Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of Glyt1

Wesley P. Blackaby,Richard T. Lewis,Joanne L. Thomson, Andrew S. R. Jennings,Simon C. Goodacre,Leslie J. Street,Angus M. MacLeod,Andrew Pike,Suzanne Wood,Steve Thomas, Terry A. Brown,Alison Smith,Gopalan Pillai,Sarah Almond,Martin R. Guscott,H. Donald Burns,Waisi Eng,Christine Ryan,Jacquelynn Cook,Terence G. Hamill

ACS medicinal chemistry letters（2010）

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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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