From Off-Target Risks to Optimized Leads: The Power of Kinase Profiling

Kinases are central regulators of nearly every cellular process, making them key targets for developing therapies across a wide range of diseases. Conducting thorough kinase profiling is critical for ensuring that a compound selectively hits its intended target, helping to guide lead optimization, explore opportunities for drug repurposing, and anticipate potential off-target effects or side effects.

What is Kinase Profiling?

Kinase profiling involves screening a candidate compound against a broad panel of kinases to determine its activity across the human kinome. This approach provides a comprehensive view of a compound’s selectivity, revealing both intended and unintended interactions. By understanding which kinases a compound inhibits, researchers can optimize potency, reduce off-target liabilities, and guide strategic decisions early in the drug discovery process.

Visualizing Selectivity with the Kinome Tree

Strategic Value of Kinase Profiling

Kinase profiling is valuable at all stages of preclinical drug discovery and offers several key advantages that directly impact the efficiency and success of drug discovery:

• Toxicity Prediction: Early identification of off-target interactions helps anticipate potential adverse effects before costly preclinical or clinical stages.
• Lead Optimization: Data informs chemical modifications that improve selectivity without compromising potency.

• Regulatory Support: Comprehensive profiling data can strengthen Investigational New Drug (IND) applications and support regulatory submissions.

In summary, integrating kinase profiling early in your discovery pipeline de-risks drug development, accelerates decision-making, and helps deliver safer, more effective therapies.