Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 8, Pages 3611-3625Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b00352
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A weak screening hit with suboptimal physicochemical properties was optimized against PFKFB3 kinase using critical structure-guided insights. The resulting compounds demonstrated high selectivity over related PFKFB isoforms and modulation of the target in a cellular context. A selected example demonstrated exposure in animals following oral dosing. Examples from this series may serve as useful probes to understand the emerging biology of this metabolic target.
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