Deorphanization strategies for dark chemical matter. (March 2017)

• Record Type: Journal Article
• Authors: Wassermann, Anne Mai; Tudor, Matthew; Glick, Meir
• Is Part Of: Drug discovery today. Volume 23(2016)
• Page Start: 69
• Page End: 74
• Publication Date: 2017-03
• Subjects: Drug development -- Periodicals; Physiology, Pathological -- Periodicals; Drugs -- Design -- Periodicals; 615.1
• DOI: 10.1016/j.ddtec.2016.11.004
• Languages: English
• ISSNs: 1740-6749

Abstract

Abstract : The term dark chemical matter (DCM) was recently introduced for those molecules in a screening collection that have never shown any substantial biological activity despite having been tested in hundreds of high-throughput assays. It was suggested that, if hits emerge from this compound pool in future screening campaigns, they should be prioritized due to their exquisite selectivity profile. In this article we define DCM at our company and describe on-going efforts to shed light on the bioactivity of these apparently silent compounds, with an emphasis on multi-parametric profiling methods. It is also demonstrated that compounds that are dark within one institution might be found active in another, but typically show the foretold selectivity.