A System for LogD Screening of New Drug Candidates Using a Water-Plug Injection Method and Automated Liquid Handler

Abstract

An efficient system for screening for the octanol/water distribution coefficient (logD) was developed. We previously developed a 96-well—based high-speed logD assay system (HSlogD) using a water-plug aspiration/injection method by auto liquid sampler (HTS-PAL) to analyze the water phase without contamination of the upper octanol phase. In this report, we introduce an automated liquid-handling system (Biomek2000) into the previously reported HSlogD system to dilute the octanol phase automatically. As a result, throughput is increased, allowing the analysis of 400 compounds per week with a range of 0 < logD < 5.