High throughput application of the NanoBiT Biochemical Assay for the discovery of selective inhibitors of the interaction of PI3K-p110α with KRAS by Mohamed Ismail, Gareth Davies, Graham Sproat, Tiziana Monteverde, Jonathan Tart, Marta Acebrón-García-de-Eulate, Andrea Gohlke, David Hancock, Santosh Adhikari, Sandra Stefanovic-Barrett, David M Smith, Vikki Flemington, Emma S. Gleave-Hanford, Geoffrey A. Holdgate, Jason G. Kettle, Julian Downward

Get full text

Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC by Thomas G. Hayhow, Beth Williamson, Mandy Lawson, Natalie Cureton, Erin L. Braybrooke, Andrew Campbell, Rodrigo J. Carbajo, Azadeh Cheraghchi-Bashi, Elisabetta Chiarparin, Coura R. Diène, Charlene Fallan, David I. Fisher, Frederick W. Goldberg, Lorna Hopcroft, Philip Hopcroft, Anne Jackson, Jason G. Kettle, Teresa Klinowska, Ulrike Künzel, Gillian Lamont, Hilary J. Lewis, Gareth Maglennon, Scott Martin, Pablo Morentin Gutierrez, Christopher J. Morrow, Myria Nikolaou, J. Willem M. Nissink, Patrick O’Shea, Radoslaw Polanski, Markus Schade, James S. Scott, Aaron Smith, Judith Weber, Joanne Wilson, Bin Yang, Claire Crafter

Get full text

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia by Adriana E. Tron, Matthew A. Belmonte, Ammar Adam, Brian M. Aquila, Lawrence H. Boise, Elisabetta Chiarparin, Justin Cidado, Kevin J. Embrey, Eric Gangl, Francis D. Gibbons, Gareth P. Gregory, David Hargreaves, J. Adam Hendricks, Jeffrey W. Johannes, Ricky W. Johnstone, Steven L. Kazmirski, Jason G. Kettle, Michelle L. Lamb, Shannon M. Matulis, Ajay K. Nooka, Martin J. Packer, Bo Peng, Philip B. Rawlins, Daniel W. Robbins, Alwin G. Schuller, Nancy Su, Wenzhan Yang, Qing Ye, Xiaolan Zheng, J. Paul Secrist, Edwin A. Clark, David M. Wilson, Stephen E. Fawell, Alexander W. Hird

Get full text