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

DCCCyB,GlyT1,Inhibitor,PET tracer ligand,structure−activity relationship

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