CORE--HIGH-THROUGHPUT SCREENING

高通量筛选核心将针对确定的靶标进行小分子文库的筛选。目前，该核心的资源包括超过215，000种单独的药物样化合物，大多数分子大小为250 - 500道尔顿，以及利用光学（荧光，吸光度，发光）或溶液相测定进行高通量筛选的自动化仪器。核心功能包括化合物储存和处理、试验设计和验证、试验执行和数据分析。通过筛选商业购买的化合物类似物（通常为100 - 500）进行验证的"命中"（具有针对靶标的活性的化合物）的初始优化。进一步的"击中领导"的发展将在个别项目中进行协商的核心。该核心将由7个项目用于化合物筛选，其余5个项目用于提供试验用先导化合物。这个核心代表了学术环境中的独特资源。

The high-throughput screening core will carry out the screening of small-molecule libraries against defined targets. Resources of the core at present include more than 215,000 individual, drug-like compounds, most of molecular size 250-500 daltons, and automated instrumentation for high-throughput screening utilizing optical (fluorescence, absorbance, luminescence) or solution-phase assays. Functions of the core include compound storage and handling, assay design and validation, assay execution, and data analysis. Initial optimization of validated 'hits' (compounds with activity against target) is done by screening of commercially purchased compound analogs (typically 100-500). Further 'hit-to-lead' development will be done in individual projects in consultation with the core. The core will be utilized by seven projects for compounds screening and by the five remaining projects for provision of lead compounds for testing. This core represents a unique resource in an academic environment.