High quality Structure-Activity Relationship data
with our biological profiling services.

Decrease the risk of failure in your drug development process with hit-to-lead profiling

A druggability assessment is a crucial step in identification of chemical lead compounds. A chemical lead is defined as a synthetically feasible, stable, and drug-like molecule active in primary and secondary assays with acceptable specificity and selectivity for the target. This requires definition of the Structure-Activity Relationship (SAR) as well as determination of synthetic feasibility and preliminary evidence of in vivo efficacy and target engagement.

The compounds from these hit series meet a threshold level of activity during the screen of a primary assay. Activity levels can be found by measuring amongst others the potency, selectivity, solubility and permeability.

Optimizing the necessary properties of these active compounds without compromising on other properties is often challenging. If we for example want to improve the absorption of a drug, we can do this by reducing its molecular weight, but the reduction of a compound’s molecular weight can have a negative impacts on its overall potency. With its longstanding experience the team at Pivot Park Screening Centre knows how to avoid these negative impacts and get you the high-quality drug-like leads you seek.