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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 Hirst, David J.; Bamborough, Paul; Al-Mahdi, Niam; Angell, Davina C.; Barnett, Heather A.; Baxter, Andrew; Bit, Rino A.; Brown, Jack A.; Chung, Chun-wa; Craggs, Peter D.; Davis, Robert P.; Demont, Emmanuel H.; Ferrie, Alan; Gordon, Laurie J.; Harada, Isobel; Ho, Tim C. T.; Holyer, Ian D.; Hooper-Greenhill, Edward; Jones, Katherine L.; Lindon, Matthew J.; Lovatt, Cerys; Lugo, David; Maller, Claire; Mcgonagle, Grant; Messenger, Cassie; Mitchell, Darren J.; Pascoe, David D.; Patel, Vipulkumar K.; Patten, Christopher; Poole, Darren L.; Shah, Rishi R.; Rioja, Inmaculada; Stafford, Kayleigh A. J.; Tape, Daniel; Taylor, Simon; Theodoulou, Natalie H.; Tomlinson, Laura; Wall, Ian D.; Wellaway, Christopher R.; White, Gemma; Prinjha, Rab K.; Humphreys, Philip G. 分享 收藏
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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 分享 收藏
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 Humphreys, Philip G.; Anderson, Niall A.; Bamborough, Paul; Baxter, Andrew; Chung, Chun-wa; Cookson, Rosa; Craggs, Peter D.; Dalton, Toryn; Fournier, Julie C. L.; Gordon, Laurie J.; Gray, Heather F.; Gray, Matthew W.; Gregory, Richard; Hirst, David J.; Jamieson, Craig; Jones, Katherine L.; Kessedjian, Hripsimee; Lugo, David; McGonagle, Grant; Patel, Vipulkumar K.; Patten, Christopher; Poole, Darren L.; Prinjha, Rab K.; Ramirez-Molina, Cesar; Rioja, Inmaculada; Seal, Gail; Stafford, Kayleigh A. J.; Shah, Rishi R.; Tape, Daniel; Theodoulou, Natalie H.; Tomlinson, Laura; Ukuser, Sabri; Wall, Ian D.; Wellaway, Natalie; White, Gemma 分享 收藏
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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 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. 分享 收藏
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. 分享 收藏
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. 分享 收藏
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. 分享 收藏
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. 分享 收藏
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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 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. 分享 收藏
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. 分享 收藏
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family Preston, Alex; Atkinson, Stephen J.; Bamborough, Paul; Chung, Chun-wa; Gordon, Laurie J.; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Lewis, Antonia J.; Lugo, David; Messenger, Cassie; Michon, Anne-Marie; Mitchell, Darren J.; Prinjha, Rab K.; Rioja, Inmaculada; Seal, Jon; Taylor, Simon; Thesmar, Pierre; Wall, Ian D.; Watson, J.; Woolven, James M.; Demont, Emmanuel H. 分享 收藏
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Mycobacterium tuberculosis Decaprenylphosphoryl-β-D-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity Borthwick, Jennifer A.; Alemparte, Carlos; Wall, Ian; Whitehurst, Benjamin C.; Argyrou, Argyrides; Burley, Glenn; de Dios-Anton, Paco; Guijarro, Laura; Monteiro, Maria Candida; Ortega, Fatima; Suckling, Colin J.; Pichel, Julia Castro; Cacho, Monica; Young, Robert J. 分享 收藏
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Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening Wellaway, Christopher R.; Amans, Dominique; Bamborough, Paul; Barnett, Heather; Bit, Rino A.; Brown, Jack A.; Carlson, Neil R.; Chung, Chun-wa; Cooper, Anthony W. J.; Craggs, Peter D.; Davis, Robert P.; Dean, Tony W.; Evans, John P.; Gordon, Laurie; Harada, Isobel L.; Hirst, David J.; Humphreys, Philip G.; Jones, Katherine L.; Lewis, Antonia J.; Lindon, Matthew J.; Lugo, Dave; Mahmood, Mahnoor; McCleary, Scott; Medeiros, Patricia; Mitchell, Darren J.; O'Sullivan, Michael; Le Gall, Armelle; Patel, Vipulkumar K.; Patten, Chris; Poole, Darren L.; Shah, Rishi R.; Smith, Jane E.; Stafford, Kayleigh A. J.; Thomas, Pamela J.; Vimal, Mythily; Wall, Ian D.; Watson, Robert J.; Wellaway, Natalie; Yao, Gang; Prinjha, Rab K. 分享 收藏
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