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• W2890791185 abstract "It has been a goal of the pharmaceutical industry to provide drugs with as few side effects as possible. In vitro off-target pharmacology assay, which includes receptors, enzymes, and ion channels, is a cost-effective way to increase efficiency in the drug discovery process to achieve that goal. Early in a project, the chemical scaffolds of interest are subjected to a panel of assays. The panel includes not only closely related targets but also targets that are known to have adverse or intolerable side effect in the patient population. The number of assays to include in the panel can get quite extensive and cost-prohibitive, but scientific expertise and experience can help limit the panel to targets that have been shown to be more promiscuous. In addition, the development of in silico modeling using 3-D structures of targets and chemical similarity searches can be used to identify targets of concern. Once the panel for a particular project is identified, the typical approach is to screen the targets using receptor binding. To verify the interactions are truly pharmacological, the hit need to be followed-up with full concentration response curves and functional assays to eliminate false positives. Early in the development process, the prudent use of in vitro pharmacology assays is of significant value to identify selective compounds for the intended target-limiting potential adverse side effects." @default.
• W2890791185 created "2018-09-27" @default.
• W2890791185 creator A5070459960 @default.
• W2890791185 date "2019-01-01" @default.
• W2890791185 modified "2023-10-07" @default.
• W2890791185 title "Use of In Vitro Models in Drug Development and Issue Resolution" @default.
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• W2890791185 doi "https://doi.org/10.1016/b978-0-12-812206-8.00014-5" @default.
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