Publications by authors named "Emmanuel Demont"

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Collection: Drug Discovery in the UK.
Simon E Ward, Emmanuel H Demont

J Med Chem· November 2024

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Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.
David J Hirst, Paul Bamborough, Niam Al-Mahdi, Davina C Angell, Heather A Barnett, Emmanuel H Demont

J Med Chem· June 2024

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Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Erin Bradley, Lucia Fusani, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont

J Med Chem· December 2023

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Design and Characterization of 1,3-Dihydro-2-benzo[]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors.
Paul Bamborough, Chun-Wa Chung, Nicole C Goodwin, Darren J Mitchell, Christopher E Neipp, Emmanuel H Demont

ACS Med Chem Lett· September 2023

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Identification of a Series of -Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
Lee A Harrison, Stephen J Atkinson, Anna Bassil, Chun-Wa Chung, Paola Grandi, Emmanuel H Demont

J Med Chem· August 2021

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Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.
Francesco Rianjongdee, Stephen J Atkinson, Chun-Wa Chung, Paola Grandi, James R J Gray, Emmanuel H Demont

J Med Chem· August 2021

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Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Jonathan T Seal, Stephen J Atkinson, Paul Bamborough, Anna Bassil, Chun-Wa Chung, Emmanuel H Demont

J Med Chem· August 2021

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Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Simon C C Lucas, Stephen J Atkinson, Chun-Wa Chung, Rob Davis, Laurie Gordon, Emmanuel H Demont

J Med Chem· August 2021

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Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Katherine L Jones, Dominic M Beaumont, Sharon G Bernard, Rino A Bit, Simon P Campbell, Emmanuel H Demont

J Med Chem· August 2021

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Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
Michael A Clegg, Natalie H Theodoulou, Paul Bamborough, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont

ACS Med Chem Lett· August 2021

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Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Helen E Aylott, Stephen J Atkinson, Paul Bamborough, Anna Bassil, Chun-Wa Chung, Emmanuel H Demont

J Med Chem· March 2021

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GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
Robert J Watson, Paul Bamborough, Heather Barnett, Chun-Wa Chung, Rob Davis, Emmanuel H Demont

J Med Chem· September 2020

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Design and Synthesis of a Highly Selective and -Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Alex Preston, Stephen Atkinson, Paul Bamborough, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont

J Med Chem· September 2020

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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.
Jonathan T Seal, Stephen J Atkinson, Helen Aylott, Paul Bamborough, Chun-Wa Chung, Emmanuel H Demont

J Med Chem· September 2020

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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.
Christopher R Wellaway, Paul Bamborough, Sharon G Bernard, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont

J Med Chem· September 2020

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Domain-selective targeting of BET proteins in cancer and immunological diseases.
Massimo Petretich, Emmanuel H Demont, Paola Grandi

Curr Opin Chem Biol· August 2020

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GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Alex Preston, Stephen J Atkinson, Paul Bamborough, Chun-Wa Chung, Laurie J Gordon, Emmanuel H Demont

ACS Med Chem Lett· August 2020

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Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
Simon C C Lucas, Stephen J Atkinson, Paul Bamborough, Heather Barnett, Chun-Wa Chung, Emmanuel H Demont

J Med Chem· May 2020

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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
Omer Gilan, Inmaculada Rioja, Kathy Knezevic, Matthew J Bell, Miriam M Yeung, Emmanuel H Demont

Science· April 2020

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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.
Paul Bamborough, Chun-Wa Chung, Emmanuel H Demont, Angela M Bridges, Peter D Craggs

J Med Chem· August 2019

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Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.
Paul Bamborough, Chun-Wa Chung, Rebecca C Furze, Paola Grandi, Anne-Marie Michon, Emmanuel H Demont

J Med Chem· September 2018

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Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Robert P Law, Stephen J Atkinson, Paul Bamborough, Chun-Wa Chung, Emmanuel H Demont

J Med Chem· May 2018

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A Chemical Probe for the ATAD2 Bromodomain.
Paul Bamborough, Chun-Wa Chung, Emmanuel H Demont, Rebecca C Furze, Andrew J Bannister

Angew Chem Int Ed Engl· September 2016

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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
Paul Bamborough, Heather A Barnett, Isabelle Becher, Mark J Bird, Chun-Wa Chung, Emmanuel H Demont

ACS Med Chem Lett· June 2016

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Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Emmanuel H Demont, James M Bailey, Rino A Bit, Jack A Brown, Colin A Campbell

J Med Chem· February 2016

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