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Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor Johannes, Jeffrey W.; Balazs, Amber Y. S.; Barratt, Derek; Bista, Michal; Chuba, Matthew D.; Cosulich, Sabina; Critchlow, Susan E.; Degorce, SebastienL.; Di Fruscia, Paolo; Edmondson, Scott D.; Embrey, Kevin J.; Fawell, Stephen; Ghosh, Avipsa; Gill, Sonja J.; Gunnarsson, Anders; Hande, Sudhir M.; Heightman, Tom D.; Hemsley, Paul; Illuzzi, Giuditta; Lane, Jordan; Larner, Carrie J. B.; Leo, Elisabetta; Liu, Lina; Madin, Andrew; Mcwilliams, Lisa; O'Connor, Mark J.; Orme, Jonathan P.; Pachl, Fiona; Packer, Martin J.; Pei, Xiaohui; Pike, Andy; Schimpl, Marianne; She, Hongyao; Staniszewska, Anna D.; Talbot, Verity; Underwood, Elizabeth; Varnes, Jeffrey G.; Xue, Lin; Yao, Tieguang; Zhang, Ke; Zhang, Andrew X.; Zheng, Xiaolan 分享 收藏
Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations Thomson, Clare; Braybrooke, Erin; Colclough, Nicola; Davies, Nichola L.; Floc'h, Nicolas; Greenwood, Ryan; Guerot, Carine; Hargreaves, David; Johnstrom, Peter; Khurana, Puneet; Kostomiris, Demetrios H.; Li, Songlei; Lister, Andrew; Lorthioir, Olivier; Martin, Scott; Mccoull, William; Mclean, Neville J.; Mcwilliams, Lisa; Orme, Jonathan P.; Packer, Martin J.; Pearson, Stuart; Swaih, Aisha M.; Tentarelli, Sharon; Tucker, Michael J.; Ward, Richard A.; Wilkinson, Stephen; Winlow, Poppy; Wood, Isabel L. 分享 收藏
Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer Bagal, Sharan K.; Astles, Peter C.; Diene, Coura; Argyrou, Argyrides; Crafter, Claire; Cassar, Doyle J.; Fallan, Charlene; Hock, Andreas; Jones, Thomas; Moreau, Kevin; Lamont, Gillian M.; Lamont, Scott; Michaloglou, Chrysiis; Packer, Martin J.; Pike, Andy; Ramos-Montoya, Antonio; Scott, James S.; Shaw, Joseph; Shologu, Ziyanda 分享 收藏
Fragment-Based Discovery of Novel MUS81 Inhibitors 基于片段的新型MUS81抑制剂的发现 Collie, Gavin W.; Borjesson, Ulf; Chen, Yunhua; Dong, Zhiqiang; Di Fruscia, Paolo; Gohlke, Andrea; Hoyle, Anna; Hunt, Thomas A.; Jesani, Mehul H.; Luo, Haiou; Luptak, Jakub; Milbradt, Alexander G.; Narasimhan, Priyanka; Packer, Martin; Patel, Saleha; Qiao, Jingchuan; Storer, R. Ian; Stubbs, Christopher J.; Tart, Jonathan; Truman, Caroline; Wang, Anderson T.; Wheeler, Matthew G.; Winter-Holt, Jon 分享 收藏
Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations Thomson, Clare; Barton, Peter; Braybrooke, Erin; Colclough, Nicola; Dong, Zhiqiang; Evans, Laura; Floc'h, Nicolas; Guerot, Carine; Hargreaves, David; Khurana, Puneet; Li, Songlei; Li, Xiuwei; Lister, Andrew; McCoull, William; McWilliams, Lisa; Orme, Jonathan P.; Packer, Martin J.; Swaih, Aisha M.; Ward, Richard A.; Winlow, Poppy; Ye, Yang 分享 收藏
Design of rigid protein-protein interaction inhibitors enables targeting of undruggable Mcl-1 刚性蛋白-蛋白相互作用抑制剂的设计使得靶向不可服用的Mcl-1成为可能 Hargreaves, David; Carbajo, Rodrigo J.; Bodnarchuk, Michael S.; Embrey, Kevin; Rawlins, Philip B.; Packer, Martin; Degorce, Sebastien L.; Hird, Alexander W.; Johannes, Jeffrey W.; Chiarparin, Elisabetta; Schade, Markus 分享 收藏
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NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24 Torres, Felix; Walser, Reto; Kaderli, Janina; Rossi, Emanuele; Bobby, Romel; Packer, Martin J.; Sarda, Sunil; Walker, Graeme; Hitchin, James R.; Milbradt, Alexander G.; Orts, Julien 分享 收藏
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs Johannes, Jeffrey W.; Balazs, Amber; Barratt, Derek; Bista, Michal; Chuba, Matthew D.; Cosulich, Sabina; Critchlow, Susan E.; Degorce, Sebastien L.; Di Fruscia, Paolo; Edmondson, Scott D.; Embrey, Kevin; Fawell, Stephen; Ghosh, Avipsa; Gill, Sonja J.; Gunnarsson, Anders; Hande, Sudhir M.; Heightman, Tom D.; Hemsley, Paul; Illuzzi, Giuditta; Lane, Jordan; Larner, Carrie; Leo, Elisabetta; Liu, Lina; Madin, Andrew; Martin, Scott; McWilliams, Lisa; O'Connor, Mark J.; Orme, Jonathan P.; Pachl, Fiona; Packer, Martin J.; Pei, Xiaohui; Pike, Andrew; Schimpl, Marianne; She, Hongyao; Staniszewska, Anna D.; Talbot, Verity; Underwood, Elizabeth; Varnes, Jeffrey G.; Xue, Lin; Yao, Tieguang; Zhang, Ke; Zhang, Andrew X.; Zheng, Xiaolan 分享 收藏
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles (vol 62, pg 9418, 2019) Balazs, Amber Y. S.; Carbajo, Rodrigo J.; Davies, Nichola L.; Dong, Yu; Hird, Alexander W.; Johannes, Jeffrey W.; Lamb, Michelle L.; McCoull, William; Raubo, Piotr; Robb, Graeme R.; Packer, Martin J.; Chiarparin, Elisabetta 分享 收藏
Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors Banks, Erica; Grondine, Michael; Bhavsar, Deepa; Barry, Evan; Kettle, Jason G.; Reddy, Venkatesh Pilla; Brown, Crystal; Wang, Haiyun; Mettetal, Jerome T.; Collins, Teresa; Adeyemi, Oladipupo; Overman, Ross; Lawson, Deborah; Harmer, Alexander R.; Reimer, Corinne; Drew, Lisa; Packer, Martin J.; Cosulich, Sabina; Jones, Rhys D. O.; Shao, Wenlin; Wilson, David; Guichard, Sylvie; Fawell, Stephen; Anjum, Rana 分享 收藏
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PELE-MSM: A Monte Carlo Based Protocol for the Estimation of Absolute Binding Free Energies Gilabert, Joan F.; Grebner, Christoph; Soler, Daniel; Lecina, Daniel; Municoy, Marti; Gracia Carmona, Oriol; Soliva, Robert; Packer, Martin J.; Hughes, Samantha J.; Tyrchan, Christian; Hogner, Anders; Guallar, Victor 分享 收藏
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles Balazs, Amber Y. S.; Carbajo, Rodrigo J.; Davies, Nichola L.; Dong, Yu; Hird, Alexander W.; Johannes, Jeffrey W.; Lamb, Michelle L.; McCoull, William; Raubo, Piotr; Robb, Graeme R.; Packer, Martin J.; Chiarparin, Elisabetta 分享 收藏
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Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia Tron, Adriana E.; Belmonte, Matthew A.; Adam, Ammar; Aquila, Brian M.; Boise, Lawrence H.; Chiarparin, Elisabetta; Cidado, Justin; Embrey, Kevin J.; Gangl, Eric; Gibbons, Francis D.; Gregory, Gareth P.; Hargreaves, David; Hendricks, J. Adam; Johannes, Jeffrey W.; Johnstone, Ricky W.; Kazmirski, Steven L.; Kettle, Jason G.; Lamb, Michelle L.; Matulis, Shannon M.; Nooka, Ajay K.; Packer, Martin J.; Peng, Bo; Rawlins, Philip B.; Robbins, Daniel W.; Schuller, Alwin G.; Su, Nancy; Yang, Wenzhan; Ye, Qing; Zheng, Xiaolan; Secrist, J. Paul; Clark, Edwin A.; Wilson, David M.; Fawell, Stephen E.; Hird, Alexander W. 分享 收藏
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