Abstract

The application of multiple biophysical techniques to validate initial HTS hits has become an important part of lead discovery. To decipher the mode of action of a new SOS1 inhibitor class, biophysics coupled with the intensive use of structural biology was instrumental.

In this case study, we targeted RAS via SOS1, its guanine nucleotide exchange factor. A combination of HTS and fragment screening resulted in the discovery of the first nanomolar SOS1 inhibitors which disrupt the interaction between RAS and SOS1. This mode of action was elucidated by a series of biophysical techniques and by crystal structures of KRASG12C–SOS1, SOS1 and SOS2.

Join us live to listen to the story of how our biophysics platform strongly contributed to the discovery of potent SOS1 inhibitors that block RAS activation, major oncogenes driving many cancers. In this 45-minute webinar, Dr. Roman Hillig, laboratory head & principal scientist at NUVISAN will cover the following topics:

• Life Science Chemistry Services – Who are we?
• Digitalization in Analytics
• Experimental Polar Surface Area (EPSA) via Supercritical fluid chromatography (SFC)
• Plate-Based Chemistry
• Metabolite Discovery Platform
• Live Q&A session