Administration and Mgmt (California)

高通量筛选（HTS）利用自动化、化学、生物学和信息技术来快速分析药物样分子的药理活性。应用于药物发现，它已经成功地发现了上市药物的前体以及各种细胞和生化途径的探针。斯克里普斯佛罗里达是斯克里普斯研究所分子筛选中心（SRIMSC）的“超”HTS （uHTS）实施核心的所在地。核心人员负责开发和实施SRIMSC的筛选分析，管理分子库小分子库（MLSMR）筛选收集的bbbb360,000个样本，每天筛选超过100万个样本的MLSMR库，质量控制和报告所有筛选结果到NIH的公共数据库（PubChem），化学信息学支持和SRIMSC的整体项目管理。核心通过筛选整个MLSMR化合物库，每年针对超过25个独特的目标，为NIH维持全面的生产能力。在撰写本文时，核心人员已经完成了175个分子靶点的185个高通量筛选活动，测试了4000多万口井。工作人员还执行低通量生物测定，以支持SRIMSC的命中探针药物化学工作，每年参与50多个探针开发项目。核心筛选的靶标类别包括受体、转录因子、转移酶、水解酶、氧化还原酶、裂解酶、异构酶和连接酶；蛋白质相互作用（蛋白质-蛋白质，蛋白质- dna和蛋白质- rna）和表型生物测定。靶标已被纯化用于筛选（如酶或蛋白质）或在全细胞哺乳动物、细菌、昆虫、酵母/真菌和寄生虫系统中进行检测。筛选形式包括生化酶和结合亲和力测定，以及全细胞报告基因、第二信使、膜电位、离子通量、互补、蛋白质构象、复性和毒性测定。各种基于平板的检测格式，包括动力学（FLIPR, Alphascreen, TR-FRET， FP等）和高含量分析（HCA）用于筛选工作。更多信息请访问：http://hts.florida.scripps.edu/

High Throughput Screening (HTS) leverages automation, chemistry, biology and information technologies to rapidly assay the pharmacologic activity of drug-like molecules. As applied to drug discovery, it has been successful for discovering the precursors of marketed drugs as well as probes of various cellular and biochemical pathways. Scripps Florida is the home of the "ultra" HTS (uHTS) Implementation core of the Scripps Research Institute Molecular Screening Center (SRIMSC). Core staff are responsible for developing and implementing the SRIMSC's screening assays, managing the Molecular Libraries Small Molecule Repository (MLSMR) screening collection of >360,000 samples, screening the MLSMR library at a throughput in excess of 1 million samples per day, quality control & reporting of all screening results to the NIH's publically available database (PubChem), cheminformatics support and overall project management for the SRIMSC. The core sustains full production capabilities for the NIH by screening the entire MLSMR compound library against more than 25 unique targets per year. As of this writing core staff have completed more than 185 high throughput screening campaigns for 175 molecular targets, with more than 40 million wells tested. Staff also execute lower-throughput bioassays to support the SRIMSC's hit-to-probe medicinal chemistry efforts, participating in more than 50 probe development projects per year. Target classes screened by the core include receptors, transcription factors, transferases, hydrolases, oxidoreductases, lyases, isomerases and ligases; protein interactions (protein-protein, protein-DNA, and protein-RNA) and phenotypic bioassays. Targets have been purified for screening (e.g. enzymes or proteins) or assayed in whole-cell mammalian, bacterial, insect, yeast/fungal, and parasite systems. Screening formats include biochemical enzymatic & binding affinity assays, as well as whole-cell reporter gene, second messenger, membrane potential, ion flux, complementation, protein conformation, renaturation and toxicity assays. A variety of plate-based detection formats including kinetic (FLIPR, Alphascreen, TR-FRET, FP etc.) and high content analysis (HCA) are utilized for screening efforts. More information can be found at: http://hts.florida.scripps.edu/