Secondary Screening

Primary screening allows direct high throughput binding measurements of small compounds without the need for labeling. However, mistakes about target-compound binding usually occur during primary HTS screening. In this role, Creative Biolabs serves an efficient secondary screening platform as complements to HTS assays.

Secondary screening is designed to confirm hits efficacy by a series of functional cellular assays. Secondary screening assays are vital to ensure that hits generated from high throughput screening campaign are reliably translated into leads. The major job of secondary screening is detecting the functional response of the compounds rather than making this assay to be a high throughput format. It can be a second messenger assay or tissue- or cell-based bioassay. Reassurance activity is given in this setting to ensure that compounds are able to modulate in more intact systems rather than simply interacting with the isolated and often engineered protein used in the primary assay. Throughout the confirmation process, the basis of lead series is formed.

Figure 1: Secondary screening analysis of the hit genes identified in the secretion screens (Simpson et al. 2012)

Creative Biolabs has established a secondary platform which is highly probe dependent (fluorescent label) to measure binding activity. The cell-based functional activity assays provide invaluable data for drug candidates screening and characterization. This platform is configured by the addition of Fluorescence Image Plate Reader (FLIPR) dye. This assay is particularly useful in identifying active compounds against disease targets, like GPCRs, ion channel, etc.

With the support of our highly experienced scientists and world-class instruments, Creative Biolabs drives forward and speeds up your drug discovery process by:

• Give consideration to every property of compounds, like SAR, core chemical motifs, physicochemical characters, and ADMET properties, for better assay design.
• Assessing the ease of preparation, potential amenability for parallel synthesis.
• Confirming the functional activities of multiple compounds and targets.
• Undertaking deeper MOA and characterizing target-compound interactions.
• Helping you with medicinal chemistry and pharmacology decision making.

The key advantages of our secondary screening platform include:

• Fast. We use scheduled protocols to get the most efficient assay in the shortest period. Results can run in overnight.
• Flexible. For instance, to support standard labeled biochemical and cell assays, FLIPR can be swap out for a standard multimode reader to build the best system for the next experiment.
• Economical. Lead to spend reduction during hit identification process.

Creative Biolabs has the ability to run multiple assays in parallel, and we dedicate in discovering innovative drugs with superior methodologies and technologies. For more detailed information, please feel free to contact us or directly sent us an inquiry.

Reference

1. Simpson J C, Joggerst B,  Laketa V,  et al. (2012). “Genome-wide RNAi screening identifies human proteins with a regulatory function in the early secretory pathway.” Nature Cell Biology 14: 764–774. doi:10.1038/ncb2510

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