A Guide to Navigating Hit Prioritization After Screening Using Biochemical Assays

So you have performed your screen. What’s next? This guide is focused on how biochemical assays are used for characterizing and prioritizing compounds following a primary screen with an enzyme target, whether using high throughput screening (HTS) or virtual screening (VS). A typical screening funnel is shown below, with the many applications of the biochemical activity assay highlighted.

Here we will discuss strategies for hit-to-lead selection including:

  • Assay Considerations
  • Hit Confirmation
  • Running a Dose-Response
  • Compound Triaging
  • Hit Expansion
  • Mechanism of Action Studies
  • Residence Time Measurement

Example Hit-to-Lead Prioritization Funnel

Preclinical Drug Discovery Funnel Fig 1
A Guide to Navigating Hit Prioritization After Screening Using Biochemical Assays

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