Drug–target residence time and its implications for lead optimization

@article{Copeland2006DrugtargetRT,
  title={Drug–target residence time and its implications for lead optimization},
  author={Robert A Copeland and David L. Pompliano and Thomas D Meek},
  journal={Nature Reviews Drug Discovery},
  year={2006},
  volume={6},
  pages={-}
}
Much of drug discovery today is predicated on the concept of selective targeting of particular bioactive macromolecules by low-molecular-mass drugs. The binding of drugs to their macromolecular targets is therefore seen as paramount for pharmacological activity. In vitro assessment of drug-target interactions is classically quantified in terms of binding parameters such as IC(50) or K(d). This article presents an alternative perspective on drug optimization in terms of drug-target binary… CONTINUE READING
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