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Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H. Levell J, et al. Among authors: czekaj m. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW. Guertin KR, et al. Among authors: czekaj m. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4. doi: 10.1016/s0960-894x(02)00213-5. Bioorg Med Chem Lett. 2002. PMID: 12039587
Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II.
Barberis C, Moorcroft N, Pribish J, Tserlin E, Gross A, Czekaj M, Barrague M, Erdman P, Majid T, Batchelor J, Levit M, Hebert A, Shen L, Moreno-Mazza S, Wang A. Barberis C, et al. Among authors: czekaj m. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4735-4740. doi: 10.1016/j.bmcl.2017.08.068. Epub 2017 Sep 9. Bioorg Med Chem Lett. 2017. PMID: 28927793
Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.
Barberis C, Erdman P, Czekaj M, Fire L, Pribish J, Tserlin E, Maniar S, Batchelor JD, Liu J, Patel VF, Hebert A, Levit M, Wang A, Sun F, Huang SA. Barberis C, et al. Among authors: czekaj m. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127625. doi: 10.1016/j.bmcl.2020.127625. Epub 2020 Oct 20. Bioorg Med Chem Lett. 2020. PMID: 33096160
Design of a new class of orally active fibrinogen receptor antagonists.
Klein SI, Molino BF, Czekaj M, Gardner CJ, Chu V, Brown K, Sabatino RD, Bostwick JS, Kasiewski C, Bentley R, Windisch V, Perrone M, Dunwiddie CT, Leadley RJ. Klein SI, et al. Among authors: czekaj m. J Med Chem. 1998 Jul 2;41(14):2492-502. doi: 10.1021/jm9801096. J Med Chem. 1998. PMID: 9651154
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