High-throughput screening (HTS) is an automated method for rapidly analyzing the activity of thousands of chemical compounds. It has become a key tool in modern drug discovery. Paired with combinatorial chemistry and bioinformatics, HTS allows potential drugs to be quickly and efficiently screened to find candidates that should be explored in more detail.

How the Process Works

Most drugs work by binding to a protein target on or in a living cell. One of the first steps in drug discovery and development is finding molecules that will bind to the target. Imagine, for instance, you want to develop an anticancer drug that binds to and inactivates a particular mutant protein known to promote aberrant cell growth. You have a couple of compounds that bind very weakly to your protein, and these serve as the starting point for generating a large number of related compounds, through combinatorial...