TargetScout
Selectivity and affinity profiling of cellular drug targets
- TargetScout™ reveals and verifies specific cellular targets of small molecules under physiological conditions with native, endogenously expressed, posttranslationally modified full length proteins in the presence of cellular co-factors and complex partners
- Determines target-specific IC50 information for the compound studied, ranking targets according to their likely physiological relevance
- Selectivity analysis on a proteome-wide scale under in vivo conditions
- Not target-class restricted - immobilization of affinity compounds typically via amine functions or Click chemistry
- Useful for informed decisions at various stages of drug development (e.g. for target deconvolution, lead optimization, pre-clinical candidate selection)
Further reading
Schirle, M., Bantscheff, M., and Kuster, B. (2012). Mass Spectrometry-based Proteomics in Preclinical Drug Discovery, Chem Biol 19(1):72-84. [Link]
Schematic representation of the TargetScout™ technology
Small molecule-protein interactions can be studied in a target-class agnostic manner under physiological conditions