones with Mycobacterium tuberculosis DprE1

scientific article published in Scientific Reports

PhotoAffinity Bits: A photoaffinity-based fragment screening platform for efficient identification of protein ligands

scientific article published on 03 August 2020

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

scientific article

Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase

scientific article published on 12 June 2017

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

scientific article published on 03 August 2020

The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins

scientific article published on 21 July 2020

The Optimisation of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode

scientific article published on 22 April 2020

The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

scientific article published on 23 July 2020

The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains

scientific article

List of works by Chun-Wa Chung

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

A Chemical Probe for the ATAD2 Bromodomain

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

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives

Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe

Enabling lead discovery for histone lysine demethylases by high-throughput RapidFire mass spectrometry

Exploring the SAR of the β-Ketoacyl-ACP Synthase Inhibitor GSK3011724A and Optimization around a Genotoxic Metabolite

Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides ⬇️

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

Getting the chemistry right: protonation, tautomers and the importance of H atoms in biological chemistry.

Identification of KasA as the cellular target of an anti-tubercular scaffold

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold

Novel insight into the reaction of nitro, nitroso and hydroxylamino benzothiazinones and of benzoxacinones with Mycobacterium tuberculosis DprE1

PhotoAffinity Bits: A photoaffinity-based fragment screening platform for efficient identification of protein ligands

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase

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

The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins

The Optimisation of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode

The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains