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Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-m ethyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through structure-based drug design: a high affinity irreversible inhibitor targeting oncogenic EGFR mutants with selectivity over wild-type EGFR

Academic Article
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Overview

authors

  • Planken, S.
  • Behenna, D. C.
  • Nair, S. K.
  • Johnson, T. O.
  • Nagata, A.
  • Almaden, C.
  • Bailey, S.
  • Ballard, T. E.
  • Bernier, L.
  • Cheng, H. M.
  • Cho-Schultz, S.
  • Dalvie, D.
  • Deal, J. G.
  • Dinh, D. M.
  • Edwards, M. P.
  • Ferre, R. A.
  • Gajiwala, K. S.
  • Hemkens, M.
  • Kania, R. S.
  • Kath, J. C.
  • Matthews, J.
  • Murray, B. W.
  • Niessen, Sherry
  • Orr, S. T. M.
  • Pairish, M.
  • Sach, N. W.
  • Shen, H.
  • Shi, M.
  • Solowiej, J.
  • Tran, K.
  • Tseng, E.
  • Vicini, P.
  • Wang, Y. L.
  • Weinrich, S. L.
  • Zhou, R.
  • Zientek, M.
  • Liu, L.
  • Luo, Y.
  • Xin, S.
  • Zhang, C.
  • Lafontaine, J.

publication date

  • April 2017

journal

  • Journal of Medicinal Chemistry  Journal

subject areas

  • Acrylamides
  • Animals
  • Carcinoma, Non-Small-Cell Lung
  • Cell Line, Tumor
  • Dogs
  • Drug Design
  • Halogenation
  • Humans
  • Lung
  • Lung Neoplasms
  • Mice
  • Models, Molecular
  • Molecular Docking Simulation
  • Mutation
  • Protein Kinase Inhibitors
  • Pyrrolidines
  • Rats
  • Receptor, Epidermal Growth Factor
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Identity

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.6b01894

PubMed ID

  • 28287730
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Additional Document Info

start page

  • 3002

end page

  • 3019

volume

  • 60

issue

  • 7

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