The high cost of compound profiling has restricted its optimum use in early stage drug discovery, which means that companies typically develop lead candidates with SAR and toxicity testing, and only then profile the few resulting compounds for selectivity. A negative result can mean many months of wasted time.
Reaction Biology Corporation (RBC) has pioneered low-cost compound profiling with its Kinase HotSpotSM platform. This 33P radio-labelled assay service is priced lower than competing fluorescent offerings, including over 325 kinases. Discovery programmes can profile more compounds earlier, eliminating non-specific portions of a scaffold. RBC has also used its profiling service to do wide-field discovery – large-scale profiles that highlight the sweet spots in a compound library.
RBC also offers exclusive profiling panels for HDAC and methyltransferase assays. HDAC ProfilerSM includes all HDAC and SIRT isoforms in one panel. HMT HotSpot is the first 3H methyltransferase assay platform optimised for volume screening and profiling. Interest has surged in epigenetic mechanisms implicated in many cancers and other indications. A major impediment to implementing programmes in this area is the lack of a standardised HMT screening platform. RBC has filled this need with HMT HotSpot.
In a time when budgets are under constant review, RBC’s low cost/high quality data can help optimise early stage discovery programmes. For the same budget, RBC can screen and profile more compounds or it can screen a profile for a fixed number of compounds for less than pharmas would likely spend for in-house or outsourced screening. Over 100 large pharma, biotech, and academic clients rely on RBC’s assay services for low cost, high quality data.