Pivot Park Screening Centre’s hit-to-lead biological profiling services support hit expansion post ultra-High Throughput Screening (uHTS) campaigns.
During the hit-to-lead stage of your project, in collaboration with our chemistry partners, we can provide a full hit-to-lead package including early in-vitro ADME-Tox profiling to identify high-quality lead candidates. During the hit-to-lead phase of the drug discovery process we explore the chemistry and biological components of hits to ultimately eliminate any sub-optimally active compounds.
We assess the potential that each of your hits has to be developed into a drug-like lead as quickly as possible. Providing you with a wealth of information and knowledge about the lead series that can be used during the next phases of the drug discovery process. Pivot Park Screening Centre is an expert in delivering lead series that can be quickly optimised to robust drug candidates.
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.
Contact our experts to find out more!