Candidate RNAseH inhibitors and data summary.
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1Structures are in Supplemental Fig. S1.2Inhibitory activity in the biochemical RNAseH assay at 10 µM; quantitative data are in Supplemental Table S1. Cutoff values were established relative to the mean and standard deviation of RNAseH activity in the presence of the irrelevant compounds tryptophan, sucrose, and IPTG normalized to the vehicle control. −, Residual activity greater than one standard deviation below the mean irrelevant inhibition (≥43% activity); +/−, Residual activity between one and two standard deviations below the mean irrelevant inhibition (42–34% activity); +, residual activity between two and three standard deviations below the mean irrelevant inhibition (33–25% activity); ++, residual activity less than three standard deviations below the mean irrelevant inhibition (≤24% activity).3Inhibitory activity against HBV replication in Huh7 cells at 10 µM. +, clear inhibition; −, no detectable inhibition; +/−, inhibition observed in some but not most assays.4Napthyridinone [68]; DHBNH, dihydroxy benzoyl naphthyl hydrazone [75], [78]; THBNH, trihydroxy benzoyl naphthyl hydrazone [106]; BHMP07 [78].
创建时间:
2015-12-02



