A three-stage biophysical screening cascade for fragment-based drug discovery

Abstract

This protocol describes the screening of a library of low-molecular-weight compounds (fragments) using a series of biophysical ligand-binding assays. Fragment-based drug discovery (FBDD) has emerged as a successful method to design high-affinity ligands for biomacromolecules of therapeutic interest. It involves detecting relatively weak interactions between… (More)
DOI: 10.1038/nprot.2013.130

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