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Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.
Liang, Jun; Van Abbema, Anne; Balazs, Mercedesz; Barrett, Kathy; Berezhkovsky, Leo; Blair, Wade S; Chang, Christine; Delarosa, Donnie; DeVoss, Jason; Driscoll, Jim; Eigenbrot, Charles; Goodacre, Simon; Ghilardi, Nico; MacLeod, Calum; Johnson, Adam; Bir Kohli, Pawan; Lai, Yingjie; Lin, Zhonghua; Mantik, Priscilla; Menghrajani, Kapil; Nguyen, Hieu; Peng, Ivan; Sambrone, Amy; Shia, Steven; Smith, Jan; Sohn, Sue; Tsui, Vickie; Ultsch, Mark; Williams, Karen; Wu, Lawren C; Yang, Wenqian; Zhang, Birong; Magnuson, Steven.
Afiliação
  • Liang J; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Van Abbema A; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Balazs M; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Barrett K; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Berezhkovsky L; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Blair WS; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Chang C; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Delarosa D; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • DeVoss J; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Driscoll J; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Eigenbrot C; Department of Structural Biology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Goodacre S; Argenta Discovery Services, CRL, 8-9 Spire Green Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Ghilardi N; Department of Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • MacLeod C; Argenta Discovery Services, CRL, 8-9 Spire Green Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Johnson A; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Bir Kohli P; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Lai Y; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Lin Z; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Mantik P; Department of Small Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Menghrajani K; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Nguyen H; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Peng I; Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Sambrone A; Department of Small Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Shia S; Department of Structural Biology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Smith J; Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Sohn S; Department of Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Tsui V; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Ultsch M; Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Williams K; Argenta Discovery Services, CRL, 8-9 Spire Green Centre, Harlow, Essex CM19 5TR, United Kingdom.
  • Wu LC; Department of Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Yang W; ChemPartner Co. Ltd., 998 Halei Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China.
  • Zhang B; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
  • Magnuson S; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: magnuson.steven@gene.com.
Bioorg Med Chem Lett ; 27(18): 4370-4376, 2017 09 15.
Article em En | MEDLINE | ID: mdl-28830649
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Inibidores de Proteínas Quinases / TYK2 Quinase / Imidazóis Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Reino Unido
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Inibidores de Proteínas Quinases / TYK2 Quinase / Imidazóis Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Reino Unido