未登录 Metabolism-driven in vitro/in vivo disconnect of an oral ERα VHL-PROTAC Hayhow, Thomas G.; Williamson, Beth; Lawson, Mandy; Cureton, Natalie; Braybrooke, Erin L.; Campbell, Andrew; Carbajo, Rodrigo J.; Cheraghchi-Bashi, Azadeh; Chiarparin, Elisabetta; Diene, Coura R.; Fallan, Charlene; Fisher, David I.; Goldberg, Frederick W.; Hopcroft, Lorna; Hopcroft, Philip; Jackson, Anne; Kettle, Jason G.; Klinowska, Teresa; Kuenzel, Ulrike; Lamont, Gillian; Lewis, Hilary J.; Maglennon, Gareth; Martin, Scott; Gutierrez, Pablo Morentin; Morrow, Christopher J.; Nikolaou, Myria; Nissink, J. Willem M.; O'Shea, Patrick; Polanski, Radoslaw; Schade, Markus; Scott, James S.; Smith, Aaron; Weber, Judith; Wilson, Joanne; Yang, Bin; Crafter, Claire 分享 收藏
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390 Pike, Kurt G.; Hunt, Thomas A.; Barlaam, Bernard; Benstead, David; Cadogan, Elaine; Chen, Kan; Cook, Calum R.; Colclough, Nicola; Deng, Chao; Durant, Stephen T.; Eatherton, Andrew; Goldberg, Kristin; Johnstro''m, Peter; Liu, Libin; Liu, Zhaoqun; Nissink, J. Willem M.; Pang, Chengling; Pass, Martin; Robb, Graeme R.; Roberts, Caroline; Schou, Magnus; Steward, Oliver; Sykes, Andy; Yan, Yumei; Zhai, Baochang; Zheng, Li 分享 收藏
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models (vol 62, pg 6540, 2019) Finlay, M. Raymond V.; Anderton, Mark; Bailey, Andrew; Boyd, Scott; Brookfield, Joanna; Cairnduff, Ceri; Charles, Mark; Cheasty, Anne; Critchlow, Susan E.; Culshaw, Janet; Debreczeni, Judit; Ekwuru, Tennyson; Hollingsworth, Ian; Jones, Neil; Leroux, Fred; Littleson, Mairi; McCarron, Hollie; McKelvie, Jennifer; Mooney, Lorraine; Nissink, J. Willem M.; Patel, Joe; Perkins, David; Powell, Steve; Quesada, Mar Jimenez; Raubo, Piotr; Sabin, Verity; Smith, James; Smith, Peter D.; Stark, Andrew; Ting, Attilla; Wang, Peng; Wilson, Zena; Winter-Holt, Jon J.; Wood, J. Matthew; Wrigley, Gail L.; Yu, Guoqing; Zhang, Peng 分享 收藏
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Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists Scott, James S.; Stead, Darren; Barlaam, Bernard; Breed, Jason; Carbajo, Rodrigo J.; Chiarparin, Elisabetta; Cureton, Natalie; Davey, Paul R. J.; Fisher, David I.; Gangl, Eric T.; Grebe, Tyler; Greenwood, Ryan D.; Hande, Sudhir; Hatoum-Mokdad, Holia; Hughes, Samantha J.; Hunt, Thomas A.; Johnson, Tony; Kavanagh, Stefan L.; Klinowska, Teresa C. M.; Larner, Carrie J. B.; Lawson, Mandy; Lister, Andrew S.; Longmire, David; Marden, Stacey; McGuire, Thomas M.; McMillan, Caroline; McMurray, Lindsay; Morrow, Christopher J.; Nissink, J. Willem M.; Moss, Thomas A.; O'Donovan, Daniel H.; Polanski, Radoslaw; Stokes, Stephen; Thakur, Kumar; Trueman, Dawn; Truman, Caroline; Tucker, Michael J.; Wang, Haixia; Whalley, Nicky; Wu, Dedong; Wu, Ye; Yang, Bin; Yang, Wenzhan 分享 收藏
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Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy McCoull, William; Boyd, Scott; Brown, Martin R.; Coen, Muireann; Collingwood, Olga; Davies, Nichola L.; Doherty, Ann; Fairley, Gary; Goldberg, Kristin; Hardaker, Elizabeth; He, Guang; Hennessy, Edward J.; Hopcroft, Philip; Hodgson, George; Jackson, Anne; Jiang, Xiefeng; Karmokar, Ankur; Laine, Anne-Laure; Lindsay, Nicola; Mao, Yumeng; Markandu, Roshini; McMurray, Lindsay; McLean, Neville; Mooney, Lorraine; Musgrove, Helen; Nissink, J. Willem M.; Pflug, Alexander; Reddy, Venkatesh Pilla; Rawlins, Philip B.; Rivers, Emma; Schimpl, Marianne; Smith, Graham F.; Tentarelli, Sharon; Travers, Jon; Troup, Robert, I; Walton, Josephine; Wang, Cheng; Wilkinson, Stephen; Williamson, Beth; Winter-Holt, Jon; Yang, Dejian; Zheng, Yuting; Zhu, Qianxiu; Smith, Paul D. 分享 收藏
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy Nissink, J. Willem M.; Bazzaz, Sana; Blackett, Carolyn; Clark, Matthew A.; Collingwood, Olga; Disch, Jeremy S.; Gikunju, Diana; Goldberg, Kristin; Guilinger, John P.; Hardaker, Elizabeth; Hennessy, Edward J.; Jetson, Rachael; Keefe, Anthony D.; McCoull, William; McMurray, Lindsay; Olszewski, Allison; Overman, Ross; Pflug, Alexander; Preston, Marian; Rawlins, Philip B.; Rivers, Emma; Schimpl, Marianne; Smith, Paul; Truman, Caroline; Underwood, Elizabeth; Warwicker, Juli; Winter-Holt, Jon; Woodcock, Simon; Zhang, Ying 分享 收藏
Nuisance compounds in cellular assays Dahlin, Jayme L.; Auld, Douglas S.; Rothenaigner, Ina; Haney, Steve; Sexton, Jonathan Z.; Nissink, J. Willem M.; Walsh, Jarrod; Lee, Jonathan A.; Strelow, John M.; Willard, Francis S.; Ferrins, Lori; Baell, Jonathan B.; Walters, Michael A.; Hua, Bruce K.; Hadian, Kamyar; Wagner, Bridget K. 分享 收藏
A-loop interactions in Mer tyrosine kinase give rise to inhibitors with two-step mechanism and long residence time of binding Pflug, Alexander; Schimpl, Marianne; Nissink, J. Willem M.; Overman, Ross C.; Rawlins, Philip B.; Truman, Caroline; Underwood, Elizabeth; Warwicker, Juli; Winter-Holt, Jon; McCoull, William 分享 收藏
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist Scott, James S.; Moss, Thomas A.; Balazs, Amber; Barlaam, Bernard; Breed, Jason; Carbajo, Rodrigo J.; Chiarparin, Elisabetta; Davey, Paul R. J.; Delpuech, Oona; Fawell, Stephen; Fisher, David, I; Gagrica, Sladjana; Gangl, Eric T.; Grebe, Tyler; Greenwood, Ryan D.; Hande, Sudhir; Hatoum-Mokdad, Holia; Herlihy, Kara; Hughes, Samantha; Hunt, Thomas A.; Hoan Huynh; Janbon, Sophie L. M.; Johnson, Tony; Kavanagh, Stefan; Klinowska, Teresa; Lawson, Mandy; Lister, Andrew S.; Marden, Stacey; McGinnity, Dermot F.; Morrow, Christopher J.; Nissink, J. Willem M.; O'Donovan, Daniel H.; Peng, Bo; Polanski, Radoslaw; Stead, Darren S.; Stokes, Stephen; Thakur, Kumar; Throner, Scott R.; Tucker, Michael J.; Varnes, Jeffrey; Wang, Haixia; Wilson, David M.; Wu, Dedong; Wu, Ye; Yang, Bin; Yang, Wenzhan 分享 收藏
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry Scott, James S.; Breed, Jason; Carbajo, Rodrigo J.; Davey, Paul R.; Greenwood, Ryan; Huynh, Hoan K.; Klinowska, Teresa; Morrow, Christopher J.; Moss, Thomas A.; Polanski, Radoslaw; Nissink, J. Willem M.; Varnes, Jeffrey; Yang, Bin 分享 收藏
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Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models Finlay, M. Raymond V.; Anderton, Mark; Bailey, Andrew; Boyd, Scott; Brookfield, Joanna; Cairnduff, Ceri; Charles, Mark; Cheasty, Anne; Critchlow, Susan E.; Culshaw, Janet; Ekwuru, Tennyson; Hollingsworth, Ian; Jones, Neil; Leroux, Fred; Littleson, Mairi; McCarron, Hollie; McKelvie, Jennifer; Mooney, Lorraine; Nissink, J. Willem M.; Perkins, David; Powell, Steve; Quesada, Mar Jimenez; Raubo, Piotr; Sabin, Verity; Smith, James; Smith, Peter D.; Stark, Andrew; Ting, Attilla; Wang, Peng; Wilson, Zena; Winter-Holt, Jon J.; Wood, J. Matthew; Wrigley, Gail L.; Yu, Guoqing; Zhang, Peng 分享 收藏
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent 共济失调毛细血管扩张症突变和Rad3相关 (ATR) 激酶的有效抑制剂AZD6738的发现和表征，并用作抗癌剂 Foote, Kevin M.; Nissink, J. Willem M.; McGuire, Thomas; Turner, Paul; Guichard, Sylvie; Yates, James W. T.; Lau, Alan; Blades, Kevin; Heathcote, Dan; Odedra, Rajesh; Wilkinson, Gary; Wilson, Zena; Wood, Christine M.; Jewsbury, Philip J. 分享 收藏
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Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site Exell, Jack C.; Thompson, Mark J.; Finger, L. David; Shaw, Steven J.; Debreczeni, Judit; Ward, Thomas A.; McWhirter, Claire; Sioberg, Catrine L. B.; Molina, Daniel Martinez; Abbott, W. Mark; Jones, Clifford D.; Nissink, J. Willem M.; Durant, Stephen T.; Grasby, Jane A. 分享 收藏
Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival Kettle, Jason G.; Alwan, Husam; Bista, Michal; Breed, Jason; Davies, Nichola L.; Eckersley, Kay; Fillery, Shaun; Foote, Kevin M.; Goodwin, Louise; Jones, David R.; Kaeck, Helena; Lau, Alan; Nissink, J. Willem M.; Read, Jon; Scott, James S.; Taylor, Ben; Walker, Graeme; Wissler, Lisa; Wylot, Marta 分享 收藏
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