Translational Research: Hit to Lead

Hit-to-lead research involves taking initial lead compounds or biologics and performing additional experiments to more fully validate the hits. This often involves activities such as re-synthesis of a small molecule or sequence verification of a biologic. Then, limited exploration of the structure activity relationships (SAR) of small molecules or structure function relationships (SFR) of proteins is conducted by testing candidates that are similar but not identical to the hits. Characterization of potential leads for off target activity or preliminary absorption, distribution, metabolism, excretion, and toxicity (ADMET) studies are sometimes carried out at this stage.