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High-throughput screening (HTS) is a method for scientific discovery especially used in drug discovery and relevant to the fields of biology, materials science [1] and chemistry. [ 2 ] [ 3 ] Using robotics , data processing/control software, liquid handling devices, and sensitive detectors, high-throughput screening allows a researcher to ...
In high-throughput screening (HTS), one of the major goals is to select compounds (including small molecules, siRNAs, shRNA, genes, et al.) with a desired size of inhibition or activation effects. A compound with a desired size of effects in an HTS screen is called a hit.
Hit to lead (H2L) also known as lead generation is a stage in early drug discovery where small molecule hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising lead compounds.
Such a molecule might be extracted from a natural product or even be a drug on the market which could be improved upon (so-called "me too" drugs). Other methods, such as virtual high throughput screening, [28] where screening is done using computer-generated models and attempting to "dock" virtual libraries to a target, are also often used. [21]
In drug discovery high-throughput screening, it is desirable to screen a drug target against a selection of chemicals that try to take advantage of as much of the appropriate chemical space as possible. The chemical space of all possible chemical structures is extraordinarily large. Most stored chemical libraries do not typically have a fully ...
Compound management in the field of drug discovery refers to the systematic collection, storage, retrieval, and quality control of small molecule chemical compounds used in high-throughput screening and other research activities to identify hits that can be developed into candidate drugs.
A high throughput assay can be either an endpoint or a kinetic assay usually done on an automated platform in 96-, 384- or 1536-well microplate formats (High Throughput Screening). Such assays are able to test large number of compounds or analytes or make functional biological readouts in response to a stimuli and/or compounds being tested. [6]
Nevertheless, the implementation of Sanger sequencing for decoding DNA-encoded chemical libraries in high-throughput fashion was the first to be described. [18] After selection and PCR amplification of the DNA-tags of the library compounds, concatamers containing multiple coding sequences were generated and ligated into a vector .