High Throuhgput Screening
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Powering lead discovery through High Throughput Screening

Throughout its lifetime, High Throughput Screening (HTS) has made significant contributions to early-stage drug discovery. HTS is the process of rapidly identifying large numbers of active compounds which have the potential to modulate a particular biological pathway, during the process of lead discovery and target validation. Today’s drug discovery labs have come to rely on HTS capabilities, which allows R&D scientists to test between 10,000 and 100,000 compounds per day.

Automated HTS and more recently, ultra high throughput screening (UHTS), provide researchers with the ability to screen huge compound libraries against a constantly increasing number of targets for lead discovery. Automated screening through robotics enables the fast turnaround of screening data and reduces the extent of manual errors, which increases the speed of overall drug discovery.

A number of different technologies, including fluorescence, nuclear magnetic resonance (NMR), affinity chromatography, surface plasmon resonance (SPR) and DNA microarray are used for HTS.

The use of NMR for HTS is gaining popularity in drug discovery, partly due to its key advantage of providing direct information on the affinity of the screening compounds and the binding location of proteins. From this, NMR can elucidate the structure-activity relationship between the drug and the target – a huge step forward in lead discovery.

Ultra High Throughput Screening (UHTS) uses mass spectrometry to rapidly screen through large compound libraries of millions of substances. Pharma labs performing UHTS demand a wide range of capabilities from their sample screening instrumentation. MALDI screening solutions for drug discovery include highly automated workflows, high-volume microplate reading and handling systems, and rapid assay screening times.