Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1
- ACS Med Chem Lett. 2010 Jun 25;1(7):350-4. doi: 10.1021/ml1001085.
- 1. Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
- 2. Research Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486.
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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Cat. No.Product NameDescriptionTargetResearch Area
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target: GlyTResearch Areas: Neurological Disease