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Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile.
Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, van Hoek M, de Zwart E, Mittag D, Demont D, Verkaik S, Krantz F, Pearson PG, Ulrich R, Kaptein A. Barf T, et al. Among authors: de zwart e. J Pharmacol Exp Ther. 2017 Nov;363(2):240-252. doi: 10.1124/jpet.117.242909. Epub 2017 Sep 7. J Pharmacol Exp Ther. 2017. PMID: 28882879
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: de zwart e. 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
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.
Hoogenboom N, Demont D, de Zwart E, Verkaik S, Emmelot M, van de Kar B, Kaptein A, Barf T. Hoogenboom N, et al. Among authors: de zwart e. Bioorg Med Chem Lett. 2021 Nov 15;52:128406. doi: 10.1016/j.bmcl.2021.128406. Epub 2021 Oct 5. Bioorg Med Chem Lett. 2021. PMID: 34624491
Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Oubrie A, Kaptein A, de Zwart E, Hoogenboom N, Goorden R, van de Kar B, van Hoek M, de Kimpe V, van der Heijden R, Borsboom J, Kazemier B, de Roos J, Scheffers M, Lommerse J, Schultz-Fademrecht C, Barf T. Oubrie A, et al. Among authors: de zwart e. Bioorg Med Chem Lett. 2012 Jan 1;22(1):613-8. doi: 10.1016/j.bmcl.2011.10.071. Epub 2011 Nov 3. Bioorg Med Chem Lett. 2012. PMID: 22119462
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Kaptein A, Oubrie A, de Zwart E, Hoogenboom N, de Wit J, van de Kar B, van Hoek M, Vogel G, de Kimpe V, Schultz-Fademrecht C, Borsboom J, van Zeeland M, Versteegh J, Kazemier B, de Roos J, Wijnands F, Dulos J, Jaeger M, Leandro-Garcia P, Barf T. Kaptein A, et al. Among authors: de zwart e. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3823-7. doi: 10.1016/j.bmcl.2011.04.016. Epub 2011 Apr 16. Bioorg Med Chem Lett. 2011. PMID: 21565498