?Addition? and ?Subtraction? [electronic resource] : Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors

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Ngôn ngữ: eng

Ký hiệu phân loại: 547 Organic chemistry

Thông tin xuất bản: Argonne, Ill. : Oak Ridge, Tenn. : Argonne National Laboratory ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2017

Mô tả vật lý: Size: p. 2155-2161 : , digital, PDF file.

Bộ sưu tập: Metadata

ID: 260644

While adding the structural features that are more favored by on-target activity is the more common strategy in selectivity optimization, the opposite strategy of subtracting the structural features that contribute more to off-target activity can also be very effective. Furthermore, reported here is our successful effort of improving the kinase selectivity of type II maternal embryonic leucine zipper kinase inhibitors by applying these two complementary approaches together, which clearly demonstrates the powerful synergy between them.
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