Compound 3 vs. Compound 8: primary activity and in vitro ADME profiling.
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aIC50 values (nM) were obtained as described in the Methods section.bMetabolic stability is reported as percentage of the original compound, at 1 µM, that remained after the incubation with liver microsomes from different species for 15 minutes.cIC50 values are reported as µM and were calculated in duplicate from radioligand binding assays using [3H]-astemizole.dPe values, reported as 10-6 cm/s were calculated by LC/MS/MS after 4 hours of incubation at 2 µM. Details for these three in vitro ADME assay conditions can be found at http://www.wuxiapptec.com/.
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2015-12-02
