High Througput Screening
High throughput screening (HTS) remains a critical step in the discovery of lead chemical structures for novel drug targets, including ion channels, GPCRs, kinases, and transporters. To increase the probability of finding new leads from HTS, many labs have invested heavily in expanding both the diversity and quality of compound libraries.
For most drug discovery labs, the library collection has grown from 400,000 to 1 million or more compounds. The standard paradigms used to screen these libraries have evolved to automated 384-well or higher density single compound test formats. Minimal throughput of 30,000 (ideally > 100,000) compounds per day is required.
A primary screen is designed to rapidly identify hits from compound libraries. The goals are to minimize the number of false positives and maximize the number of confirmed hits. Depending on the assay, hit rates typically range between 0.1 and 5 percent. This number also depends on the cutoff parameters set by the researchers, as well as the dynamic range of a given assay.
Typically, primary screens are run in multiplets (i.e., two, three, or more assay data points) of single compound concentrations. Readouts are expressed as percent activity in comparison to a positive (100 percent) and a negative (0 percent) control. Hits are then retested, usually independently from the first assay. If a compound exhibits the same activity, it is termed a confirmed hit, which proceeds to secondary screens or lead optimization.
Molecular Devices provides several screening platforms to support high-throughput screening for ion channel, GPCR, kinase, and transporter target classes as well as others. Please select among the links below to learn how we can help drive the success of your drug development, bioanalytical, and life science research lead identification efforts.