Assay Development

第一单元.试验开发、调整和实施 单元1负责所有检测活动以及HTS命中后表征，执行：（a） HTS和HCS的测定开发和适应性，（B）通过验证性分析对命中进行初始表征 测定和EC 50/IC 50测定，（c）二级和正交测定和筛选，（d）类似物的测试 和化学优化的化合物，以及（e）关于命中和优化的初步作用模式研究 化合物.第1单元通过开发和调整36个初级HTS，超过了MLSCN的目标 由各种读数组成的分析，迄今为止进行了39次筛查活动。该股还 开发了27个二级/计数器分析，以支持MLSCN项目。此外，该股还支助了22次打击 优化/SAR项目使用41个剂量-反应测定，生成了> 24，000个IC 50 10点曲线， 重复并进行了>20项作用方式研究。第1单元分为两个子单元：子单元1A将 开发和实施所有HTS检测，而子单位1B负责开发和优化软件 HCS的算法。

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.