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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Liang, Jun; Zhang, Birong; Labadie, Sharada; Ortwine, Daniel F; Vinogradova, Maia; Kiefer, James R; Gehling, Victor S; Harmange, Jean-Christophe; Cummings, Richard; Lai, Tommy; Liao, Jiangpeng; Zheng, Xiaoping; Liu, Yichin; Gustafson, Amy; Van der Porten, Erica; Mao, Weifeng; Liederer, Bianca M; Deshmukh, Gauri; Classon, Marie; Trojer, Patrick; Dragovich, Peter S; Murray, Lesley.
Afiliación
  • Liang J; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
  • Zhang B; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Labadie S; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Ortwine DF; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Vinogradova M; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Kiefer JR; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Gehling VS; Constellation Pharmaceuticals Inc., 215 First Street, Suite 200, Cambridge, MA 02142, USA.
  • Harmange JC; Constellation Pharmaceuticals Inc., 215 First Street, Suite 200, Cambridge, MA 02142, USA.
  • Cummings R; Constellation Pharmaceuticals Inc., 215 First Street, Suite 200, Cambridge, MA 02142, USA.
  • Lai T; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • Liao J; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • Zheng X; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • Liu Y; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Gustafson A; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Van der Porten E; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Mao W; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • Liederer BM; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Deshmukh G; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Classon M; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Trojer P; Constellation Pharmaceuticals Inc., 215 First Street, Suite 200, Cambridge, MA 02142, USA.
  • Dragovich PS; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Murray L; Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett ; 26(16): 4036-41, 2016 08 15.
Article en En | MEDLINE | ID: mdl-27406798
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Pirazoles / Pirimidinonas / Proteína 2 de Unión a Retinoblastoma Límite: Animals / Female / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Pirazoles / Pirimidinonas / Proteína 2 de Unión a Retinoblastoma Límite: Animals / Female / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article