CETSA® Navigate HT: A New Paradigm For High-Throughput Screening
Introduction to CETSA® Navigate HT
CETSA® Navigate HT is a high-throughput format for screening and/or profiling larger sets of drug molecules. Once established, a CETSA® Navigate HT assay can generate TE data in several forms, e.g., SP data for screening large libraries and concentration response (CR) for generating TE potency (EC50) data. As a case study to demonstrate the applicability of CETSA® Navigate HT in hit identification, we have applied the technology to CDK4, a recognised target of interest in several cancers.
Key Learnings
- A CETSA® Navigate HT assay in intact THP1 cells was established for CDK4 and successfully applied for hit identification in a screening campaign.
- The efforts identified both known and novel chemotypes involved in CDK4-driven cellular effects and further studies to deconvolute potentially different mechanisms of action of the hits are planned (e.g., selectivity profiling using the proteome-wide CETSA® Explore format).
- Due to its broad applicability to native, full length protein targets in the live cellular environment, CETSA® Navigate HT may be regarded as a new paradigm for high-throughput screening.
Download our poster and learn how to use CETSA® Navigate HT for High-Throughput Screening.
Publications
- Martinez Molina, D. et al. Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay. Science 341, 84-87 (2013)
- Chernobrovkin at al., SLAS Discovery 2021, DOI: 10.1177/2472555220984372