Using Microscale Thermophoresis to Characterize Hits from High-Throughput Screening: A European Lead Factory Perspective

Julie M. Rainard, George C. Pandarakalam, Stuart P. McElroy (Lead / Corresponding author)

Research output: Contribution to journalReview articlepeer-review

13 Citations (Scopus)
321 Downloads (Pure)

Abstract

High-throughput screening (HTS) is a proven method for discovering new lead matter for drug discovery and chemical biology. To maximize the likelihood of identifying genuine binders to a molecular target, and avoid wasting resources following up compounds with unproductive/nonspecific mechanisms of action, it is important to employ a range of assays during an HTS campaign that build confidence of target engagement for hit compounds. Biophysical methods that measure direct target/compound engagement have established themselves as key techniques in generating this confidence, and they are now integral to the latter stages of HTS triage at the European Lead Factory (ELF). One relatively new technique that the ELF is using is microscale thermophoresis (MST), which measures the differences in rate of movement through a temperature gradient that are caused when single molecular species form complexes. Here we provide an overview of the MST assay development workflow that the ELF employs and a perspective of our experience to date of using MST to triage the output of HTS campaigns and how it compares and contrasts with the use of other biophysical techniques.

Original languageEnglish
Pages (from-to)225-241
Number of pages17
JournalSLAS Discovery
Volume23
Issue number3
Early online date20 Feb 2018
DOIs
Publication statusPublished - 1 Mar 2018

Keywords

  • assay development
  • biophysical assays
  • drug discovery
  • high-throughput screening
  • microscale thermophoresis

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