Publication | Open Access
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design
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Citations
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References
2016
Year
Drug TargetPotent InhibitorMolecular BiologyChemical BiologyPharmaceutical ChemistryMedicinal ChemistryReceptor Tyrosine KinaseVitro Target ValidationStructure-based Drug DesignMechanism Of ActionHts HitDrug DevelopmentPharmacologyMolecular DockingAminopyrazine Benzimidazole SeriesNatural SciencesRational Drug DesignSystems BiologyMedicineSmall MoleculesDrug Discovery
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.
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