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Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors

Academic Article
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  • Additional Document Info
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Overview

authors

  • Liang, J.
  • van Abbema, A.
  • Balazs, M.
  • Barrett, K.
  • Berezhkovsky, L.
  • Blair, W.
  • Chang, C.
  • Delarosa, D.
  • DeVoss, J.
  • Driscoll, J.
  • Eigenbrot, C.
  • Ghilardi, N.
  • Gibbons, P.
  • Halladay, J.
  • Johnson, A.
  • Kohli, P. B.
  • Lai, Y.
  • Liu, Y.
  • Lyssikatos, J.
  • Mantik, P.
  • Menghrajani, K.
  • Murray, J.
  • Peng, I.
  • Sambrone, A.
  • Shia, S.
  • Shin, Y.
  • Smith, J.
  • Sohn, S.
  • Tsui, Vickie
  • Ultsch, M.
  • Wu, L. C.
  • Xiao, Y.
  • Yang, W.
  • Young, J.
  • Zhang, B.
  • Zhu, B. Y.
  • Magnuson, S.

publication date

  • June 2013

journal

  • Journal of Medicinal Chemistry  Journal

subject areas

  • 4-Aminopyridine
  • Administration, Oral
  • Aminopyridines
  • Animals
  • Benzamides
  • Biological Availability
  • Crystallography, X-Ray
  • Interferon-gamma
  • Interleukin-12
  • Janus Kinase 1
  • Janus Kinase 2
  • Janus Kinase 3
  • Mice
  • Microsomes, Liver
  • Models, Molecular
  • Protein Binding
  • Rats
  • STAT4 Transcription Factor
  • Stereoisomerism
  • Structure-Activity Relationship
  • TYK2 Kinase
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Identity

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm400266t

PubMed ID

  • 23668484
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Additional Document Info

start page

  • 4521

end page

  • 4536

volume

  • 56

issue

  • 11

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