[SLAS 2022]High Throughput Screening Cascade to Generate Highly Selective Hits for PIM3 Kinase
- File Name/Number:
Kinase discovery efforts are particularly challenging due to the conservation of active sites and high structural homology between kinases, leading to safety liabilities and sometimes suboptimal success rates in high-throughput screening (HTS) campaigns.
Access to highly purified sources of active recombinant kinases and automated, high-throughput technologies facilitate the design of rapid and efficient strategies for the discovery of novel kinase inhibitors. In addition, the design and execution of today’s screening cascades require coordinated chemical library management, as well as optimized project and resource management, to meet the current standards of modern hit programs to deliver on time.