# Medicinal Chemistry Core

> **NIH NIH U19** · UNIVERSITY OF PENNSYLVANIA · 2021 · $1,661,993

## Abstract

MEDICINAL CHEMISTRY AND RADIOCHEMISTRY CORE ABSTRACT
The Medicinal Chemistry and Radiochemistry (MCRC) Core represents the central hub of activity of this
U19 Center. The initial focus of the MCRC Core is the use of novel in silico methods for the identification
of lead compounds for PET radiotracer development for alpha synuclein (Asyn) and 4R tau. This
approach to lead compound identification is highly innovative since it has never been applied prior to this
in the field of PET radiotracer development. Once in silico hits have been confirmed as true lead
compounds from the radioligand binding studies conducted in Projects 1 and 2, the MCRC Core will be
responsible for conducting structure-activity relationship (SAR) studies to identify compounds having the
appropriate properties for radiolabeling and additional in vitro and in vivo characterization. The
radiolabeling studies will be conducted by the radiochemistry component of the MCRC Core.
There are four different sites involved in the MCRC Core, the University of Pennsylvania, Washington
University-St. Louis, the University of Pittsburgh, and the contract research organization, MedChem
Imaging. The Core Co-Directors are Drs. Robert H. Mach and E. James Petersson of Penn; each site
will also have a site P.I. (C. Mathis, Pitt; Z. Tu, Wash U; Neil Vasdev, MedChem Imaging). The site P.I.s
will serve as members of the Executive Steering Committee, who will meet via video teleconference on
a bi-weekly basis. The goal of the Executive Steering Committee is to monitor progress of the in silico
screening methods and in vitro binding studies, and the determination of which group should be assigned
the resultant SAR studies on the true lead compounds. Another goal of the MCRC Core is to conduct an
in vitro assay to determine if promising compounds are substrates for P-glycoprotein. A final function of
the MCRC Core is to conduct scale-up synthesis of precursors and standards required for the imaging
studies conducted by the Clinical Imaging Core.

## Key facts

- **NIH application ID:** 10241510
- **Project number:** 5U19NS110456-03
- **Recipient organization:** UNIVERSITY OF PENNSYLVANIA
- **Principal Investigator:** ROBERT H MACH
- **Activity code:** U19 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $1,661,993
- **Award type:** 5
- **Project period:** 2019-09-24 → 2024-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10241510

## Citation

> US National Institutes of Health, RePORTER application 10241510, Medicinal Chemistry Core (5U19NS110456-03). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10241510. Licensed CC0.

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