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Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Rohde JM, Karavadhi S, Pragani R, Liu L, Fang Y, Zhang W, McIver A, Zheng H, Liu Q, Davis MI, Urban DJ, Lee TD, Cheff DM, Hollingshead M, Henderson MJ, Martinez NJ, Brimacombe KR, Yasgar A, Zhao W, Klumpp-Thomas C, Michael S, Covey J, Moore WJ, Stott GM, Li Z, Simeonov A, Jadhav A, Frye S, Hall MD, Shen M, Wang X, Patnaik S, Boxer MB. Rohde JM, et al. Among authors: zheng h. J Med Chem. 2021 Apr 22;64(8):4913-4946. doi: 10.1021/acs.jmedchem.1c00019. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33822623 Free PMC article.
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD. Urban DJ, et al. Among authors: zheng h. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.
Zheng H, Zhao J, Li B, Zhang W, Stashko MA, Minson KA, Huey MG, Zhou Y, Earp HS, Kireev D, Graham DK, DeRyckere D, Frye SV, Wang X. Zheng H, et al. Eur J Med Chem. 2021 Aug 5;220:113534. doi: 10.1016/j.ejmech.2021.113534. Epub 2021 May 17. Eur J Med Chem. 2021. PMID: 34038857
Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors.
Kong D, Tian Q, Chen Z, Zheng H, Stashko MA, Yan D, Earp HS, Frye SV, DeRyckere D, Kireev D, Graham DK, Wang X. Kong D, et al. Among authors: zheng h. J Med Chem. 2024 Apr 11;67(7):5866-5882. doi: 10.1021/acs.jmedchem.4c00148. Epub 2024 Mar 31. J Med Chem. 2024. PMID: 38556760
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