One signal

A Promega assay called BRETSA measures changes in a protein’s thermal stability inside living cells, offering researchers one way to investigate whether compounds engage a target. Promega product specialist Joshua Sopp described the method to Drug Target Review.

Unlike tracer-based approaches, BRETSA does not require an existing target-specific ligand or fluorescent tracer. That could help researchers examine poorly characterised targets, including ones identified using AI. A shift in thermal stability is evidence consistent with target engagement, not definitive proof of direct binding or selectivity. For AI-designed compounds, is this kind of early cellular check enough to help decide what gets tested next?

Discuss: For AI-designed compounds, is early cellular target-engagement evidence enough to decide what gets tested next, or should stronger proof come first?

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