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Grand Challenge Commentary: Accessing new chemical space for 'undruggable' targets

Nature Chemical Biology volume 6, pages 861–863 (2010)Cite this article

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The synthesis and biological annotation of small molecules from underexplored chemical space will play a central role in the development of drugs for challenging targets currently being identified in frontier areas of biological research such as human genetics.

Currently there are several public and private initiatives for submitting libraries made in academic labs for biological screens. In the public sphere, the US National Institutes of Health (NIH) has set up the MLSMR to accept compounds from several sources, including academic labs. These libraries of compounds are then screened in a broad range of assays run in the Molecular Libraries Probe Production Center Networks (MLPCNs) and Molecular Libraries Screening Center Networks (MLSCNs; http://mli.nih.gov/mli/). So far, more than 16,000 compounds have been submitted to the MLSMR from various academic labs. In focused public screening centers, libraries can be screened for specific disease areas; one example is the Psychoactive Drug Screening Program (PDSP; http://pdsp.med.unc.edu/). In a public-private partnership mode, Eli Lilly has announced an initiative to carry out a limited evaluation of the therapeutic potential of compounds synthesized in university and biotechnology laboratories.

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Figure 1
Figure 2: Analysis of structural complexity of MLSMR collection.

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  1. Sivaraman Dandapani and Lisa A. Marcaurelle are members of the Chemical Biology Platform at the Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge, Massachusetts, USA.

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  1. Sivaraman Dandapani

  2. Lisa A Marcaurelle

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  1. Sivaraman Dandapani
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Correspondence to Sivaraman Dandapani or Lisa A Marcaurelle.

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Dandapani, S., Marcaurelle, L. Grand Challenge Commentary: Accessing new chemical space for 'undruggable' targets. Nat Chem Biol 6, 861–863 (2010). https://doi.org/10.1038/nchembio.479

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