Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of Glyt1
ACS medicinal chemistry letters(2010)
摘要
Amalgamation of the structure-activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus monkey as determined by displacement of a PET tracer ligand.
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关键词
Inhibitor,GlyT1,structure-activity relationship,DCCCyB,PET tracer ligand
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