Small-molecule Screening

These screens use purified proteins and substrates in buffered solutions to produce an optical (fluorescent, luminescent, etc.) readout that monitors enzymatic or binding activity. In this types of screens, small compound inhibitors are ranked by the signals, referring to targeted protein function.

Examples:

• FRET substrates for proteases

• Fluorophore-tagged glycosides for glycosidases

• HDAC-Glo for HDACs

• NADP-Glo for NADP-utilizing enzymes

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These screens can be macromolecular or small-molecule screens that utilize cells plated in 96 or 384 or 1536 well plates to produce visual phenotypic or signal changes in the cells. The measurement can be a signal- or image-based readouts.

Examples:

• Promoter-driven expression of luciferase (firefly, NanoLuc, Lucia) 

• Promoter-driven expression of fluorescent proteins 

• Luciferase- or FP-tagged proteins

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