Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug ...

ID: ALA3797138

Journal: J Med Chem

Title: Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.

Authors: Han W, Ding Y, Xu Y, Pfister K, Zhu S, Warne B, Doyle M, Aikawa M, Amiri P, Appleton B, Stuart DD, Fanidi A, Shafer CM.

Abstract: The discovery of a highly potent and selective small molecule inhibitor 9 for in vitro target validation of MNK1/2 kinases is described. The aminopyrazine benzimidazole series was derived from an HTS hit and optimized by utilization of a docking model, conformation analysis, and binding pocket comparison against antitargets.

CiteXplore: 27002243

DOI: 10.1021/acs.jmedchem.5b01657

Patent ID: ┄