The interdependence between screening methods and screening libraries

Anang A. Shelat, R. Kiplin Guy

Research output: Contribution to journalReview articlepeer-review

51 Scopus citations


The most common methods for discovery of chemical compounds capable of manipulating biological function involves some form of screening. The success of such screens is highly dependent on the chemical materials - commonly referred to as libraries - that are assayed. Classic methods for the design of screening libraries have depended on knowledge of target structure and relevant pharmacophores for target focus, and on simple count-based measures to assess other properties. The recent proliferation of two novel screening paradigms, structure-based screening and high-content screening, prompts a profound rethink about the ideal composition of small-molecule screening libraries. We suggest that currently utilized libraries are not optimal for addressing new targets by high-throughput screening, or complex phenotypes by high-content screening.

Original languageEnglish
Pages (from-to)244-251
Number of pages8
JournalCurrent Opinion in Chemical Biology
Issue number3
StatePublished - Jun 2007

Bibliographical note

Funding Information:
We thank the suppliers listed in Table 1 for graciously providing the composition of their libraries. This work was supported by the American Lebanese Syrian Associated Charities (ALSAC) and St. Jude Children's Research Hospital.

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry


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