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

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 tr...

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Published in:ACS medicinal chemistry letters 2010-10, Vol.1 (7), p.350-354
Main Authors: 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
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Language:English
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Summary: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml1001085