The Discovery of I‑BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor
Gosmini, Romain, Nguyen, Van Loc, Toum, Jérôme, Simon, Christophe, Brusq, Jean-Marie G, Krysa, Gael, Mirguet, Olivier, Riou-Eymard, Alizon M, Boursier, Eric V, Trottet, Lionel, Bamborough, Paul, Clark, Hugh, Chung, Chun-wa, Cutler, Leanne, Demont, Emmanuel H, Kaur, Rejbinder, Lewis, Antonia J, Schilling, Mark B, Soden, Peter E, Taylor, Simon, Walker, Ann L, Walker, Matthew D, Prinjha, Rab K, Nicodème, Edwige
Published in Journal of medicinal chemistry (09.10.2014)
Published in Journal of medicinal chemistry (09.10.2014)
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Domain-selective targeting of BET proteins in cancer and immunological diseases
Petretich, Massimo, Demont, Emmanuel H., Grandi, Paola
Published in Current opinion in chemical biology (01.08.2020)
Published in Current opinion in chemical biology (01.08.2020)
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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
Bamborough, Paul, Barnett, Heather A, Becher, Isabelle, Bird, Mark J, Chung, Chun-wa, Craggs, Peter D, Demont, Emmanuel H, Diallo, Hawa, Fallon, David J, Gordon, Laurie J, Grandi, Paola, Hobbs, Clare I, Hooper-Greenhill, Edward, Jones, Emma J, Law, Robert P, Le Gall, Armelle, Lugo, David, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Sheppard, Robert J, Watson, Allan J. B, Watson, Robert J
Published in ACS medicinal chemistry letters (09.06.2016)
Published in ACS medicinal chemistry letters (09.06.2016)
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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
Gilan, Omer, Rioja, Inmaculada, Knezevic, Kathy, Bell, Matthew J, Yeung, Miriam M, Harker, Nicola R, Lam, Enid Y N, Chung, Chun-Wa, Bamborough, Paul, Petretich, Massimo, Urh, Marjeta, Atkinson, Stephen J, Bassil, Anna K, Roberts, Emma J, Vassiliadis, Dane, Burr, Marian L, Preston, Alex G S, Wellaway, Christopher, Werner, Thilo, Gray, James R, Michon, Anne-Marie, Gobbetti, Thomas, Kumar, Vinod, Soden, Peter E, Haynes, Andrea, Vappiani, Johanna, Tough, David F, Taylor, Simon, Dawson, Sarah-Jane, Bantscheff, Marcus, Lindon, Matthew, Drewes, Gerard, Demont, Emmanuel H, Daniels, Danette L, Grandi, Paola, Prinjha, Rab K, Dawson, Mark A
Published in Science (American Association for the Advancement of Science) (24.04.2020)
Published in Science (American Association for the Advancement of Science) (24.04.2020)
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GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins
Watson, Robert J, Bamborough, Paul, Barnett, Heather, Chung, Chun-wa, Davis, Rob, Gordon, Laurie, Grandi, Paola, Petretich, Massimo, Phillipou, Alex, Prinjha, Rab K, Rioja, Inmaculada, Soden, Peter, Werner, Thilo, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
Law, Robert P, Atkinson, Stephen J, Bamborough, Paul, Chung, Chun-wa, Demont, Emmanuel H, Gordon, Laurie J, Lindon, Matthew, Prinjha, Rab K, Watson, Allan J. B, Hirst, David J
Published in Journal of medicinal chemistry (24.05.2018)
Published in Journal of medicinal chemistry (24.05.2018)
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Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit
Rianjongdee, Francesco, Atkinson, Stephen J, Chung, Chun-wa, Grandi, Paola, Gray, James R. J, Kaushansky, Laura J, Medeiros, Patricia, Messenger, Cassie, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Satz, Alexander L, Taylor, Simon, Wall, Ian D, Watson, Robert J, Yao, Gang, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
Seal, Jonathan T, Atkinson, Stephen J, Aylott, Helen, Bamborough, Paul, Chung, Chun-wa, Copley, Royston C. B, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Lindon, Matthew, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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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
Wellaway, Christopher R, Bamborough, Paul, Bernard, Sharon G, Chung, Chun-wa, Craggs, Peter D, Cutler, Leanne, Demont, Emmanuel H, Evans, John P, Gordon, Laurie, Karamshi, Bhumika, Lewis, Antonia J, Lindon, Matthew J, Mitchell, Darren J, Rioja, Inmaculada, Soden, Peter E, Taylor, Simon, Watson, Robert J, Willis, Rob, Woolven, James M, Wyspiańska, Beata S, Kerr, William J, Prinjha, Rab K
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins
Preston, Alex, Atkinson, Stephen, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Jones, Emma J, Lindon, Matthew, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan, Taylor, Simon, Wall, Ian, Watson, Robert J, Woolven, James, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N‑Terminal Bromodomain Chemical Probe
Bradley, Erin, Fusani, Lucia, Chung, Chun-wa, Craggs, Peter D., Demont, Emmanuel H., Humphreys, Philip G., Mitchell, Darren J., Phillipou, Alex, Rioja, Inmaculada, Shah, Rishi R., Wellaway, Christopher R., Prinjha, Rab K., Palmer, David S., Kerr, William J., Reid, Marc, Wall, Ian D., Cookson, Rosa
Published in Journal of medicinal chemistry (14.12.2023)
Published in Journal of medicinal chemistry (14.12.2023)
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A Chemical Probe for the ATAD2 Bromodomain
Bamborough, Paul, Chung, Chun-wa, Demont, Emmanuel H., Furze, Rebecca C., Bannister, Andrew J., Che, Ka Hing, Diallo, Hawa, Douault, Clement, Grandi, Paola, Kouzarides, Tony, Michon, Anne-Marie, Mitchell, Darren J., Prinjha, Rab K., Rau, Christina, Robson, Samuel, Sheppard, Robert J., Upton, Richard, Watson, Robert J.
Published in Angewandte Chemie (International ed.) (12.09.2016)
Published in Angewandte Chemie (International ed.) (12.09.2016)
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Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors
Bamborough, Paul, Chung, Chun-wa, Furze, Rebecca C, Grandi, Paola, Michon, Anne-Marie, Sheppard, Robert J, Barnett, Heather, Diallo, Hawa, Dixon, David P, Douault, Clement, Jones, Emma J, Karamshi, Bhumika, Mitchell, Darren J, Prinjha, Rab K, Rau, Christina, Watson, Robert J, Werner, Thilo, Demont, Emmanuel H
Published in Journal of medicinal chemistry (13.08.2015)
Published in Journal of medicinal chemistry (13.08.2015)
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Journal Article
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors
Lucas, Simon C. C, Atkinson, Stephen J, Chung, Chun-wa, Davis, Rob, Gordon, Laurie, Grandi, Paola, Gray, James J. R, Grimes, Thomas, Phillipou, Alexander, Preston, Alex G, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Tomkinson, Nicholas C. O, Wall, Ian, Watson, Robert J, Woolven, James, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors
Seal, Jonathan T, Atkinson, Stephen J, Bamborough, Paul, Bassil, Anna, Chung, Chun-wa, Foley, James, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Kruger, Ryan G, Matteo, Jeanne J, McCabe, Michael T, Messenger, Cassie, Mitchell, Darren, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Wyce, Anastasia, Zhang, Xi-Ping, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors
Aylott, Helen E, Atkinson, Stephen J, Bamborough, Paul, Bassil, Anna, Chung, Chun-wa, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Messenger, Cassie, Mitchell, Darren, Phillipou, Alexander, Preston, Alex, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan T, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Identification of a Series of N‑Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins
Harrison, Lee A, Atkinson, Stephen J, Bassil, Anna, Chung, Chun-wa, Grandi, Paola, Gray, James R. J, Levernier, Etienne, Lewis, Antonia, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jonathan T, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression
Jones, Katherine L., Beaumont, Dominic M., Bernard, Sharon G., Bit, Rino A., Campbell, Simon P., Chung, Chun-wa, Cutler, Leanne, Demont, Emmanuel H., Dennis, Kate, Gordon, Laurie, Gray, James R., Haase, Michael, Lewis, Antonia J., McCleary, Scott, Mitchell, Darren J., Moore, Susanne M., Parr, Nigel, Robb, Olivia J., Smithers, Nicholas, Soden, Peter E., Suckling, Colin J., Taylor, Simon, Walker, Ann L., Watson, Robert J., Prinjha, Rab K.
Published in Journal of medicinal chemistry (26.08.2021)
Published in Journal of medicinal chemistry (26.08.2021)
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Journal Article
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode
Lucas, Simon C. C, Atkinson, Stephen J, Bamborough, Paul, Barnett, Heather, Chung, Chun-wa, Gordon, Laurie, Mitchell, Darren J, Phillipou, Alexander, Prinjha, Rab K, Sheppard, Robert J, Tomkinson, Nicholas C. O, Watson, Robert J, Demont, Emmanuel H
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
Demont, Emmanuel H., Chung, Chun-wa, Furze, Rebecca C., Grandi, Paola, Michon, Anne-Marie, Wellaway, Chris, Barrett, Nathalie, Bridges, Angela M., Craggs, Peter D., Diallo, Hawa, Dixon, David P., Douault, Clement, Emmons, Amanda J., Jones, Emma J., Karamshi, Bhumika V., Locke, Kelly, Mitchell, Darren J., Mouzon, Bernadette H., Prinjha, Rab K., Roberts, Andy D., Sheppard, Robert J., Watson, Robert J., Bamborough, Paul
Published in Journal of medicinal chemistry (23.07.2015)
Published in Journal of medicinal chemistry (23.07.2015)
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