Non-Degrading Molecular Glues: A Platform for Finding Novel Chemical Matter for Inhibiting Intracellular & Transmembrane Proteins
Time: 1:00 pm
day: Day 2, Track 2, PM
Details:
- The described macrocycles form ternary complexes comprising a presenter protein (FKBP12), the molecular glue, and a target protein. Inhibition through formation of a ternary complex often results in potency, selectivity over homologous proteins and favourable drug like properties such as slow binding kinetics
- The principles of constructing DEL libraries with Topological diversity is a key driver for broadly unlocking target classes
- The performance platform against a number of target classes will be presented
- SAR studies directed at optimising lead molecules against a target will be described
