Assay Development

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UNIT 1. ASSAY DEVELOPMENT, ADAPTATION, AND IMPLEMENTATION Unit 1 is a responsible for all assay activities, as well as for post-HTS hit characterization, performing: (a) assay development and adaptation for HTS and HCS, (b) initial characterization of hits through confirmatory assays and ECso/ICsq determination, (c) secondary and orthogonal assays and screens, (d) testing of analogs and chemistry-optimized compounds, and (e) preliminary mode-of-action studies on hits and optimized compounds. Unit 1 surpassed the MLSCN goals with the development and adaptation of 36 primary HTS assays consisting of a variety of read-outs, resulting in 39 screening campaigns thus far. The Unit also developed 27 secondary/counter assays to support the MLSCN projects. Additionally, the Unit supported 22 hit optimization/SAR projects using 41 dose-response assays, generated >24,000 IC50 10-point curves in duplicate and performed >20 mode-of-action studies. Unit 1 is organized into two subunits: subunit 1A will develop and implement all HTS assays, while subunit 1B is responsible for developing and optimizing software algorithms for HCS.