Identification of the cellular targets of bioactive small organic molecules using affinity reagents

Chem Soc Rev. 2008 Jul;37(7):1347-60. doi: 10.1039/b702942j. Epub 2008 May 23.


The elucidation of molecular targets of bioactive small organic molecules remains a significant challenge in modern biomedical research and drug discovery. This tutorial review summarizes strategies for the derivatization of bioactive small molecules and their use as affinity probes to identify cellular binding partners. Special emphasis is placed on logistical concerns as well as common problems encountered during such target identification experiments. The roadmap provided is a guide through the process of affinity probe selection, target identification, and downstream target validation.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Affinity Labels / chemistry
  • Affinity Labels / pharmacology*
  • Binding Sites / drug effects
  • Binding Sites / physiology
  • Cells / cytology
  • Cells / drug effects*
  • Cells / metabolism
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Organic Chemicals / chemical synthesis
  • Organic Chemicals / pharmacology*
  • Pharmaceutical Preparations / chemical synthesis*


  • Affinity Labels
  • Organic Chemicals
  • Pharmaceutical Preparations