Biochemical and biophysical assays using TR-FRET, Alphascreen, FP, SPR etc. to detect PROTAC-target protein, or PROTAC-E3 ligase binary complex formation, and target protein-PROTAC-E3 ligase ternary complex formation. Cellular assays could detect protein degradation induced by PROTAC and its target engagement. Customize cellular functional assay to confirm the bioactivity of PROTAC on treating specific indication.
PROTAC Degradation Agent Assay Case Study:
Development of a kinase degrader for inhibiting cancer cell proliferation
Case Study: Although less potent on inhibiting enzyme activity than inhibitor X, degrader compound Y degraded enzyme efficiently, leading to more potent inhibition on cell survival than inhibitor.