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.
Target AssayScreeningHits and
HitHit to LeadLead Series
NIDDK-Specific Funding Opportunities
- PAR-16-121, Early-Stage Preclinical Validation of Therapeutic Leads for Diseases of Interest to the NIDDK (R01)
- Academic Drug Discovery Consortium
- NIH Molecular Libraries and Imaging
- NIDDK Small Business Programs
For additional information, contact Dr. Aaron Pawlyk.