Chemical predictive modelling to improve compound quality

Nat Rev Drug Discov. 2013 Dec;12(12):948-62. doi: 10.1038/nrd4128.

Abstract

The 'quality' of small-molecule drug candidates, encompassing aspects including their potency, selectivity and ADMET (absorption, distribution, metabolism, excretion and toxicity) characteristics, is a key factor influencing the chances of success in clinical trials. Importantly, such characteristics are under the control of chemists during the identification and optimization of lead compounds. Here, we discuss the application of computational methods, particularly quantitative structure-activity relationships (QSARs), in guiding the selection of higher-quality drug candidates, as well as cultural factors that may have affected their use and impact.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Compounding / standards*
  • Forecasting
  • Humans
  • Models, Chemical*
  • Pharmaceutical Preparations / chemistry*
  • Quantitative Structure-Activity Relationship*

Substances

  • Pharmaceutical Preparations