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.

Key learning objectives will include:

1. Understand the principles and advantages of using cell-based reporter assays for nuclear receptor profiling, including the ability to evaluate the potency, selectivity, and potential off-target effects of drug candidates


2. Learn about the different types of cell-based assays that can be used to triage compounds in the drug discovery pipeline with safety liabilities


3. Discover how nuclear receptor profiling can help identify potential drug candidates with desirable pharmacological properties