Cellular penetration is a crucial property of bioactive molecules to reach intracellular targets, however, current penetration assays are limited when it comes to measuring the exact cytosolic accumulation. Here, the authors introduce a chloroalkane HaloTag azide-based membrane penetration (CHAMP) assay, a high-throughput method using azide tags and click chemistry to accurately measure cytosolic accumulation, offering a powerful tool for the development of drugs targeting intracellular pathways.
- Sobika Bhandari
- George M. Ongwae
- Marcos M. Pires