Display Settings:


Send to:

Choose Destination
See comment in PubMed Commons below
Nat Rev Drug Discov. 2002 Feb;1(2):103-10.

Efficacy at G-protein-coupled receptors.

Author information

  • GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. tpk1348@gsk.com


At present, the drug-discovery process centres on ligands that either block or produce physiological responses. However, there are therapeutic uses for ligands that do neither of these things, but which still affect receptors in other ways. This review discusses the intimate relationship between the affinity of a ligand for its receptor, and the probability that the binding of the ligand will produce some change in the receptor, resulting in efficacy. This, in turn, argues that ligands that have affinity should be tested more broadly, for a wider range of efficacies, to detect hidden therapeutic activities.

[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Nature Publishing Group
    Loading ...
    Write to the Help Desk