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"Addition" and "Subtraction": Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors.

Abstract：

: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. 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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Chen X,Giraldes J,Sprague ER,Shakya S,Chen Z,Wang Y,Joud C,Mathieu S,Chen CH,Straub C,Duca J,Hurov K,Yuan Y,Shao W,Touré BB

doi

10.1021/acs.jmedchem.7b00033

subject

Has Abstract

pub_date

2017-03-09 00:00:00

pages

2155-2161

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

60

pub_type

杂志文章

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