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Receptor Targets in Drug Discovery


  1. Michael Williams1,
  2. Rita Raddatz1,
  3. Christopher Mehlin2,
  4. David J. Triggle3

Published Online: 15 SEP 2006

DOI: 10.1002/3527600906.mcb.200500063

Reviews in Cell Biology and Molecular Medicine

Reviews in Cell Biology and Molecular Medicine

How to Cite

Williams, M., Raddatz, R., Mehlin, C. and Triggle, D. J. 2006. Receptor Targets in Drug Discovery. Reviews in Cell Biology and Molecular Medicine. .

Author Information

  1. 1

    Cephalon Incorporated, West Chester, PA

  2. 2

    University Of Washington, Seattle, WA

  3. 3

    State University of New York, Buffalo, NY

Publication History

  1. Published Online: 15 SEP 2006


Receptors, located on both the cell surface and within the cell are the defined molecular targets through which drugs produce their beneficial effects in various disease states. Initially conceptualized over a century ago by Ehrlich and Langley, receptor concepts and receptor theory have undergone continuous modification as their behavior in normal and disease states/tissues have been more clearly characterized. Since the isolation of the nicotinic acetylcholine receptor (nAChR) from the Torpedo , some 50 years ago, new techniques of molecular biology have made it relatively routine to isolate receptors, including orphan receptors. Once these have been validated, they can be used in conjunction with high- throughput screening approaches to identify “hits,” molecules that bind with relatively high affinity to these targets. Such hits can then be optimized to druglike entities using combinatorial/parallel synthesis technology platforms to yield clinical candidates that are potent, efficacious, and bioavailable entities with appropriate safety profiles.


  • Agonist;
  • Antagonist;
  • Drug;
  • G-protein–Coupled Receptors;
  • Heterotrimeric G-protein;
  • High-throughput Screening;
  • Ion Channels;
  • Ligand;
  • New Chemical Entity (NCE);
  • Orphan Receptor;
  • Receptor;
  • SAR;
  • Therapeutic Index