Chemical Diversity

The goals of this initiative are two-fold:

1. To support the development of new methodologies related to chemical diversity
2. To support the production of chemical libraries in unexplored regions of “chemical diversity space” where there is reason to believe that novel bioactivities may be found.

Related to the first goal, six R01 grants have been made with ML funds to support the development of new methodologies for natural products chemistry. Over the years, a disproportionate share of drugs have originated from, or were inspired by, natural products (i.e., compounds from natural sources). This is not surprising, since natural products have evolved in order to enhance the survival of the organisms that produce them-in other words, for their bioactivites. However, in recent years, most pharmaceutical companies have moved away from natural products as leads for drug discovery and development. This often is due in large part to the limitations of current methodologies for natural products chemistry, including production, isolation, purification, and characterization.

The projects funded under RFA-RM-05-013 were designed to address such bottlenecks and to afford improved procedures. This will enhance the availability of biologically active natural products for screening by the MLSCN as well as for drug discovery and development.

The second Chemical Diversity Technology Development goal is being addressed through a series of P41 (Biotechnology Research Resource) grants (RFA-RM-06-003). Under the terms of these grants, the grantees are providing novel libraries to MLSMR, for HTS evaluation by the MLSCN. A key provision of this funding initiative is that the library designs are driven by biological rather than purely chemical considerations. Additionally, since the goal is to identify effectors of truly novel biological phenotypes and mechanisms, the compounds produced under this initiative represent chemotypes that are distinct from what is available commercially and in existing compound collections.

Data Sharing

As the objectives of each RFA offered on behalf of the Chemical Diversity Initiative are unique, so are the particular data sharing plans associated with them. Interested investigators should review the data sharing plans of each RFA in concert with the specific aims of the particular Announcement.

• See “Section V” of the New Methodologies for Natural Products Chemistry (R01) RFA, RFA-RM-05-013
• See “Section V” of the Pilot-Scale Libraries for High-Throughput Screening (P41) RFA, RFA-RM-06-003

Further Information

Please see the left menu information on chemical diversity funded research from the pilot phase and production phase, or see Funded Research for all ML initiatives

For MLPCN phase Chemical Diversity information, see Tech Development

For currently available funding opportunities, see Funding Opportunities

Or contact:

John M. Schwab, Ph.D.
National Institute of General Medical Sciences