The enormity of modern chemical libraries, which typically
contain over a million compounds at major pharmaceutical
companies, necessitates high-throughput
biomolecular screening for lead discovery and optimization.
In recent years, HTS has been effectively applied to
the discovery of small-molecule inhibitors for enzyme
targets, either in multi-well or microarray formats. In this
section, we discuss different types of platforms available
for high-throughput screening of biocatalytic assays.