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The addition of the BODIPY-FL fluorophore resulted in molecules with much reduced potency, which was probably due to a reduction in affinity, as no binding was detectable.
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The binding mode was similar to that of A66, although the Chemscore was much lower in the absence of the predicted carboxamide-mediated hydrogen bonds (8.44 compared with 17.46), suggesting reduced potency.
But a 2012 study suggested that the antibodies would have reduced potency if made in CHO cells.
This is consistent with the relatively reduced potency of wogonin compared with the other two flavones.
The reduced potency at Arg292Cys may have resulted predominantly from an effect on binding (Roberts and Evans, 2007).
The 3-chloro analogue (14) showed reduced potency relative to lead 3.
GlyB4Gln was expected to have a higher potency than hagfish insulin, but it exhibited a marginally reduced potency compared to that of hagfish.
They also showed the same pattern of activity as paclitaxel, with higher potency to paclitaxel-sensitive cell lines and reduced potency against paclitaxel-resistant cell lines.
We also checked fostriecin against commercially obtained PP2A dimeric enzyme reacted with myelin basic protein as the substrate, and again the potency was much reduced relative to our expectations.
Removal of the bromine reduces potency >6-fold, and removal of both the bromine and methyl groups reduces potency ≥10-fold (Table 2).
The controlled-current EC method was shown to assess such a cumulative reducing potency.
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