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In vitro drug screening

Published on October 30, 2025   8 min

A selection of talks on Biochemistry

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0:00
My name is Dr. Wayne Carter. This lecture is entitled In Vitro Drug Screening.
0:08
Systematic Screening Rationale. For compounds with potential biological efficacy, there's a need to assess their activity, and this is further tested and validated using specific biochemical and cellular assays.
0:25
Bioassays. Bioassays are undertaken to establish a concentration-response curve for the drug to target binding. They determine the effective dose (ED) or inhibitor concentration (IC) responses that relate to drug potency. Ideally, they should be rapid, cost-effective, and facilitate high-throughput drug screening methods. An example is spectrophotometric measurements of enzymatic activity, in which a concentration curve for drug binding is considered with associated enzymatic inhibition, and these are performed in microtitre plates. For example, the one shown is a 384-well plate. You can get ones that are 96-well, or even 1000 or more wells.
1:14
Drug-Target Binding. An example, central nervous system (CNS) drug assessment as inhibition of cholinesterase, so cholinesterase inhibitors, and this is the first-line treatment for Alzheimer's disease. In the panel, we have a concentration curve of inhibition of butyrylcholinesterase by ethopropazine hydrochloride. On the y-axis is optical density. This is a spectrophotometric colour assay in which there is an increase in coloured product depending on the enzymatic activity. The ethopropazine hydrochloride is present at between nought and 30 nanomolar. With increasing drug concentration, there's a flattening of the line consistent with more enzymatic inhibition.

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In vitro drug screening

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