Accelerating the Validation of Endogenous On-Target Engagement and In-cellulo Kinetic Assessment for Covalent Inhibitors of KRASG12C in Early Drug Discovery
V. Kantae, R. Polanski, H. Lewis, D. Barratt, B. SRINIVASAN
This paper develops a high-throughput targeted proteomics workflow using UPLC-MRM to assess on-target engagement of covalent inhibitors in cells, demonstrating its application with KRASG12C.
bioRxiv · Feb 17, 2022Biochemistry