未登录 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
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Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor Tamanini, Emiliano; Miyamura, Shin; Buck, Ildiko M.; Cons, Benjamin D.; Dawson, Lee; East, Charlotte; Futamura, Takashi; Goto, Shintaro; Griffiths-Jones, Charlotte; Hashimoto, Tetsuya; Heightman, Tom D.; Ishikawa, Shunpei; Ito, Hideki; Kaneko, Yosuke; Kawato, Tatsuya; Kondo, Kazumi; Kurihara, Naoki; McCarthy, James M.; Mori, Yukiko; Nagase, Tsuyoshi; Nakaishi, Yuichiro; Reeks, Judith; Sato, Akimasa; Schopf, Patrick; Tai, Kuninori; Tamai, Taichi; Tisi, Dominic; Woolford, Alison J. -A. 分享 收藏
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction Norton, David; Bonnette, William G.; Callahan, James F.; Carr, Maria G.; Griffiths-Jones, Charlotte M.; Heightman, Tom D.; Kerns, Jeffrey K.; Nie, Hong; Rich, Sharna J.; Richardson, Caroline; Rumsey, William; Sanchez, Yolanda; Verdonk, Marcel L.; Willems, Henriette M. G.; Wixted, William E.; Wolfe, Lawrence, III; Woolford, Alison J-A; Wu, Zining; Davies, Thomas G. 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
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2 Heightman, Tom D.; Berdini, Valerio; Bevan, Luke; Buck, Ildiko M.; Carr, Maria G.; Courtin, Aurelie; Coyle, Joseph E.; Day, James E. H.; East, Charlotte; Fazal, Lynsey; Griffiths-Jones, Charlotte M.; Howard, Steven; Kucia-Tran, Justyna; Martins, Vanessa; Muench, Sandra; Munck, Joanne M.; Norton, David; O'Reilly, Marc; Palmer, Nicholas; Pathuri, Puja; Peakman, Torren M.; Reader, Michael; Rees, David C.; Rich, Sharna J.; Shah, Alpesh; Wallis, Nicola G.; Walton, Hugh; Wilsher, Nicola E.; Woolford, Alison J-A; Cooke, Michael; Cousin, David; Onions, Stuart; Shannon, Jonathan; Watts, John; Murray, Christopher W. 分享 收藏
ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK Munck, Joanne M.; Berdini, Valerio; Bevan, Luke; Brothwood, Jessica L.; Castro, Juan; Courtin, Aurelie; East, Charlotte; Ferraldeschi, Roberta; Heightman, Tom D.; Hindley, Christopher J.; Kucia-Tran, Justyna; Lyons, John F.; Martins, Vanessa; Muench, Sandra; Murray, Christopher W.; Norton, David; O'Reilly, Marc; Reader, Michael; Rees, David C.; Rich, Sharna J.; Richardson, Caroline J.; Shah, Alpesh D.; Stanczuk, Lukas; Thompson, Neil T.; Wilsher, Nicola E.; Woolford, Alison J-A; Wallis, Nicola G. 分享 收藏
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Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction Heightman, Tom D.; Callahan, James F.; Chiarparin, Elisabetta; Coyle, Joseph E.; Griffiths-Jones, Charlotte; Lakdawala, Ami S.; McMenamin, Rachel; Mortenson, Paul N.; Norton, David; Peakman, Torren M.; Rich, Sharna J.; Richardson, Caroline; Rumsey, William L.; Sanchez, Yolanda; Saxty, Gordon; Willems, Henriette M. G.; Wolfe, Lawrence, III; Woolford, Alison J. -A.; Wu, Zining; Yan, Hongxing; Kerns, Jeffrey K.; Davis, Thomas G. 分享 收藏
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A novel ERK1/2 inhibitor has potent activity in KRAS-mutant non-small cell lung cancer models Courtin, Aurelie; Bevan, Luke; Heightman, Tom; Kidane, Birikiti; Kucia-Tran, Justyna; Lyons, John; Muench, Sandra; Shah, Alpesh; Stanczuk, Lukas; Thompson, Neil; Wallis, Nicola; Wilsher, Nicola; Munck, Joanne 分享 收藏
Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition Lebraud, Honorine; Noble, Richard A.; Phillips, Nicole; Heam, Keisha; Castro, Juan; Zhao, Yan; Newell, David R.; Lunec, John; Wedge, Stephen R.; Heightman, Tom D. 分享 收藏
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2 Heightman, Tom D.; Berdini, Valerio; Braithwaite, Hannah; Buck, Ildiko M.; Cassidy, Megan; Castro, Juan; Courtin, Aurelie; Day, James E. H.; East, Charlotte; Fazal, Lynsey; Graham, Brent; Griffiths-Jones, Charlotte M.; Lyons, John F.; Martins, Vanessa; Muench, Sandra; Munck, Joanne M.; Norton, David; O'Reilly, Marc; Palmer, Nick; Pathuri, Puja; Reader, Michael; Rees, David C.; Rich, Sharna J.; Richardson, Caroline; Saini, Harpreet; Thompson, Neil T.; Wallis, Nicola G.; Walton, Hugh; Wilsher, Nicola E.; Woolford, Alison J. -A.; Cooke, Michael; Cousin, David; Onions, Stuart; Shannon, Jonathan; Watts, John; Murray, Christopher W. 分享 收藏
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Fragment-based discovery of a highly potent, orally bioavailable ERK1/2 inhibitor that modulates the phosphorylation and catalytic activity of ERK1/2 Heightman, Tom D.; Berdini, Valerio; Braithwaite, Hannah; Buck, Ildiko; Cassidy, Megan; Castro, Juan; Courtin, Aurelie; Day, James; East, Charlotte; Fazal, Lynsey; Graham, Brent; Griffiths-Jones, Charlotte; Lyons, John; Martins, Vanessa; Muench, Sandra; Munck, Joanne; Norton, David; O'Reilly, Marc; Palmer, Nick; Pathuri, Puja; Reader, Mike; Rees, David; Rich, Sharna; Richardson, Caroline; Saini, Harpreet; Thompson, Neil; Wallis, Nicola; Walton, Hugh; Wilsher, Nicola; Woolford, Alison; Murray, Chris 分享 收藏
Characterization of a novel ERK1/2 inhibitor, which modulates the phosphorylation and catalytic activity of ERK1/2 Munck, Joanne M.; Berdini, Valerio; Bevan, Luke D.; Braithwaite, Hannah; Buck, Ildiko M.; Cassidy, Megan; Castro, Juan; Courtin, Aurelie; Day, James E.; East, Charlotte; Fazal, Lynsey; Graham, Brent; Griffiths-Jones, Charlotte M.; Heightman, Tom D.; Hindley, Chris J.; Kidane, Birikiti; Kucia-Tran, Justyna; Lyons, John F.; Martins, Vanessa; Muench, Sandra; Murray, Chris W.; Norton, David; O'Reilly, Marc; Palmer, Nick; Pathuri, Puja; Reader, Mike; Rees, David C.; Rich, Sharna J.; Richardson, Caroline J.; Saini, Harpreet K.; Shah, Alpesh; Stanczuk, Lukas; Thompson, Neil T.; Walton, Hugh; Wilsher, Nicola E.; Woolford, Alison J.; Wallis, Nicola G. 分享 收藏
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Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP) Tamanini, Emiliano; Buck, Ildiko M.; Chessari, Gianni; Chiarparin, Elisabetta; Day, James E. H.; Frederickson, Martyn; Griffiths-Jones, Charlotte M.; Hearn, Keisha; Heightman, Tom D.; Iqbal, Aman; Johnson, Christopher N.; Lewis, Edward J.; Martins, Vanessa; Peakman, Torren; Reader, Michael; Rich, Sharna J.; Ward, George A.; Williams, Pamela A.; Wilsher, Nicola E. 分享 收藏
Visualization of Endogenous ERK1/2 in Cells with a Bioorthogonal Covalent Probe Sipthorp, James; Lebraud, Honorine; Gilley, Rebecca; Kidger, Andrew M.; Okkenhaug, Hanneke; Saba-El-Lei, Marc; Meloche, Sylvain; Caunt, Christopher J.; Cook, Simon J.; Heightman, Tom D. 分享 收藏
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