PCL102H1 Lecture 2: High Throughput Screening

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High throughput screening: fits in the discover/preclinical testing section of the drug discovery pipeline, chemical libraries and chemical space, target-based screening, phenotypic screening. Target based screening: found a protein of interest (from target validation) -> figure out which chemicals might bind to that protein and change the proteins function. Chemical libraries: after having validated our target, we have a protein of interest. Background to screening: chemical space vs. biological space finding chemicals that interact with biological space, biological space is a series of very small islands in a large universe of chemical space. Chemical space is huge: chemical space is the physioco-chemical properties of a drug. In contrast to chemical space, biological islands are very small -> need to figure out what the chances of hitting these biological targets with limited chemical libraries are. Chemical libraries: assumption: the more chemicals we use, the better, represent a valuable research asset for a drug company.

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