Discovery of branebrutinib (BMS-986195): a strategy for identifying a highly potent and selective covalent inhibitor providing rapid in vivo inactivation of Bruton's tyrosine kinase (BTK)

Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR & Tino JA
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Watterson, S. H., Liu, Q., Beaudoin Bertrand, M., Batt, D. G., Li, L., Pattoli, M. A., … Tino, J. A. (2019). Discovery of branebrutinib (BMS-986195): a strategy for identifying a highly potent and selective covalent inhibitor providing rapid in vivo inactivation of Bruton's tyrosine kinase (BTK). Journal of Medicinal Chemistry, 62(7), 3228-3250. https://doi.org/10.1021/acs.jmedchem.9b00167