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Updated: May 22, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
Published on: April 3, 2026
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors
D Vijay Kumar1, Christophe Hoarau, Matthew Bursavich
1Department of Medicinal Chemistry, Myrexis Inc., 305 Chipeta Way, Salt Lake City, UT 84108, USA. dvijayku@hotmail.com
Abstract:
Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter. Mps1 biochemical activity and cytotoxicity in HCT-116 cell line were improved. On-target activity confirmation via mechanism based G2/M escape assay was demonstrated. Physico-chemical and ADME properties were optimized to improve oral bioavailability in mouse.
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