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                    Hit to Lead

    Related Topics
        Translational Research
        Disease Biology
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                Hit to Lead
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                Clinical DevelopmentTranslational 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.

    
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NIH Funding Opportunities
PAR-22-111, Early-Stage Preclinical Validation of Therapeutic Leads for Diseases of Interest to the NIDDK (R01 Clinical Trial Not Allowed) has expired. The NIDDK is still interested in supporting this type of translational science and another potential option is to apply to the Parent R01 NOFO (PA-20-185) and consider requesting review assignment to any ofCSR’s Drug Synthesis, Discovery, Disposition, and Xenobiotics study sections, or another relevant review panel. Applicants should consult theNIH/CSR study section descriptions before requesting a specific review panel.
    RFA-NS-24-019, HEAL Initiative: Non-addictive Analgesic Therapeutics Development [Small Molecules and Biologics] to Treat Pain (UG3/UH3 Clinical Trial Optional)Related Resources
Academic Drug Discovery Consortium
    NIH Molecular Libraries and Imaging
    PubChem
    NIDDK Small Business ProgramsStaff Contacts
**Division of Kidney, Urologic, and Hematologic Diseases**Dr. Anna Sadusky
**Division of Digestive Diseases and Nutrition**Dr. Bonnie Burgess-Beusse
**Division of Diabetes, Endocrinology, and Metabolic Diseases**Dr. Yan Li        Last Reviewed October 2023 Contact Us
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