Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

ABSTRACT: 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.

SUBMITTER: Blackaby WP 

PROVIDER: S-EPMC4007840 | biostudies-literature | 2010 Oct

REPOSITORIES: biostudies-literature