After screening out the compounds showing potential activity against the target through the hit identification stage, it is necessary to carry out further characterization and optimization of these hit compounds. And this stage is termed as hit to lead. The goal of this stage is to identify the most promising hit series through limited structure-activity relationship (SAR) studies to enter the lead optimization and preclinical development stage. With a dedicated team of skilled scientists and technicians, Creative Biostructure provides MagHelix™ hit evaluation and lead identification (hit to lead) solutions to meet our clients’ needs and goals.
Whether your therapeutic goal focuses on the development of small molecules, peptides, or other biologics, Creative Biostructure can ensure that the performance of your initial hits is significantly improved to meet the standards required to enter the lead optimization stage. We can prioritize and classify the hit compounds identified through screening platforms and utilize advanced biophysical techniques to analyze the target-ligand binding modes. In addition, computer-aided drug design (CADD) tools can help you perform pharmacophore modeling, QSAR analysis, ADME/T prediction, etc. The molecules after the hit to lead stage are the most likely potential leads, which have enhanced potency, reduced off-target activity, and predicted physiochemical/metabolic properties of reasonable in vivo pharmacokinetics.