BROMOscan® Technology Platform
Based on the proven KINOMEscan® technology, BROMOscan is a novel bromodomain inhibitor binding platform that measures the interactions between test compounds and a panel of bromodomain assays. This robust and reliable assay technology affords investigators the ability to extensively annotate compounds with accurate, precise and reproducible data.
Compounds that bind the bromodomain active site and directly (sterically) or indirectly (allosterically) prevent bromodomain binding to the immobilized ligand, will reduce the amount of protein captured on the solid support (Panels A & B). Conversely, test molecules that do not bind the bromodomain have no effect on the amount of bromodomain captured on the solid support (Panel C). Screening “hits” are identified by measuring the amount of bromodomain captured in test versus control samples by using a quantitative, precise and ultra-sensitive qPCR method that detects the associated DNA label. In a similar manner, dissociation constants (Kds) for test compound-bromodomain interactions are calculated by measuring the amount of bromodomain captured on the solid support as a function of the test compound concentration.
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BROMOscan Platform Feature & Benefits
Reports true thermodynamic inhibitor Kd values over a broad range (<100 pM to >10 uM)
Test compounds do not interfere with assay readout
Enables rapid assay development without common bottlenecks
Technology translates to any protein class with the few requirements
Screening & profiling: single or multi-target HTS, selectivity profiling and inhibitor Kd determination