Probes
The NIH Chemical Genomics Center plays a role within the NIH Molecular Libraries Initiative (MLI), mandated to bring advanced technologies and expertise to researchers who lack the means to perform high-throughput screens and follow-up medicinal chemistry efforts as a means of identifying and optimizing small molecule probes of novel, unexplored cellular targets. These reagents offer the research community much-needed proof-of-concept pharmacological tools that may serve as starting points for therapeutic development into clinical agents. Results from these projects are disseminated to the scientific community through the publicly accessible PubChem database and via peer-reviewed publications. This highly collaborative program merges academic researchers' wide-ranging expertise within the study of new biochemical targets and pathways with the translational infrastructure of NCATS.
To date, NCATS scientists, in collaboration with hundreds of extramural scientists, have developed more than 60 probes that are freely accessible to the scientific community. A number of these probes are highlighted below:
Project: Activators for Human Pyruvate Kinase M2 (hPK) as Leads in Cancer Therapeutics
- Assay Provider: Matthew Vander Heiden, Koch Institute at Massachusetts Institute of Technology and Dana-Farber Cancer Institute
- Probe Report
Project: Inhibitors of Caspase 1 for the Treatment of Numerous Autoimmune and Inflammatory Diseases
- Assay Provider: Theodore R. Holman, University of California, Santa Cruz
- Probe Report
Project: Inhibitors of 12-Human Lipoxygenase (12-hLO) for the Treatment of Diabetes and Clotting
- Assay Provider: Theodore R. Holman, University of California, Santa Cruz
- Probe Report
Project: Inhibitors of Cruzain as Therapeutic Leads for Chagas Disease
- Assay Provider: Brian Shoichet, University of California, San Francisco
- Probe Report
- Assay Provider: Udo Oppermann, Structural Genomics Consortium, University of Oxford
- Probe Report
Project: Inhibitors of Cdc2-Like Kinase 4 (Clk4) to Elucidate the Mechanism and Controlling Gene Splicing
- Assay Provider: Tom Misteli, National Cancer Institute
- Probe Report
Project: Agonists of the Thyroid Stimulating Hormone Receptor for the Treatment of Graves' Disease
- Assay Provider: Marvin Gershengorn, National Institute of Diabetes and Digestive and Kidney Diseases
- Probe Report
- Assay Provider: Ellen Sidransky, National Human Genome Research Institute
- Probe Report 1
- Probe Report 2
Project: Identification of SMN Modulators for Potential SMA Disease Therapeutics
- Assay Provider: Elliot Androphy, University of Massachusetts Medical School
- Probe Report
Project: Inhibitors of Platelet Integrin αIIbβ3
- Assay Provider: Barry Coller, Rockefeller University
- Probe Report
Project: Identification of Novel Small Molecule Antagonists of the Neuropeptide-S Receptor
- Assay Provider: Markus Heilig, National Institute on Alcohol Abuse and Alcoholism
- Probe Report
Project: Inhibitors of Schistosoma mansoni Redox Cascade
- Assay Provider: David Williams, Rush University Medical Center
- Probe Report
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