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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: day je. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA, Weinberg RA, Stegeman RA, Wrightstone A, Christine L, Compton R, Li X. Trujillo JI, et al. Among authors: day je. Bioorg Med Chem Lett. 2009 Feb 1;19(3):908-11. doi: 10.1016/j.bmcl.2008.11.105. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097791
Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): a tale of two waters.
Trujillo JI, Kiefer JR, Huang W, Day JE, Moon J, Jerome GM, Bono CP, Kornmeier CM, Williams ML, Kuhn C, Rennie GR, Wynn TA, Carron CP, Thorarensen A. Trujillo JI, et al. Among authors: day je. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3795-9. doi: 10.1016/j.bmcl.2012.04.004. Epub 2012 Apr 13. Bioorg Med Chem Lett. 2012. PMID: 22546671
Crystallization and preliminary X-ray diffraction analysis of rat autotaxin.
Day JE, Hall T, Pegg LE, Benson TE, Hausmann J, Kamtekar S. Day JE, et al. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010 Sep 1;66(Pt 9):1127-9. doi: 10.1107/S1744309110030228. Epub 2010 Aug 31. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010. PMID: 20823544 Free PMC article.
Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6.
Chrencik JE, Patny A, Leung IK, Korniski B, Emmons TL, Hall T, Weinberg RA, Gormley JA, Williams JM, Day JE, Hirsch JL, Kiefer JR, Leone JW, Fischer HD, Sommers CD, Huang HC, Jacobsen EJ, Tenbrink RE, Tomasselli AG, Benson TE. Chrencik JE, et al. Among authors: day je. J Mol Biol. 2010 Jul 16;400(3):413-33. doi: 10.1016/j.jmb.2010.05.020. Epub 2010 May 15. J Mol Biol. 2010. PMID: 20478313
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).
Carron CP, Trujillo JI, Olson KL, Huang W, Hamper BC, Dice T, Neal BE, Pelc MJ, Day JE, Rohrer DC, Kiefer JR, Moon JB, Schweitzer BA, Blake TD, Turner SR, Woerndle R, Case BL, Bono CP, Dilworth VM, Funckes-Shippy CL, Hood BL, Jerome GM, Kornmeier CM, Radabaugh MR, Williams ML, Davies MS, Wegner CD, Welsch DJ, Abraham WM, Warren CJ, Dowty ME, Hua F, Zutshi A, Yang JZ, Thorarensen A. Carron CP, et al. Among authors: day je. ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900177 Free PMC article.
Expression, purification, and characterization of TYK-2 kinase domain, a member of the Janus kinase family.
Korniski B, Wittwer AJ, Emmons TL, Hall T, Brown S, Wrightstone AD, Hirsch JL, Gormley JA, Weinberg RA, Leone JW, Day JE, Chrencik JE, Sommers CD, Fischer HD, Tomasselli AG. Korniski B, et al. Among authors: day je. Biochem Biophys Res Commun. 2010 May 28;396(2):543-8. doi: 10.1016/j.bbrc.2010.04.141. Epub 2010 May 8. Biochem Biophys Res Commun. 2010. PMID: 20435017
Expression, purification, characterization and crystallization of non- and phosphorylated states of JAK2 and JAK3 kinase domain.
Hall T, Emmons TL, Chrencik JE, Gormley JA, Weinberg RA, Leone JW, Hirsch JL, Saabye MJ, Schindler JF, Day JE, Williams JM, Kiefer JR, Lightle SA, Harris MS, Guru S, Fischer HD, Tomasselli AG. Hall T, et al. Among authors: day je. Protein Expr Purif. 2010 Jan;69(1):54-63. doi: 10.1016/j.pep.2009.09.011. Epub 2009 Sep 23. Protein Expr Purif. 2010. PMID: 19781647
46 results