Notice of Intent to Publish a Funding Opportunity Announcement to Solicit Validated Hits for the Discovery of in vivo Chemical Probes (R01)

Notice Number: NOT-MH-12-006

Key Dates
Release Date: November 8, 2011

Issued by
National Institute of Mental Health (NIMH)

Purpose

The National Institute of Mental Health (NIMH), in conjunction with the NIH Molecular Libraries Program and other participating NIH Institutes, intends to issue a Funding Opportunity Announcement (FOA) to encourage investigators to submit applications for the discovery of in vivo chemical probes.

Recent technological innovations in chemical synthesis, cheminformatics, and high throughput bioactivity and drug property assays have allowed rapid discovery of novel, small-molecule probes for the study of disease related biological processes and mechanisms in an academic environment. This provides an unprecedented opportunity for investigators to translate knowledge about diseases into tangible tools and to reshape their research frontier toward a cure. This FOA intends to support investigators who have interest and capability to join efforts for the discovery of in vivo chemical probes. It is intended that applicants will have in hand the starting compounds (“validated hits”) for chemical optimization and bioassays for testing new analog compounds.

Through this planned FOA, NIH wishes to stimulate research in 1) discovery and development of novel, small molecules for their potential use in studying disease treatment relevant to the missions of the participating NIH Institutes, and 2) discovery and/or validation of novel, biological targets that will inform studies of disease mechanisms.  Emphasis will be placed on assays that provide new insight into important disease targets and processes.  

The FOA plans to utilize the NIH Research Project Grant (R01) award mechanism with a total project period not to exceed 3 years. The FOA is expected to be published in December 2011 with its first receipt date planned for February 2012. 

Research Initiative Details

This program intends to create an opportunity for integrated research in biology and chemistry on structure-activity relationships (SAR) of novel compounds through an iterative and parallel optimization process, which will ultimately allow the researchers to take a holistic approach and make rapid progress toward successful development of in vivo chemical probes. The iterative bioassay and chemical optimization cycles may encompass:

  • In vitro cellular and tissue activities (potency, selectivity, specificity, etc.);
  • In vitro structural, physicochemical, and biochemical properties (solubility, stability, membrane permeability, protein binding, microsome stability, metabolite identification, CYP inhibition, etc.);
  • In vivo pharmacokinetics (PK) with absorption, distribution, metabolism, excretion (ADME) and toxicity;
  • In vivo efficacy

APPLICATIONS ARE NOT BEING SOLICITED AT THIS TIME.

Inquiries

Inquiries regarding this Notice may be directed to:

Yong Yao, Ph.D.
National Institute of Mental Health (NIMH)
NIH Molecular Libraries Initiative
Telephone:  301-443-6102
Email: [email protected]