Insights into Covalent Drug Discovery from FX-909
Time: 11:30 am
day: Day One
Details:
- FX-909 is a potent and selective inverse agonist of PPARG currently being explored in muscle-invasive luminal urothelial cancer
- FX-909’s selectivity and in vivo properties are derived from the “context-dependent reactivity” exhibited by its unique warhead
- Mechanistic investigations into covalent capture of PPARG were critical for the design and discovery of FX-909 and have also revealed insights into the physical basis of its “context-dependence”