Assay development and screening for discovery of chemical probes, drugs or immunomodulators (R01 Clinical Trial Not Allowed)
Last verified by NonDilute: 2026-04-29. Official notice and agency instructions control.
If you have validated a screening assay or identified promising chemical hits and want NIH funding to optimize them into therapeutic leads, this R01 is designed for your team.
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What this is
This R01 grant from the National Cancer Institute supports discovery-phase research in small-molecule drug development, spanning assay design, screening campaigns, hit validation with secondary assays, and lead optimization including SAR and ADME studies. The work targets disease mechanisms and biological targets relevant to NCI and participating NIH institutes, stopping short of clinical trials. It is well-suited to researchers and small teams with chemistry, biology, and screening expertise who want to move validated chemical leads toward therapeutic potential.
Who can apply
Open to small businesses, nonprofits (with or without 501(c)(3) status), universities, government agencies, and tribal organizations. For-profit organizations and small businesses are explicitly eligible. Solo individuals are not eligible; you must apply through an eligible organizational entity.
Eligible applicant types
- Native American tribal organizations (other than Federally recognized tribal governments)
- Independent school districts
- Nonprofits having a 501(c)(3) status with the IRS, other than institutions of higher education
- Small businesses
- Native American tribal governments (Federally recognized)
- County governments
- Others (see text field entitled "Additional Information on Eligibility" for clarification)
- City or township governments
- Nonprofits that do not have a 501(c)(3) status with the IRS, other than institutions of higher education
- Public and State controlled institutions of higher education
- For profit organizations other than small businesses
- State governments
- Public housing authorities/Indian housing authorities
- Private institutions of higher education
- Special district governments
Full description — from the agency
Through this Notice of Funding Opportunity (NOFO), the National Cancer Institute (NCI) solicits applications for identification of small molecules that function to elucidate the biology of disease as chemical probes or function as agonists or antagonists of disease target(s) for therapy or immunotherapy. The NOFO is intended to support discovery research for the identification of validated hits relevant to health-related outcomes of participating NIH Institutes. Stages of discovery research covered by this NOFO include: 1) assay development for specific biological targets and disease mechanisms relevant to the mission of participating NIH Institutes with the intent to screen for small molecule compounds that show potential as probes for use in advancing knowledge about the known targets, identifying new targets, or as pre-therapeutic leads; 2) screen implementation high throughput target-focused approaches or moderate throughput phenotypic- and fragment-based approaches to identify initial screening hits; 3) hit validation, including implementation of secondary assays that are orthogonal to the primary assay, advanced cheminformatics analysis and initial medicinal chemistry inspection to prioritize the hit set, and follow-up assays to characterize mode and mechanism of action of the validated hits; 4) hit-to-lead optimization, including SAR to optimize target engagement, selectivity and to minimize chemical liabilities, ADME, PK and PD studies, and, if appropriate, in vivo modeling to test efficacy or biological effects.
Topics: small molecule discovery · chemical probes · high-throughput screening · hit validation · drug lead optimization · assay development · medicinal chemistry
Public-source funding discovery only. This summary is generated from public agency data and may be incomplete or stale. NonDilute is not affiliated with, endorsed by, or acting on behalf of any government agency. Official notices and agency instructions control. NonDilute does not determine eligibility, provide grant-writing advice, or guarantee funding.