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- W3021488032 abstract "Publisher SummaryThe measurement of drug-like properties accelerated during the 1990s for the purpose of reducing the attrition of clinical compounds during development, owing to poor biopharmaceutical properties. In vitro property measurement provided a cost-effective and successful strategy for improving absorption, distribution, metabolism, excretion, and toxicity (ADME/Tox) properties and led to improved human pharmacokinetics (PK) and bioavailability. Property measurement has benefited another major drug discovery area in an unexpected manner. The availability of property data led to the recognition that physicochemical and biochemical properties are also related to the performance of compounds in biological assays. Drug-like property activities began with living systems (animals to humans), by improving the delivery of compounds to the therapeutic target through improvement of PK and reduction of toxicity. Potential property barriers at each stage of biological testing are summarized and the effects of individual properties on biological assays are discussed. Various approaches are used to deal with insolubility of compounds in bioassays. Awareness of the potential problem is the first step. It is useful to assess the solubilities of compounds early. Several commercial software programs predict aqueous solubility from the molecular structure." @default.
- W3021488032 created "2020-05-13" @default.
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- W3021488032 date "2008-01-01" @default.
- W3021488032 modified "2023-09-24" @default.
- W3021488032 title "Effects of Properties on Biological Assays" @default.
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- W3021488032 doi "https://doi.org/10.1016/b978-012369520-8.50041-3" @default.
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