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MS-based quantification of the basal/apical transfer rate of a test compound at 2 μM across contiguous monolayers from MDCK (Madin Darby Canine Kidney) cells.
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Ratio from the MS-based quantification of apical/basal and basal/apical transfer rates of a test compound at 2 μM across contiguous monolayers from MDR1-transfected MDCK cells.
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50 value depends on the concentration of glutamate present in the assay, the precise assessment of the ligand efficiency based on this assay was not possible. At the same time, comparison of LE profiles of multiple chemotypes using the same mGluR2 assay provided a valuable perspective when assessing lead generation potential of different chemical series.
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Fluorescence-based measurement of CYP inhibition by incubating the recombinant CYP (Cytochrome P450) with a test compound and the corresponding fluorescent probe at 3 μM.
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3H-dofetilide binding to membranes from hERG-expressing HEK cells at 10 μM.
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64249141114
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In efforts to obtain analogs in solid form, we compared the MPs of small alkoxyphenyl ethers (oils) to benzylphenyl ether (∼40 °C), phenyl ether (∼28 °C) and biphenyl (∼70 °C).
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