Hit to lead is an early stage in drug discovery where hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising compounds. These lead compounds undergo more extensive optimization in a subsequent step of drug discovery called lead optimization.
Drug hit to lead service providers work closely with sponsors to define the compound profile required, prioritize compounds for detailed evaluation, and interpret results from a customized screening cascade. This includes primary target discovery and cellular activity together with ADME/PK assessment and target engagement biomarker assay development.