Building in molecular diversity for targeted libraries

Drug Discov Today Technol. 2013 Dec;10(4):e461-6. doi: 10.1016/j.ddtec.2012.12.002.

Abstract

The use of gene-focussed libraries for screening against protein targets can improve timelines for drug discovery projects. This is especially true when the library is based on a novel core scaffold, avoiding the potential need to scaffold hop from early hits. Identification of an appropriate novel scaffold is therefore integral to the success of such a library. In this article we outline a new method to aid scaffold design that combines structure- based virtual screening (VS) with a second phase in which fragmentation of the output is made before the final scaffold design step. Through consideration of a refined set of bound fragments, in the context of the compounds from which they originated, appropriate vectors for appended R-groups can be assigned before validation of the final library.

Publication types

  • Review

MeSH terms

  • Drug Design*
  • Pharmaceutical Preparations / metabolism
  • Protein Binding
  • Small Molecule Libraries

Substances

  • Pharmaceutical Preparations
  • Small Molecule Libraries