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Page 1
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Holsworth DD, Jalaie M, Belliotti T, Cai C, Collard W, Ferreira S, Powell NA, Stier M, Zhang E, McConnell P, Mochalkin I, Ryan MJ, Bryant J, Li T, Kasani A, Subedi R, Maiti SN, Edmunds JJ. Holsworth DD, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3575-80. doi: 10.1016/j.bmcl.2007.04.052. Epub 2007 Apr 25. Bioorg Med Chem Lett. 2007. PMID: 17482464
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Sarver RW, Peevers J, Cody WL, Ciske FL, Dyer J, Emerson SD, Hagadorn JC, Holsworth DD, Jalaie M, Kaufman M, Mastronardi M, McConnell P, Powell NA, Quin J 3rd, Van Huis CA, Zhang E, Mochalkin I. Sarver RW, et al. Among authors: mochalkin i. Anal Biochem. 2007 Jan 1;360(1):30-40. doi: 10.1016/j.ab.2006.10.017. Epub 2006 Oct 30. Anal Biochem. 2007. PMID: 17113558
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ. Powell NA, et al. Among authors: mochalkin i. Bioorg Med Chem. 2007 Sep 1;15(17):5912-49. doi: 10.1016/j.bmc.2007.05.069. Epub 2007 Jun 2. Bioorg Med Chem. 2007. PMID: 17574423
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Van Huis CA, Casimiro-Garcia A, Bigge CF, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Leadley RJ Jr, Narasimhan LS, McClanahan T, Mochalkin I, Pamment M, Peterson JT, Sahasrabudhe V, Schaum RP, Edmunds JJ. Van Huis CA, et al. Among authors: mochalkin i. Bioorg Med Chem. 2009 Mar 15;17(6):2501-11. doi: 10.1016/j.bmc.2009.01.063. Epub 2009 Feb 3. Bioorg Med Chem. 2009. PMID: 19231206
Structure based design of an in vivo active hydroxamic acid inhibitor of P. aeruginosa LpxC.
Warmus JS, Quinn CL, Taylor C, Murphy ST, Johnson TA, Limberakis C, Ortwine D, Bronstein J, Pagano P, Knafels JD, Lightle S, Mochalkin I, Brideau R, Podoll T. Warmus JS, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2536-43. doi: 10.1016/j.bmcl.2012.01.140. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22401863
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B. Qiu H, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2018 Sep 15;28(17):2939-2944. doi: 10.1016/j.bmcl.2018.07.008. Epub 2018 Jul 5. Bioorg Med Chem Lett. 2018. PMID: 30122225
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
Caldwell R, Liu-Bujalski L, Qiu H, Mochalkin I, Jones R, Neagu C, Goutopoulos A, Grenningloh R, Johnson T, Sherer B, Gardberg A, Follis AV, Morandi F, Head J. Caldwell R, et al. Among authors: mochalkin i. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3419-3424. doi: 10.1016/j.bmcl.2018.09.033. Epub 2018 Sep 27. Bioorg Med Chem Lett. 2018. PMID: 30290988
32 results