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The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function.
Jensen, Thomas; Elster, Lisbeth; Nielsen, Søren Møller; Poda, Suresh Babu; Loechel, Frosty; Volbracht, Christiane; Klewe, Ib Vestergaard; David, Laurent; Watson, Stephen P.
Afiliação
  • Jensen T; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Elster L; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Nielsen SM; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Poda SB; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Loechel F; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Volbracht C; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Klewe IV; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • David L; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
  • Watson SP; Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
Bioorg Med Chem Lett ; 24(22): 5195-8, 2014 Nov 15.
Article em En | MEDLINE | ID: mdl-25442311
The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Triazóis / Receptores Acoplados a Proteínas G / Agonismo Inverso de Drogas Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Dinamarca

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Triazóis / Receptores Acoplados a Proteínas G / Agonismo Inverso de Drogas Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Dinamarca