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Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.
Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: zhang j. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f. J Med Chem. 2010. PMID: 20860370 Free PMC article.
Expanding the diversity of allosteric bcr-abl inhibitors.
Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS. Deng X, et al. Among authors: zhang g, zhang j. J Med Chem. 2010 Oct 14;53(19):6934-46. doi: 10.1021/jm100555f. J Med Chem. 2010. PMID: 20828158 Free PMC article.
Development of ATP-competitive mTOR inhibitors.
Liu Q, Kang SA, Thoreen CC, Hur W, Wang J, Chang JW, Markhard A, Zhang J, Sim T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: zhang j. Methods Mol Biol. 2012;821:447-60. doi: 10.1007/978-1-61779-430-8_29. Methods Mol Biol. 2012. PMID: 22125084 Free PMC article.
Discovery of potent and selective covalent inhibitors of JNK.
Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS. Zhang T, et al. Among authors: zhang j. Chem Biol. 2012 Jan 27;19(1):140-54. doi: 10.1016/j.chembiol.2011.11.010. Chem Biol. 2012. PMID: 22284361 Free PMC article.
Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.
Choi HG, Zhang J, Weisberg E, Griffin JD, Sim T, Gray NS. Choi HG, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5297-302. doi: 10.1016/j.bmcl.2012.06.036. Epub 2012 Jun 23. Bioorg Med Chem Lett. 2012. PMID: 22819762 Free PMC article.
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y, Choi HG, Xie T, Deng X, Buhrlage SJ, Sim T, Cohen P, Sapkota G, Westover KD, Gray NS. Tan L, et al. Among authors: zhang j. J Med Chem. 2015 Jan 8;58(1):183-96. doi: 10.1021/jm500480k. Epub 2014 Jul 30. J Med Chem. 2015. PMID: 25075558 Free PMC article.
A structure-guided approach to creating covalent FGFR inhibitors.
Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS. Zhou W, et al. Among authors: zhang j. Chem Biol. 2010 Mar 26;17(3):285-95. doi: 10.1016/j.chembiol.2010.02.007. Chem Biol. 2010. PMID: 20338520 Free PMC article.
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