FlashPlate scintillation proximity assays for characterization and screening of DNA polymerase, primase, and helicase activities [0.03%]
用于DNA聚合酶、引物酶和解旋酶活性表征及筛选的快速平板闪烁接近分析法
D L Earnshaw,A J Pope
D L Earnshaw
DNA replication proteins represent a class of extremely well-established anti-infective drug targets for which improvements in assay technology are required in order to support enzyme characterization, HTS, and structure-activity relationsh...
Comparative Study
Journal of biomolecular screening. 2001 Feb;6(1):39-46. DOI:10.1177/108705710100600106 2001
Single-molecule detection technologies in miniaturized high throughput screening: binding assays for g protein-coupled receptors using fluorescence intensity distribution analysis and fluorescence anisotropy [0.03%]
单分子检测技术在微型高通量筛选中的应用：采用荧光强度分布分析和荧光各向异性法测定G蛋白偶联受体的结合试验
M Rüdiger,U Haupts,K J Moore et al.
M Rüdiger et al.
G Protein-coupled receptors (GPCRs) represent one of the most important target classes for drug discovery. Various assay formats are currently applied to screen large compound libraries for agonists or antagonists. However, the development ...
Comparative Study
Journal of biomolecular screening. 2001 Feb;6(1):29-37. DOI:10.1177/108705710100600105 2001
Development of a homogeneous MAP kinase reporter gene screen for the identification of agonists and antagonists at the CXCR1 chemokine receptor [0.03%]
均质MAP激酶报告基因筛选的开发，用于识别CXCR1趋化因子受体的激动剂和拮抗剂
S Rees,D P Martin,S V Scott et al.
S Rees et al.
Agonist activity at G protein-coupled receptors (GPCRs) that regulate heterotrimeric G proteins of the Galpha(i/o) or Galpha(q) families has been shown to result in activation of the mitogen-activated protein (MAP) kinase cascade. To facili...
Receptor-ligand interactions studied with homogeneous fluorescence-based assays suitable for miniaturized screening [0.03%]
用于小型化筛选的均相荧光测定法研究受体-配体相互作用
A A Scheel,B Funsch,M Busch et al.
A A Scheel et al.
Cell membrane receptors play a central role in controlling cellular functions, making them the target of drugs for a wide variety of diseases. This report describes how a recently developed method, fluorescence intensity distribution analys...
P Lavery,M J Brown,A J Pope
P Lavery
In order to accommodate the predicted increase in screening required of successful pharmaceutical companies, miniaturized, high-speed HTS formats are necessary. Much emphasis has been placed on sensitive fluorescence techniques, but some sy...
Comparative Study
Journal of biomolecular screening. 2001 Feb;6(1):3-9. DOI:10.1177/108705710100600102 2001
Development of a homogeneous time-resolved fluorescence assay for high throughput screening to identify Lck inhibitors: comparison with scintillation proximity assay and streptavidin-coated plate assay [0.03%]
用于高通量筛选Lck抑制剂的均相时间分辨荧光分析法的发展：与闪烁接近共振和链霉抗生物素蛋白包被板测定法比较
N Ohmi,J M Wingfield,H Yazawa et al.
N Ohmi et al.
This study details the development of a homogeneous time-resolved fluorescence (HTRF) high throughput screening assay to identify inhibitors of Lck. HTRF was compared with scintillation proximity and streptavidin-coated plate assays. Becaus...
Comparative Study
Journal of biomolecular screening. 2000 Dec;5(6):463-70. DOI:10.1177/108705710000500609 2000
Development of a fluorescent ligand-binding assay using the AcroWell filter plate [0.03%]
一种采用AcroWell滤板的荧光配体结合试验的发展方法
K J Valenzano,W Miller,J N Kravitz et al.
K J Valenzano et al.
One of the most powerful tools for receptor research and drug discovery is the use of receptor-ligand affinity screening of combinatorial libraries. Early work involved the use of radioactive ligands to identify a binding event; however, th...
Comparative Study
Journal of biomolecular screening. 2000 Dec;5(6):455-61. DOI:10.1177/108705710000500608 2000
Detection of oligonucleotide-ligand complexes by ESI-MS (DOLCE-MS) as a component of high throughput screening [0.03%]
基于ESI-MS的寡核苷酸-配体复合物检测(DOLCE-MS)在高通量筛选中的应用
M J Greig,J M Robinson
M J Greig
With the advent of combinatorial chemistry and high throughput screening, a major bottleneck in the pharmaceutical industry has changed from quickly finding active compounds to limiting them to a manageable number for proper follow-up. With...
Isolation of peptide ligands that inhibit glutamate racemase activity from a random phage display library [0.03%]
从随机噬菌体展示库中分离出抑制谷氨酸消旋酶活性的肽配体
W C Kim,H I Rhee,B K Park et al.
W C Kim et al.
Several new antibacterial agents are currently being developed in response to the emergence of bacterial resistance to existing antibiotic substances. The new agents include compounds that interfere with bacterial membrane function. The pep...
The design and development of an integrated natural products screening database [0.03%]
集成天然产物筛选数据库的设计与开发
T G Holt,C Dufresne,J M Liesch et al.
T G Holt et al.
We designed and developed NEXUS--a new natural products screening database and related suite of software applications--to utilize the spectacular increases in assay capacity of the modern high throughput screening (HTS) environment. NEXUS n...