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Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors .
Podoll T, Pearson PG, Kaptein A, Evarts J, de Bruin G, Emmelot-van Hoek M, de Jong A, van Lith B, Sun H, Byard S, Fretland A, Hoogenboom N, Barf T, Slatter JG. Podoll T, et al. Among authors: emmelot van hoek m. J Pharmacol Exp Ther. 2023 Jan;384(1):173-186. doi: 10.1124/jpet.122.001116. Epub 2022 Oct 30. J Pharmacol Exp Ther. 2023. PMID: 36310034
Discovery of quinoline-based irreversible BTK inhibitors.
de Bruin G, Demont D, de Zwart E, Verkaik S, Hoogenboom N, van de Kar B, van Lith B, Emmelot-van Hoek M, Gulrajani M, Covey T, Kaptein A, Barf T. de Bruin G, et al. Among authors: emmelot van hoek m. Bioorg Med Chem Lett. 2020 Jul 15;30(14):127261. doi: 10.1016/j.bmcl.2020.127261. Epub 2020 May 13. Bioorg Med Chem Lett. 2020. PMID: 32527559