Chapter 9. Discovery of Allosteric MEK Inhibitors

  1. Rongshi Li and
  2. Jeffrey A. Stafford
  1. Eli Wallace and
  2. James F. Blake

Published Online: 28 SEP 2009

DOI: 10.1002/9780470524961.ch9

Kinase Inhibitor Drugs

Kinase Inhibitor Drugs

How to Cite

Wallace, E. and Blake, J. F. (2009) Discovery of Allosteric MEK Inhibitors, in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch9

Editor Information

  1. Takeda San Diego, Inc., San Diego, CA 92121, USA

Author Information

  1. Drug Discovery, Array BioPharma, Boulder, CO 80301, USA

Publication History

  1. Published Online: 28 SEP 2009
  2. Published Print: 2 OCT 2009

Book Series:

  1. Wiley Series in Drug Discovery and Development

Book Series Editors:

  1. Binghe Wang

ISBN Information

Print ISBN: 9780470278291

Online ISBN: 9780470524961



  • allosteric MEK inhibitor discovery;
  • pyridone MEK inhibitors;
  • preclinical pharmacokinetics of AZD 6244


This chapter contains sections titled:

  • Introduction

  • Development of a MEK Pharmacophore Model

  • Pyridone MEK Inhibitors

  • Preclinical Evaluation of AZD 6244

  • Clinical Evaluation of AZD 6244

  • New Directions for MEK Inhibitions

  • MEK Protein-Inhibitor Docking Studies

  • Summary

  • References