Scripps Florida is a full service NIH screening and chemistry center for discovering proof-of-concept molecules, or molecular probes, typically against novel targets with no known small molecule modulators.  It is expected that these compounds will be useful in understanding important biological disease mechanisms and ultimately in developing new treatments for human diseases. We develop ultra high throughput screens of the NIH Molecular Libraries Small Molecule Repository (MLSMR), encountering a wide  range of targets (enzymes, GPCRs, ion channels, PPIs), and a wide  range of therapeutic areas, screening protocols, chemistry, and biology.  Follow-up chemistry optimization, including addressing potency, selectivity, and DMPK issues, are central to the effort.  Data (and compounds) are freely shared upon completion of the project, as the aim is to seed future discovery in new fields where proof-of-concept molecules no not yet exist.  This talk will give a quick description of the efforts, how they are integrated, and a case study of a probe development project.  The case study will cover efforts from uHTS development, to hit ID, to SAR studies, and to the selection of a designated probe compound.

Probe development at The Scripps Research Institute's Molecular Screening Center

245th National Meeting (2013)

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