未登录 BET Isoform Selectivity through Diverse Linkers for Bivalent Inhibitors: GSK785, a BRD2/4-Selective Bivalent BET Inhibitor Rianjongdee, Francesco; Atkinson, Stephen J.; Bamborough, Paul; Barnett, Heather A.; Friston, Kallie; Grandi, Paola; Neipp, Christopher E.; Petretich, Massimo; Phillipou, Alex; Preston, Alex G. S.; Prinjha, Rab K.; Tomkinson, Nicholas C. O.; Demont, Emmanuel H. 分享 收藏
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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
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
Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors Bamborough, Paul; Chung, Chun-wa; Goodwin, Nicole C. C.; Mitchell, Darren J. J.; Neipp, Christopher E. E.; Phillipou, Alex; Preston, Alex; Prinjha, Rab K. K.; Soden, Peter E. E.; Watson, Robert J. J.; Demont, Emmanuel H. H. 分享 收藏
Multigram Synthesis of Tetrasubstituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow (vol 26, pg 365, 2022) Alder, Catherine M.; Gray, Matthew; Huff, Chelsea A.; Manning, Calvin O.; Preston, Alex; Rushworth, Philip; Shuster, Leanna E.; Watson, Robert J.; Wheelhouse, Katherine M. P.; Williams, Glynn D.; Demont, Emmanuel H. 分享 收藏
Multigram Synthesis of Tetrasubsituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow Alder, Catherine M.; Gray, Matthew; Huff, Chelsea A.; Manning, Calvin O.; Preston, Alex; Rushworth, Philip; Shuster, Leanna E.; Watson, Robert J.; Wheelhouse, Katherine M. P.; Williams, Glynn D.; Demont, Emmanuel H. 分享 收藏
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, V; 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. 分享 收藏
Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors Clegg, Michael A.; Theodoulou, Natalie H.; Bamborough, Paul; Chung, Chun-wa; Craggs, Peter D.; Demont, Emmanuel H.; Gordon, Laurie J.; Liwicki, Gemma M.; Phillipou, Alex; Tomkinson, Nicholas C. O.; Prinjha, Rab K.; Humphreys, Philip G. 分享 收藏
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
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.; Wyspianska, Beata S.; Kerr, William J.; Prinjha, Rab K. 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
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. 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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