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Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Tichenor MS, Wiener JJM, Rao NL, Bacani GM, Wei J, Pooley Deckhut C, Barbay JK, Kreutter KD, Chang L, Clancy KW, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Rui H, Sepassi K, Gaudiano M, Bekkers M, Cornelissen I, Packman K, Seierstad M, Xiouras C, Bembenek SD, Alexander R, Milligan C, Balasubramanian S, Lebsack AD, Venable JD, Philippar U, Edwards JP, Hirst G. Tichenor MS, et al. Among authors: hirst g. J Med Chem. 2022 Nov 10;65(21):14326-14336. doi: 10.1021/acs.jmedchem.2c01026. Epub 2022 Oct 31. J Med Chem. 2022. PMID: 36314537
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
Leonard KA, Madge LA, Krawczuk PJ, Wang A, Kreutter KD, Bacani GM, Chai W, Smith RC, Tichenor MS, Harris MC, Malaviya R, Seierstad M, Johnson ME, Venable JD, Kim S, Hirst GC, Mathur AS, Rao TS, Edwards JP, Rizzolio MC, Koudriakova T. Leonard KA, et al. J Med Chem. 2020 Mar 26;63(6):2915-2929. doi: 10.1021/acs.jmedchem.9b01439. Epub 2020 Mar 16. J Med Chem. 2020. PMID: 32134643
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Hecker SJ, Reddy KR, Totrov M, Hirst GC, Lomovskaya O, Griffith DC, King P, Tsivkovski R, Sun D, Sabet M, Tarazi Z, Clifton MC, Atkins K, Raymond A, Potts KT, Abendroth J, Boyer SH, Loutit JS, Morgan EE, Durso S, Dudley MN. Hecker SJ, et al. J Med Chem. 2015 May 14;58(9):3682-92. doi: 10.1021/acs.jmedchem.5b00127. Epub 2015 Mar 17. J Med Chem. 2015. PMID: 25782055
Fragment-based discovery of JAK-2 inhibitors.
Antonysamy S, Hirst G, Park F, Sprengeler P, Stappenbeck F, Steensma R, Wilson M, Wong M. Antonysamy S, et al. Among authors: hirst g. Bioorg Med Chem Lett. 2009 Jan 1;19(1):279-82. doi: 10.1016/j.bmcl.2008.08.064. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2009. PMID: 19019674
Discovery of thienopyridines as Src-family selective Lck inhibitors.
Abbott L, Betschmann P, Burchat A, Calderwood DJ, Davis H, Hrnciar P, Hirst GC, Li B, Morytko M, Mullen K, Yang B. Abbott L, et al. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1167-71. doi: 10.1016/j.bmcl.2006.12.035. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17234410
312 results