Identification and Strategies to Mitigate High Total Clearance of Benzylamine-Substituted Biphenyl Ring Systems

Autor: Beth Williamson, Lindsay McMurray, Scott Boyd, Olga Collingwood, Neville McLean, Jon Winter-Holt, Christina Chan, Aixiang Xue, William McCoull
Rok vydání: 2022
Předmět:
Zdroj: Molecular pharmaceutics. 19(7)
ISSN: 1543-8392
Popis: 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
Databáze: OpenAIRE