Chemistry Biology and Technology

The technologies such as (combinatorial) chemistry, robotics, cell-based assays, miniaturization, and genomic sciences is starting to change the drug discovery process significantly. Thus, the effective use of HTS depends largely on the effective synergy between these disciplines. Screening, therefore, is the link between biology (targets) and chemistry (druglike molecules). In the age of genomics and combinatorial chemistry, that link must achieve high throughput. Figure 2 illustrates the unification of targets, compounds, and assays in screening applications for drug discovery.

At the screening rates enabled by HTS and ultra-HTS (uHTS) applications, reagent consumption is a critical factor. Cost reduction will not come from economics of scale of the microminiaturized systems but from reductions in the costs of reagents and manpower [3]. Approximately three-quarters of the costs of screening derive from the costs of both chemical and biological reagents. Miniaturization of HTS results in three significant benefits that address the pharma-

Figure 2 The integration of the three primary components of drug discovery screening: compounds, targets, and assays.

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