916159-99-4Relevant articles and documents
Identification of an orally bioavailable, potent, and selective inhibitor of GlyT1
Blackaby, Wesley P.,Lewis, Richard T.,Thomson, Joanne L.,Jennings, Andrew S. R.,Goodacre, Simon C.,Street, Leslie J.,MacLeod, Angus M.,Pike, Andrew,Wood, Suzanne,Thomas, Steve,Brown, Terry A.,Smith, Alison,Pillai, Gopalan,Almond, Sarah,Guscott, Martin R.,Burns, H. Donald,Eng, Waisi,Ryan, Christine,Cook, Jacquelynn,Hamill, Terence G.
scheme or table, p. 350 - 354 (2010/11/18)
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 mon