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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.
Afiliação
  • Blackaby WP; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Lewis RT; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Thomson JL; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Jennings AS; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Goodacre SC; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Street LJ; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • MacLeod AM; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Pike A; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Wood S; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Thomas S; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Brown TA; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Smith A; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Pillai G; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Almond S; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Guscott MR; Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom.
  • Burns HD; Research Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486.
  • Eng W; Research Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486.
  • Ryan C; Research Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486.
  • Cook J; Research Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486.
  • Hamill TG; Research Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486.
ACS Med Chem Lett ; 1(7): 350-4, 2010 Oct 14.
Article em En | MEDLINE | ID: mdl-24900218
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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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies Idioma: En Ano de publicação: 2010 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies Idioma: En Ano de publicação: 2010 Tipo de documento: Article