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Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Robarge, Kirk D; Lee, Wendy; Eigenbrot, Charles; Ultsch, Mark; Wiesmann, Christian; Heald, Robert; Price, Steve; Hewitt, Joanne; Jackson, Philip; Savy, Pascal; Burton, Brenda; Choo, Edna F; Pang, Jodie; Boggs, Jason; Yang, April; Yang, Xioaye; Baumgardner, Matthew.
Afiliación
  • Robarge KD; Discovery Chemistry, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA. Electronic address: kir@gene.com.
  • Lee W; Discovery Chemistry, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Eigenbrot C; Structural Biology, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Ultsch M; Structural Biology, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Wiesmann C; Structural Biology, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Heald R; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Price S; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Hewitt J; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Jackson P; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Savy P; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Burton B; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Choo EF; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Pang J; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Boggs J; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Yang A; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Yang X; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
  • Baumgardner M; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.
Bioorg Med Chem Lett ; 24(19): 4714-4723, 2014 Oct 01.
Article en En | MEDLINE | ID: mdl-25193232
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazinas / Quinasas de Proteína Quinasa Activadas por Mitógenos / Inhibidores de Proteínas Quinasas / Descubrimiento de Drogas / Compuestos Heterocíclicos / Imidazoles Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazinas / Quinasas de Proteína Quinasa Activadas por Mitógenos / Inhibidores de Proteínas Quinasas / Descubrimiento de Drogas / Compuestos Heterocíclicos / Imidazoles Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article