Target assay technology

The first step in the process involves the development of a suitable HTS assay format. A more detailed discussion of the formats available for HTS by target class are outlined later in this chapter. This section will focus on some of the practical considerations to determine the proper assay technology for an HTS campaign. 

The truth most likely lies somewhere in between. Bender [67] published the most quantitative study to date on the success of HTS at Novartis. Several conclusions could be drawn. Particular target types and assay technologies have a great impact on screening success, and this was not always correlated to the number of identifying hits in the HTS runs. For assay formats used a minimum of five times, LC/MS readouts succeed 83% of the time, followed by FP assays, which succeed in 72% of the cases. TR-FRET showed a success rate of 70%, with FLIPR assays (61%), fluorescence intensity readouts (59%), and AlphaScreen (60%) performing... 

G Zhao, TI Meier, WK Yeh. Penicillin-binding proteins as antimicrobial targets expression, purification, and assay technologies. In HA Kirst, WK Yeh, MJZmijew-ski, Jr., eds. Enzyme Technologies for Pharmaceutical and Biotechnological Applications. New York Marcel Dekker, 2001, pp. 263-287. 

Penicillin-Binding Proteins as Antimicrobial Targets Expression, Purification, and Assay Technologies... 

Fig.1 HTS assays connect target biology and screening technology. 3D cell image is reproduced from http // www.ebi.ac.uk/microarray/biologyJntro.html and ref therein...

HTS-compatible assay technologies for general assay formats to target classes or types adapted and updated from [4])... 

Cellular Assays Live cell assays fully automate sample handling and quantify cellular characteristics such as motility, proliferation, and morphology. This functional assay technology is amenable to high-throughput analysis, and therefore it is complementary to many proteomic technologies focused on identification of potential therapeutic targets. 

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