J Chromatogr A. 2008 Feb 22;1182(1):72-6. Epub 2008 Jan 9.

High-speed solubility screening assay using ultra-performance liquid chromatography/mass spectrometry in drug discovery.

Yamashita T, Dohta Y, Nakamura T, Fukami T.

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Tsukuba Research Institute, BANYU Pharmaceutical Co. Ltd., 3 Okubo, Tsukuba, Ibaraki 300-2611, Japan. taro_yamashita@merck.com

Abstract

Ultra-performance liquid chromatography (UPLC) was investigated as an alternative to high-performance liquid chromatography (HPLC) for analyzing pharmaceutical drug candidates. We previously developed a 96-well-based high-speed solubility assay system (HSSOL) using HPLC/UV and a LogD assay system (HSLogD) using HPLC/MS [Y. Dohta, T. Yamashita, S. Horiike, T. Nakamura, T. Fukami, Anal. Chem. 79 (2007) 8312]. We have introduced the UPLC/MS system into this previously developed HSSOL system to increase throughput. Results obtained by the UPLC/MS and HPLC/UV systems showed good agreement, validating the usefulness of the UPLC/MS system. A high-speed solubility assay system was developed employing the UPLC/MS system, thereby tripling the throughput.

PMID:: 18207155; [PubMed - indexed for MEDLINE]

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High-speed solubility screening assay using ultra-performance liquid chromatography/mass spectrometry in drug discovery.

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