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283 results

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Page 1
Evaluation of endo- and exo-aryl-substitutions and central scaffold modifications on diphenyl substituted alkanes as 5-lipoxygenase activating protein inhibitors.
Chu L, Armstrong HM, Chang LL, Cheng AF, Colwell L, Cui J, Evans J, Galka A, Goulet MT, Hayes N, Lo J, Menke J, Ok HO, Ondeyka DL, Patel M, Quaker GM, Sings H, Witkin SL, Zhao A, Ujjainwalla F. Chu L, et al. Among authors: menke j. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4133-8. doi: 10.1016/j.bmcl.2012.04.064. Epub 2012 Apr 20. Bioorg Med Chem Lett. 2012. PMID: 22578458
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
de Vicente J, Lemoine R, Bartlett M, Hermann JC, Hekmat-Nejad M, Henningsen R, Jin S, Kuglstatter A, Li H, Lovey AJ, Menke J, Niu L, Patel V, Petersen A, Setti L, Shao A, Tivitmahaisoon P, Vu MD, Soth M. de Vicente J, et al. Among authors: menke j. Bioorg Med Chem Lett. 2014 Nov 1;24(21):4969-75. doi: 10.1016/j.bmcl.2014.09.031. Epub 2014 Sep 21. Bioorg Med Chem Lett. 2014. PMID: 25262541
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
Lynch SM, DeVicente J, Hermann JC, Jaime-Figueroa S, Jin S, Kuglstatter A, Li H, Lovey A, Menke J, Niu L, Patel V, Roy D, Soth M, Steiner S, Tivitmahaisoon P, Vu MD, Yee C. Lynch SM, et al. Among authors: menke j. Bioorg Med Chem Lett. 2013 May 1;23(9):2793-800. doi: 10.1016/j.bmcl.2013.02.012. Epub 2013 Feb 13. Bioorg Med Chem Lett. 2013. PMID: 23540648
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S, He Y, Hekmat-Nejad M, Hendricks T, Henningsen R, Hilgenkamp R, Ho H, Hoffman A, Hsu PY, Hu DQ, Itano A, Jaime-Figueroa S, Jahangir A, Jin S, Kuglstatter A, Kutach AK, Liao C, Lynch S, Menke J, Niu L, Patel V, Railkar A, Roy D, Shao A, Shaw D, Steiner S, Sun Y, Tan SL, Wang S, Vu MD. Soth M, et al. Among authors: menke j. J Med Chem. 2013 Jan 10;56(1):345-56. doi: 10.1021/jm301646k. Epub 2012 Dec 19. J Med Chem. 2013. PMID: 23214979
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.
Lucas MC, Bhagirath N, Chiao E, Goldstein DM, Hermann JC, Hsu PY, Kirchner S, Kennedy-Smith JJ, Kuglstatter A, Lukacs C, Menke J, Niu L, Padilla F, Peng Y, Polonchuk L, Railkar A, Slade M, Soth M, Xu D, Yadava P, Yee C, Zhou M, Liao C. Lucas MC, et al. Among authors: menke j. J Med Chem. 2014 Mar 27;57(6):2683-91. doi: 10.1021/jm401982j. Epub 2014 Feb 26. J Med Chem. 2014. PMID: 24520947
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villaseñor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC. Padilla F, et al. Among authors: menke j. J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12. J Med Chem. 2013. PMID: 23350847
Metal impurities cause false positives in high-throughput screening campaigns.
Hermann JC, Chen Y, Wartchow C, Menke J, Gao L, Gleason SK, Haynes NE, Scott N, Petersen A, Gabriel S, Vu B, George KM, Narayanan A, Li SH, Qian H, Beatini N, Niu L, Gan QF. Hermann JC, et al. Among authors: menke j. ACS Med Chem Lett. 2012 Dec 12;4(2):197-200. doi: 10.1021/ml3003296. eCollection 2013 Feb 14. ACS Med Chem Lett. 2012. PMID: 24900642 Free PMC article.
Selective inhibition of spleen tyrosine kinase (SYK) with a novel orally bioavailable small molecule inhibitor, RO9021, impinges on various innate and adaptive immune responses: implications for SYK inhibitors in autoimmune disease therapy.
Liao C, Hsu J, Kim Y, Hu DQ, Xu D, Zhang J, Pashine A, Menke J, Whittard T, Romero N, Truitt T, Slade M, Lukacs C, Hermann J, Zhou M, Lucas M, Narula S, DeMartino J, Tan SL. Liao C, et al. Among authors: menke j. Arthritis Res Ther. 2013 Oct 4;15(5):R146. doi: 10.1186/ar4329. Arthritis Res Ther. 2013. PMID: 24286216 Free PMC article.
283 results