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Start Over Author "Aixiang Xue" Journal molecular pharmaceutics
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1. Identification and Strategies to Mitigate High Total Clearance of Benzylamine-Substituted Biphenyl Ring Systems

Author

Beth Williamson, Lindsay McMurray, Scott Boyd, Olga Collingwood, Neville McLean, Jon Winter-Holt, Christina Chan, Aixiang Xue, and William McCoull

Subjects
Benzylamines, c-Mer Tyrosine Kinase, Metabolic Clearance Rate, Drug Discovery, Biphenyl Compounds, Hepatocytes, Pharmaceutical Science, Molecular Medicine, Animals, Models, Biological, Rats
Abstract

For most oral small-molecule projects within drug discovery, the extent and duration of the effect are influenced by the total clearance of the compound; hence, designing compounds with low clearance remains a key focus to help enable sufficient protein target engagement. Comprehensive understanding and accurate prediction of animal clearance and pharmacokinetics provides confidence that the same can be observed for human. During a MERTK inhibitor lead optimization project, a series containing a biphenyl ring system with benzylamine

Published
2022

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