The Development, Characterisation and Application of an OATP1B1 Inhibition Assay in Drug Discovery
نویسندگان
چکیده
Department of Discovery DMPK AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire UK (MI, PB); Department of Medicinal Chemistry AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire UK (RJR); Department of Bioscience AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire UK (RJ); Metabolism and Pharmacokinetics, Bristol-Myers Squibb, 5 Research Pathway, Wallingford, CT, 06492, USA (MGS) DMD Fast Forward. Published on May 15, 2012 as doi:10.1124/dmd.111.042382
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Withdrawing of Article ''Application of Cell-Based Assay Systems for the Early Screening of Human Drug Hepatotoxicity in the Discovery Phase of Drug Development''
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***Removed from the Issue*** Application of Cell-Based Assay Systems for the Early Screening of Human Drug Hepatotoxicity in the Discovery Phase of Drug Development
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The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
The pivotal role of organic anion-transporting polypeptide 1B1 (OATP1B1) in drug disposition has become clear over the last decade. Therefore, an OATP1B1 inhibition assay suitable for use within early drug discovery was developed and characterized. IC(50) estimates for 10 literature compounds using pitavastatin and estradiol-17β-glucuronide as substrates were within 2-fold of each other. In add...
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