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ID: ALA2384992
Journal: Bioorg Med Chem Lett
Title: Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Authors: Xiao D, Palani A, Huang X, Sofolarides M, Zhou W, Chen X, Aslanian R, Guo Z, Fossetta J, Tian F, Trivedi P, Spacciapoli P, Whitehurst CE, Lundell D.
Abstract: Conformation restriction of linear N-alkylanilide MK2 inhibitors to their E-conformer was developed. This strategy enabled rapid advance in identifying a series of potent non-ATP competitive inhibitors that exhibited cell based activity in anti-TNFα assay.
CiteXplore: 23602398