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• W4281718399 abstract "SETD2, a lysine N-methyltransferase, is a histone methyltransferase that plays an important role in various cellular processes and was identified as a target of interest in multiple myeloma that features a t(4,14) translocation. We recently reported the discovery of a novel small-molecule SETD2 inhibitor tool compound that is suitable for preclinical studies. Herein we describe the conformational-design-driven evolution of the advanced chemistry lead, which resulted in compounds appropriate for clinical evaluation. Further optimization of this chemical series led to the discovery of EZM0414, which is a potent, selective, and orally bioavailable inhibitor of SETD2 with good pharmacokinetic properties and robust pharmacodynamic activity in a mouse xenograft model." @default.
• W4281718399 created "2022-06-13" @default.
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• W4281718399 date "2022-06-07" @default.
• W4281718399 modified "2023-09-26" @default.
• W4281718399 title "Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies" @default.
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• W4281718399 doi "https://doi.org/10.1021/acsmedchemlett.2c00167" @default.
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