Use of cryopreserved transiently transfected cells in high-throughput pregnane X receptor transactivation assay [0.03%]
用于高效孕烷X受体转录激活试验的冷冻瞬时转染细胞的应用
Zhengrong Zhu,Jaime Puglisi,David Connors et al.
Zhengrong Zhu et al.
Cryopreserved, transiently transfected HepG2 cells were compared to freshly transfected HepG2 cells for use in a pregnane X receptor (PXR) transactivation assay. Assay performance was similar for both cell preparations; however, cryopreserv...
Comparative Study
Journal of biomolecular screening. 2007 Mar;12(2):248-54. DOI:10.1177/1087057106297828 2007
Miniaturized receptor binding assays: complications arising from ligand depletion [0.03%]
微型化受体结合实验中的配体耗竭问题
Clare M Scaramellini Carter,Juliet R Leighton-Davies,Steven J Charlton
Clare M Scaramellini Carter
The advent of miniaturized assay formats has made possible the screening of large numbers of compounds against a single target, known as high-throughput screening. Despite this clear advantage, assay miniaturization also increases the risk ...
A novel platform for accelerated pharmacodynamic profiling for lead optimization of anticancer drug candidates [0.03%]
一种针对抗癌药物候选化合物优化的新平台以加速药动学谱分析
Jeffrey Szwaya,Charles Bruseo,Enkeleda Nakuci et al.
Jeffrey Szwaya et al.
Oncology drug discovery is, by definition, a target-rich enterprise. High-throughput screening (HTS) laboratories have supported a wide array of molecularly targeted and chemical genomic approaches for anticancer lead generation, and the nu...
Alternative statistical parameter for high-throughput screening assay quality assessment [0.03%]
高通量筛选实验质量评估的统计参数替代指标研究
Yunxia Sui,Zhijin Wu
Yunxia Sui
High-throughput screening is an essential process in drug discovery. The ability to identify true active compounds depends on the high quality of assays and proper analysis of data. The Z factor, presented by Zhang et al. in 1999, provides ...
Drug-membrane interactions studied in phospholipid monolayers adsorbed on nonporous alkylated microspheres [0.03%]
药物与单层磷脂分子膜相互作用的研究吸附在非多孔烷基化微球上
Viera Lukacova,Ming Peng,Gail Fanucci et al.
Viera Lukacova et al.
Characterization of interactions with phospholipids is an integral part of the in vitro profiling of drug candidates because of the roles the interactions play in tissue accumulation and passive diffusion. Currently used test systems may in...
Automated multiple ligand screening by frontal affinity chromatography-mass spectrometry (FAC-MS) [0.03%]
自动化亲和色谱-质谱法筛选多种配体
William Ng,Jin-Rui Dai,Jacek J Slon-Usakiewicz et al.
William Ng et al.
High-throughput screening (HTS) efforts to discover "hits" typically rely on the large-scale parallel screening of individual compounds with attempts to screen mixtures of compounds typically and, unfortunately, giving rise to false positiv...
High-throughput liberation of water-soluble yeast content by irreversible electropermeation (HT-irEP) [0.03%]
高通量不可逆电穿孔高效释放酵母水溶性成分技术(HT-irEP)
Maxim Zakhartsev,Carmen Momeu,Valentina Ganeva
Maxim Zakhartsev
The article describes a high-throughput method for the liberation of water-soluble cell contents by exploiting the phenomenon of irreversible membrane electropermeation (HT-irEP). The method is exemplified in recombinant proteins and plasmi...
Scintillation proximity assay as a high-throughput method to identify slowly dissociating nonpeptide ligand binding to the GnRH receptor [0.03%]
闪烁接近分析法作为高通量识别缓慢解离非肽配体结合GnRH受体的方法
Christopher E Heise,Susan K Sullivan,Paul D Crowe
Christopher E Heise
Many nonpeptide antagonists of the gonadotropin-releasing hormone (GnRH) receptor, as well as other drug targets, possess a broad range of dissociation kinetic rate constants. Current methods to accurately define kinetic rate parameters suc...
Image-based screening for the identification of novel proteasome inhibitors [0.03%]
基于图像的筛选用于新型蛋白酶抑制剂的鉴定
Linda Rickardson,Malin Wickström,Rolf Larsson et al.
Linda Rickardson et al.
The proteasome is a new, interesting target in cancer drug therapy, and the proteasome inhibitor bortezomib has shown an effect in myeloma patients. It is of interest to efficiently discover and evaluate new proteasome inhibitors. The autho...
Development and validation of a high-throughput screen for inhibitors of SARS CoV and its application in screening of a 100,000-compound library [0.03%]
高通量筛选SARS冠状病毒抑制剂的方法的建立及其在筛选化合物库中的应用
William E Severson,Nice Shindo,Mindy Sosa et al.
William E Severson et al.
The authors have developed a high-throughput screen (HTS) that allows for the identification of potential inhibitors of the severe acute respiratory syndrome coronavirus (SARS CoV) from large compound libraries. The luminescent-based assay ...