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Page 1
Three mechanistically distinct kinase assays compared: Measurement of intrinsic ATPase activity identified the most comprehensive set of ITK inhibitors.
Kashem MA, Nelson RM, Yingling JD, Pullen SS, Prokopowicz AS 3rd, Jones JW, Wolak JP, Rogers GR, Morelock MM, Snow RJ, Homon CA, Jakes S. Kashem MA, et al. Among authors: jakes s. J Biomol Screen. 2007 Feb;12(1):70-83. doi: 10.1177/1087057106296047. Epub 2006 Dec 8. J Biomol Screen. 2007. PMID: 17166826
Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).
Cywin CL, Zhao BP, McNeil DW, Hrapchak M, Prokopowicz AS, Goldberg DR, Morwick TM, Gao A, Jakes S, Kashem M, Magolda RL, Soll RM, Player MR, Bobko MA, Rinker J, DesJarlais RL, Winters MP. Cywin CL, et al. Among authors: jakes s. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1415-8. doi: 10.1016/s0960-894x(03)00163-x. Bioorg Med Chem Lett. 2003. PMID: 12668002
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.
Goldberg DR, Butz T, Cardozo MG, Eckner RJ, Hammach A, Huang J, Jakes S, Kapadia S, Kashem M, Lukas S, Morwick TM, Panzenbeck M, Patel U, Pav S, Peet GW, Peterson JD, Prokopowicz AS 3rd, Snow RJ, Sellati R, Takahashi H, Tan J, Tschantz MA, Wang XJ, Wang Y, Wolak J, Xiong P, Moss N. Goldberg DR, et al. Among authors: jakes s. J Med Chem. 2003 Apr 10;46(8):1337-49. doi: 10.1021/jm020446l. J Med Chem. 2003. PMID: 12672234
Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.
Morwick T, Berry A, Brickwood J, Cardozo M, Catron K, DeTuri M, Emeigh J, Homon C, Hrapchak M, Jacober S, Jakes S, Kaplita P, Kelly TA, Ksiazek J, Liuzzi M, Magolda R, Mao C, Marshall D, McNeil D, Prokopowicz A 3rd, Sarko C, Scouten E, Sledziona C, Sun S, Watrous J, Wu JP, Cywin CL. Morwick T, et al. Among authors: jakes s. J Med Chem. 2006 May 18;49(10):2898-908. doi: 10.1021/jm0510979. J Med Chem. 2006. PMID: 16686533
Identification of pharmacological inhibitors of the MEK5/ERK5 pathway.
Tatake RJ, O'Neill MM, Kennedy CA, Wayne AL, Jakes S, Wu D, Kugler SZ Jr, Kashem MA, Kaplita P, Snow RJ. Tatake RJ, et al. Among authors: jakes s. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. doi: 10.1016/j.bbrc.2008.09.087. Epub 2008 Oct 1. Biochem Biophys Res Commun. 2008. PMID: 18834865
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Qian K, Wang L, Cywin CL, Farmer BT 2nd, Hickey E, Homon C, Jakes S, Kashem MA, Lee G, Leonard S, Li J, Magboo R, Mao W, Pack E, Peng C, Prokopowicz A 3rd, Welzel M, Wolak J, Morwick T. Qian K, et al. Among authors: jakes s. J Med Chem. 2009 Apr 9;52(7):1814-27. doi: 10.1021/jm801242y. J Med Chem. 2009. PMID: 19256503
56 results