Chapter 10. Discovery of MK-0457 (VX-680)

  1. Rongshi Li and
  2. Jeffrey A. Stafford
  1. Julian M. C. Golec

Published Online: 28 SEP 2009

DOI: 10.1002/9780470524961.ch10

Kinase Inhibitor Drugs

Kinase Inhibitor Drugs

How to Cite

Golec, J. M. C. (2009) Discovery of MK-0457 (VX-680), in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch10

Editor Information

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

Author Information

  1. Vertex Pharmaceuticals (Europe) Ltd, Oxfordshire OX14 4RY, United Kingdom

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



  • cell cycle kinase inhibitors - Aurora kinase and PLK inhibitors;
  • MK-0457 (VX-680) discovery;
  • insights into mechanism and structure–activity relationships


This chapter contains sections titled:

  • Introduction

  • Early Medicinal Chemistry

  • First Crystal Structures

  • First in vivo Experiments

  • The Discovery of MK-0457 (VX-680)

  • Insights into Mechanism and Structure-Activity Relationships

  • MK-0457 (VX-680) and ABL

  • Other Aurora Inhibitors

  • Summary

  • Acknowledgment

  • References