The new platform designated as BROMOscan(TM), is based on the proven KINOMEscan(TM) technology and will enable high throughput screening, selectivity profiling and quantitative Kd determinations across several sub-families of bromodomains, including the BET family.
The platform enables screening for selective inhibitors of Bromodomain epigenetic "reader" proteins that bind and recognize acetylated lysine residues on histone tails, which are important epigenetic marks associated with gene expression and regulation. With many drug discovery programs aimed at identifying small molecules that inhibit Bromodomains, the availability of a quantitative and high-throughput platform represents a substantial leap forward and a powerful solution to support new discovery programs while supporting and expediting existing projects.
"With the recent understanding that epigenetics plays a pivotal role in inflammation and oncology, now more than ever the drug discovery community is seeking an enabling platform for high throughput screening of epigenetic targets," said Dr. Pyare Khanna, President & CEO of DiscoveRx. "Our goal was to leverage our in-house expertise platforms to build a high quality, first in class panel of Bromodomain ligand binding assays."
With over 25% coverage of the human bromodomain targets anticipated in the first panel, DiscoveRx extends its leadership position by offering screening and profiling solutions for key drug targets such as GPCRs, Kinases, NHRs and now epigenetic targets. This milestone achievement reaffirms DiscoveRx's continued commitment to invest in developing innovative products and solutions for the drug discovery community.