Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors

por Lainchbury, Michael, Matthews, Thomas P., McHardy, Tatiana, Boxall, Kathy J., Walton, Michael I., Eve, Paul D., Hayes, Angela, Valenti, Melanie R., de Haven Brandon, Alexis K., Box, Gary, Aherne, G. Wynne, Reader, John C., Raynaud, Florence I., Eccles, Suzanne A., Garrett, Michelle D., Collins, Ian
Publicado 2012

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma

por Walton, Mike I., Eve, Paul D., Hayes, Angela, Henley, Alan T., Valenti, Melanie R., De Haven Brandon, Alexis K., Box, Gary, Boxall, Kathy J., Tall, Matthew, Swales, Karen, Matthews, Thomas P., McHardy, Tatiana, Lainchbury, Michael, Osborne, James, Hunter, Jill E., Perkins, Neil D., Aherne, G. Wynne, Reader, John C., Raynaud, Florence I., Eccles, Suzanne A., Collins, Ian, Garrett, Michelle D.
Publicado 2015

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

por Faisal, Amir, Mak, Grace W Y, Gurden, Mark D, Xavier, Cristina P R, Anderhub, Simon J, Innocenti, Paolo, Westwood, Isaac M, Naud, Sébastien, Hayes, Angela, Box, Gary, Valenti, Melanie R, De Haven Brandon, Alexis K, O'Fee, Lisa, Schmitt, Jessica, Woodward, Hannah L, Burke, Rosemary, vanMontfort, Rob L M, Blagg, Julian, Raynaud, Florence I, Eccles, Suzanne A, Hoelder, Swen, Linardopoulos, Spiros
Publicado 2017

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

por Harnden, Alice C., Davis, Owen A., Box, Gary M., Hayes, Angela, Johnson, Louise D., Henley, Alan T., de Haven Brandon, Alexis K., Valenti, Melanie, Cheung, Kwai-Ming J., Brennan, Alfie, Huckvale, Rosemary, Pierrat, Olivier A., Talbot, Rachel, Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, de Klerk, Selby, McAndrew, Peter Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2023

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

por Huckvale, Rosemary, Harnden, Alice C., Cheung, Kwai-Ming J., Pierrat, Olivier A., Talbot, Rachel, Box, Gary M., Henley, Alan T., de Haven Brandon, Alexis K., Hallsworth, Albert E., Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, Hayes, Angela, Gunnell, Emma A., Brennan, Alfie, Davis, Owen A., Johnson, Louise D., de Klerk, Selby, McAndrew, Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2022