Applications of chemogenomic library screening in drug discovery

Nat Rev Drug Discov. 2017 Apr;16(4):285-296. doi: 10.1038/nrd.2016.244. Epub 2017 Jan 20.


The allure of phenotypic screening, combined with the industry preference for target-based approaches, has prompted the development of innovative chemical biology technologies that facilitate the identification of new therapeutic targets for accelerated drug discovery. A chemogenomic library is a collection of selective small-molecule pharmacological agents, and a hit from such a set in a phenotypic screen suggests that the annotated target or targets of that pharmacological agent may be involved in perturbing the observable phenotype. In this Review, we describe opportunities for chemogenomic screening to considerably expedite the conversion of phenotypic screening projects into target-based drug discovery approaches. Other applications are explored, including drug repositioning, predictive toxicology and the discovery of novel pharmacological modalities.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Design
  • Drug Discovery / methods*
  • Drug Repositioning / methods
  • Humans
  • Molecular Targeted Therapy / methods*
  • Phenotype
  • Small Molecule Libraries / pharmacology*
  • Small Molecule Libraries / toxicity


  • Small Molecule Libraries