ADMETInVitroProfiling – Utility and Applications in Lead Discovery

Edward H. Kerns, Xun Zhang, Li Di · Burger's Medicinal Chemistry and Drug Discovery · 2021

ADMET properties are a vital integral part of drug discovery because they determine the pharmacokinetics and safety of clinical development candidates. Diverse ADMET profiling assays have been developed and implemented to provide property data for drug discovery team decision-making. Their utility and applications in lead discovery include the following: select leads, diagnose poor PK, guide structure modification, solve specific project team property issues, provide accurate biological data for SAR, select compounds for in vivo PK and PD studies, and improve dosing for optimum exposure in vivo. ADMET properties are discussed along with case studies and assays.

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