Library Screening

CETSA^® can determine cellular target engagement in physiologically relevant settings of the native, full-length protein and can potentially unlock novel chemical space. CETSA^® library screening in intact cells gives direct confirmation on target engagement of your library compounds in physiological conditions from the onset. 

The high-throughput CETSA^® format, known as CETSA^® Navigate HT, is based on dual-antibody proximity detection systems suitable for miniaturization in 384 and 1536 microtiter plates. Subsequently, the CETSA^® Navigate HT format enables rapid screening of compound libraries. Almqvist et al. reported on the first use of CETSA^® Navigate HT for screening of a compound library of more than 10K  structurally diverse compounds against the therapeutically relevant protein target thymidylate synthase (TS). AstraZeneca recently reported on the use of CETSA^® Navigate HT for primary screening of a 500K compound large library against the validated oncology target CRAF. The CETSA^® Navigate HT format has proven to be robust, with low liability towards PAINS and, thus, to be a reliable tool for screening of both large and focused libraries for identifying new chemical starting points.