Applications of Biophysics in High-Throughput Screening Hit Validation
نویسندگان
چکیده
منابع مشابه
Hit and lead generation: beyond high-throughput screening.
The identification of small-molecule modulators of protein function, and the process of transforming these into high-content lead series, are key activities in modern drug discovery. The decisions taken during this process have far-reaching consequences for success later in lead optimization and even more crucially in clinical development. Recently, there has been an increased focus on these ac...
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A typical modern high-throughput screening (HTS) operation consists of testing thousands of chemical compounds to select active ones for future detailed examination. The authors describe 3 clustering techniques that can be used to improve the selection of active compounds (i.e., hits). They are designed to identify quality hits in the observed HTS measurements. The considered clustering techniq...
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The high-throughput affinity-selection screening platform SpeedScreen was recently reported by the Novartis Institutes for BioMedical Research as a homogeneous, label-free screening technology with mass-spectrometry readout. SpeedScreen relies on the screening of compound mixtures with various target proteins and uses fast size-exclusion chromatography to separate target-bound from unbound subs...
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High-Throughput Screening (HTS) is widely used in the pharmaceutical industry to identify novel chemical starting points for drug discovery projects. The current study focuses on the relationship between molecular HTS hit rate and four common molecular descriptors: molecular lipophilicity (as described by ClogP), size (heavy atom count, HEV), degree of aromaticity content (Fsp3) and fraction of...
متن کاملImpact of normalization methods on high-throughput screening data with high hit rates and drug testing with dose–response data
MOTIVATION Most data analysis tools for high-throughput screening (HTS) seek to uncover interesting hits for further analysis. They typically assume a low hit rate per plate. Hit rates can be dramatically higher in secondary screening, RNAi screening and in drug sensitivity testing using biologically active drugs. In particular, drug sensitivity testing on primary cells is often based on dose-r...
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ژورنال
عنوان ژورنال: Journal of Biomolecular Screening
سال: 2014
ISSN: 1087-0571,1552-454X
DOI: 10.1177/1087057114529462