# Drug Discovery and Development Core

> **NIH NIH P50** · UNIVERSITY OF MINNESOTA · 2020 · $765,837

## Abstract

PROJECT SUMMARY - Drug Discovery and Development Core (Core B)
 The Drug Discovery and Development (DDD) Core is a closed core that will support contraceptive
development research projects 1-3 of this interdisciplinary U54 center with the expertise to discover and develop
male contraceptive agents.
The DDD Core will develop a BRDT tandem screen (project 2), ATP-competitive kinase inhibitor and allosteric
inhibitor assays for TSSK6 (project 3), and perform high throughput screens with 100,000 compounds for both
projects 2 and 3. Screening hits will be prioritized computationally and confirmed using biochemical, biophysical,
and analytical chemistry methods.
Additionally, the DDD Core will support projects 1-3 with protein production, crystallography, and biophysical and
biochemical characterization. Purified proteins will be co-crystallized with small molecules and the structures of
the molecular complexes will be determined at atomic resolution. The resultant structural data will be used for in
silico screening and will be combined with biochemical and biophysical data for rational, structure-based drug
design to drive lead optimization.
The DDD Core will support projects 1-3 by optimizing screening hits and leads using an iterative medicinal
chemistry approach. Leads will be optimized for potency, selectivity, and drug-like properties using structure-
based drug design and the results from the binding, functional, and ADMET assays. Optimized lead compounds
will be provided in quantities needed for animal studies. Pharmacokinetic studies will also be performed in the
DDD Core to support the medicinal chemistry studies.
The core will provide optimized leads to the projects for in vivo assessment of reversible induction of sterility in
preparation for contraception trials and preclinical development. The optimized lead compounds may have the
potential to enter human clinical trials with the ultimate goal of commercializing them for male contraception.

## Key facts

- **NIH application ID:** 9931060
- **Project number:** 5P50HD093540-04
- **Recipient organization:** UNIVERSITY OF MINNESOTA
- **Principal Investigator:** Gunda I. Georg
- **Activity code:** P50 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $765,837
- **Award type:** 5
- **Project period:** — → 2022-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9931060

## Citation

> US National Institutes of Health, RePORTER application 9931060, Drug Discovery and Development Core (5P50HD093540-04). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/9931060. Licensed CC0.

---

*[NIH grants dataset](/datasets/nih-grants) · CC0 1.0*