Exact(41)
The dianionic conjugate inhibited hASBT with moderate potency but was not a substrate.
Substitutions with electron-donating groups at phenyl ring like methoxy (compounds 8a, 8b and 8c) showed moderate potency against RT.
However, the Achilles' heel of flavonols as drug candidates is their moderate potency and poor pharmacokinetic profiles.
For comparison, the effects of another compound NS1643 was in-parallel assessed, which also acts primarily to attenuate channel inactivation with moderate potency.
Selected compounds were then tested in a functional cAMP stimulation assay and found to act as 5-HT6 althoughsts, although with moderate potency at the micromolar level.
The compound has showed good selectivity towards FLT3 kinase, associated with a moderate potency, with an IC50 value of 1.74 μM.
Similar(19)
Most compounds showed moderate potencies in micromolar range, with the most promising analogue 6f showing active at submicromolar concentration against HT-1080 cellsr cells which was selected to investigate the antitumor mechanisms.
The pathway slices thus represent knowledge-based aggregations of individual assay results and serve to highlight bioactivity in cases where singular assay components demonstrated only low-to-moderate potency.
Most of synthesized compounds showed moderate enzymatic potency at the same order of magnitude, and compound 12b possessed better potency to the positive control (3.8 μM vs 13.0 μM).
Both of these chemical classes displayed moderate inhibitory potency against SUMO E1.
The results indicated that most of them exhibited potent Bcr Abl inhibition and moderate antiproliferative potency against K562 cells.
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