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

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

ABSTRACT

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.

Palavras-chave

DCCCyB; GlyT1; Inhibitor; PET tracer ligand; structure−activity relationship

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2010 Tipo de documento: Article País de afiliação: Reino Unido

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