Chemoproteomic Profiling of Covalent Inhibitors in Multiple Cell Types to Assess Pharmacological Targets & Off-Target Safety Risks
Time: 9:30 am
day: Conference Day Two
Details:
- Chemoproteomic profiling using clickable probes of covalent inhibitors in multiple cell types is a crucial technique for evaluating their proteome-wide selectivity to assess target engagement and off-targets
- Importance of selecting appropriate cell lines and organ systems for screening covalent inhibitors to comprehensively assess potential off-target toxicities
- While no single method can definitively determine a compound’s propensity for causing DILI, broadening the scope of chemoproteomic profiling to encompass liver systems in the evaluation of covalent inhibitors could pinpoint off-targets to avoid, thereby helping to mitigate the risk of DILI
