Potent and selective monopolar spindle 1 (Mps1) inhibitor (IC50
= 6.4 nM). Selective for Mps1 over a panel of 95 kinases including JNK. Inhibits A549 lung carcinoma cell proliferation and attenuates A549 cell xenograft growth in mice. Orally active.
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Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation.
Kusakabe et al.
ACS Med.Chem.Lett., 2012;3:560