BROMOscan℠ Bromodomain Assay Panel

New epigenetic screening platform for inhibitors of bromodomain proteins


BROMOscan is a novel industry leading platform for identifying small molecule bromodomain inhibitors.  Bromodomains are epigenetic “reader” proteins that have emerged as an important new druggable target class in small-molecule inhibitor drug discovery with several bromodomain-containing proteins being associated with disease.

Based on the proven KINOMEscan℠ technology platform, BROMOscan is a robust bromodomain assay panel suitable for high throughput screening that delivers quantitative ligand binding data to facilitate the identification and optimization of potent and selective small molecule bromodomain inhibitors for both pharmaceutical use and as tool compounds to further elucidate the roles of bromodomains in human disease.

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BROMOscan Bromodomain Assay Panel

Red circles represent bromodomain assays available in the BROMOscan panel [click image to enlarge].



 
Platform Highlights and Benefits

  • Reports true thermodynamic inhibitor Kd values over a broad affinity range (<100pM to >10 uM)
  • Test compounds do not interfere with assay readout
  • Enables rapid assay development without common bottlenecks
  • Screening & profiling: single or multi-target HTS, selectivity profiling and inhibitor Kd determination
 

How BROMOscan Works: Competition Binding Assays

How it works Bromoscan technology schematic

 

Assay Process and Principle

  • Human bromodomains tagged with DNA
  • Known ligand immobilized on solid support
  • Test compound or DMSO
  • Measure amount of bromodomain bound to immobilized ligand (by qPCR) in the presence and absence of test compound

 

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