Dr. Jack Vanden Heuvel discusses the use of cell-based reporter assays for nuclear receptor profiling to efficiently prioritize drug candidates and minimize off-target effects.

In preclinical drug discovery, the identification of potential drug candidates requires a thorough evaluation of their pharmacological effects, as well as any potential off-target liabilities. Nuclear receptors play a crucial role in many physiological processes and have emerged as important targets for drug discovery. However, potential drugs often have multiple effects, often within a gene family, leading to potential polypharmacology, where new beneficial effects, as well as off-target liabilities, can be discovered.

To triage or prioritize data, dose-response experiments with nuclear receptor assays can be used. In this presentation, we discuss the use of cell-based reporter assays for nuclear receptor profiling and how this strategy can help identify potential drug candidates with desirable pharmacological properties and reduced off-target effects.