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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 Share Save
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Discovery of potent and selective pan-TEAD autopalmitoylation inhibitors for the treatment of Hippo-pathway altered cancers Gordon, Jacob A.; Dubauskaite, Jolanta; DuPont, Michelle; Guan, Nin; Holdgate, Geoff; Mlynarski, Scott; Umbreit, Neil; Sanchez, Danielle; Srivastava, Abhishek; Suski, Janek; Su, Nancy; Richards, Ryan; Cosulich, Sabina; Reimer, Corinne; Brownell, James Share Save
PLEKHS1 drives PI3Ks and remodels pathway homeostasis in PTEN-null prostate Chessa, Tamara A. M.; Jung, Piotr; Anwar, Arqum; Suire, Sabine; Anderson, Karen E.; Barneda, David; Kielkowska, Anna; Sadiq, Barzan A.; Lai, Ieng Wai; Felisbino, Sergio; Turnham, Daniel J.; Pearson, Helen B.; Phillips, Wayne A.; Sasaki, Junko; Sasaki, Takehiko; Oxley, David; Spensberger, Dominik; Segonds-Pichon, Anne; Wilson, Michael; Walker, Simon; Okkenhaug, Hanneke; Cosulich, Sabina; Hawkins, Phillip T.; Stephens, Len R. Share Save
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration Kettle, Jason G.; Bagal, Sharan K.; Barratt, Derek; Bodnarchuk, Michael S.; Boyd, Scott; Braybrooke, Erin; Breed, Jason; Cassar, Doyle J.; Cosulich, Sabina; Davies, Michael; Davies, Nichola L.; Deng, Chao; Eatherton, Andrew; Evans, Laura; Feron, Lyman J.; Fillery, Shaun; Gleave, Emma S.; Goldberg, Frederick W.; Gonzalez, Miguel A. Cortes; Guerot, Carine; Haider, Afreen; Harlfinger, Stephanie; Howells, Rachel; Jackson, Anne; Johnstrom, Peter; Kemmitt, Paul D.; Koers, Alex; Kondrashov, Mikhail; Lamont, Gillian M.; Lamont, Scott; Lewis, Hilary J.; Liu, Libin; Mylrea, Megan; Nash, Samuel; Niedbala, Michael J.; Peter, Alison; Phillips, Christopher; Pike, Kurt; Raubo, Piotr; Robb, Graeme R.; Ross, Sarah; Sanders, Matthew G.; Schou, Magnus; Simpson, Iain; Steward, Oliver Share Save
A highly sensitive and specific PARylation assay confirms significant and durable target engagement by AZD5305 in patients Lombardi, Benedetta; Marco-Casanova, Paola; Karapetsas, Athanasios; Hornett, Mya; Lukacs, Edit; Sugibayashi, Ko; Cosulich, Sabina; Dowson, Adam; Moorthy, Ganesh; Brown, Jessica; Yap, Timothy A.; Schram, Alison M.; Balmana, Judith; Luen, Stephen J.; Im, Seock-Ah; Sharp, Adam; Baird, Richard; Harrington, Elizabeth A.; Linardopoulos, Spiros Share Save
Preclinical evaluation of a novel B7-H4 targeted antibody-drug conjugate AZD8205 as a single agent and in combination with novel PARP inhibitor and checkpoint blockade Cazes, Alex; Kinneer, Krista; Omar, Bilal; Chesebrough, Jon; Anderton, Judith; Wang, Jixin; Staniszewska, Anna D.; Arbitman, Steven; Daita, Kalyani; Desai, Himanshi; Johnson, Yoshimi; Rothstein, Raymond; Gymnopoulos, Marco; Fabbri, Giulia; Cooper, Zachary A.; Albertella, Mark; Hammond, Scott A.; Cosulich, Sabina; Luheshi, Nadia; Sapra, Puja Share Save
Clonal somatic copy number altered driver events inform drug sensitivity in high-grade serous ovarian cancer Martins, Filipe Correia; Couturier, Dominique-Laurent; de Santiago, Ines; Sauer, Carolin Margarethe; Vias, Maria; Angelova, Mihaela; Sanders, Deborah; Piskorz, Anna; Hall, James; Hosking, Karen; Amirthanayagam, Anumithra; Cosulich, Sabina; Carnevalli, Larissa; Davies, Barry; Watkins, Thomas B. K.; Funingana, Ionut G.; Bolton, Helen; Haldar, Krishnayan; Latimer, John; Baldwin, Peter; Crawford, Robin; Eldridge, Matthew; Basu, Bristi; Jimenez-Linan, Mercedes; Mcpherson, Andrew W.; McGranahan, Nicholas; Litchfield, Kevin; Shah, Sohrab P.; McNeish, Iain; Caldas, Carlos; Evan, Gerard; Swanton, Charles; Brenton, James D. Share Save
AZD4625 is a Potent and Selective Inhibitor of KRASG12C Chakraborty, Atanu; Hanson, Lyndsey; Robinson, David; Lewis, Hilary; Bickerton, Sue; Davies, Michael; Polanski, Radoslaw; Whiteley, Rebecca; Koers, Alex; Atkinson, James; Baker, Tamara; Barrantes, Ivan del Barco; Ciotta, Giovanni; Kettle, Jason G.; Magiera, Lukasz; Martins, Carla P.; Peter, Alison; Wigmore, Eleanor; Underwood, Zoe; Cosulich, Sabina; Niedbala, Michael; Ross, Sarah Share Save
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Discovery of AZD4625, a Covalent Allosteric Inhibitor of the MutantGTPase KRASG12C Kettle, Jason G.; Bagal, Sharan K.; Bickerton, Sue; Bodnarchuk, Michael S.; Boyd, Scott; Breed, Jason; Carbajo, Rodrigo J.; Cassar, Doyle J.; Chakraborty, Atanu; Cosulich, Sabina; Cumming, Iain; Davies, Michael; Davies, Nichola L.; Eatherton, Andrew; Evans, Laura; Feron, Lyman; Fillery, Shaun; Gleave, Emma S.; Goldberg, Frederick W.; Hanson, Lyndsey; Harlfinger, Stephanie; Howard, Martin; Howells, Rachel; Jackson, Anne; Kemmitt, Paul; Lamont, Gillian; Lamont, Scott; Lewis, Hilary J.; Liu, Libin; Niedbala, Michael J.; Phillips, Christopher; Polanski, Radek; Raubo, Piotr; Robb, Graeme; Robinson, David M.; Ross, Sarah; Sanders, Matthew G.; Tonge, Michael; Whiteley, Rebecca; Wilkinson, Stephen; Yang, Junsheng; Zhang, Wenman Share Save
Identification and optimization of a novel series of selective PIP5K inhibitors Andrews, David M.; Cartic, Sharon; Cosulich, Sabina; Divecha, Nullin; Faulder, Paul; Flemington, Vikki; Kern, Oliver; Kettle, Jason G.; MacDonald, Ellen; McKelvie, Jennifer; Pike, Kurt G.; Roberts, Bryan; Rowlinson, Rachel; Smith, James M.; Stockley, Martin; Swarbrick, Martin E.; Treinies, Iris; Waring, Michael J. Share Save
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 Share Save
AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib Flemington, Vikki; Davies, Emma J.; Robinson, David; Sandin, Linda C.; Delpuech, Oona; Zhang, Pei; Hanson, Lyndsey; Farrington, Paul; Bell, Sigourney; Falenta, Katarzyna; Gibbons, Francis D.; Lindsay, Nicola; Smith, Aaron; Wilson, Joanne; Roberts, Karen; Tonge, Michael; Hopcroft, Philip; Willis, Sophie E.; Roudier, Martine P.; Rooney, Claire; Coker, Elizabeth A.; Jaaks, Patricia; Garnett, Mathew J.; Fawell, Stephen E.; Jones, Clifford D.; Ward, Richard A.; Simpson, Iain; Cosulich, Sabina C.; Pease, J. Elizabeth; Smith, Paul D. Share Save
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Characterising the in vivo response of lung tumors to KrasG12C inhibition Martins, Carla P.; Bidar, Abdel; Karrberg, Lillevi; Porritt, Michelle; Seeliger, Frank; Whiteley, Rebecca; Hanson, Lyndsey; Hallengren, Liselotte; Hardaker, Elizabeth; Barry, Simon; Maresca, Maresca; Bohlooly, Mohammad; Cosulich, Sabina; Ross, Sarah Share Save
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 Share Save
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