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The lower the EC50 the greater the potency of the antagonist, and the lower the concentration of drug that is required to inhibit the maximum biological response.
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Crystallographic studies of AMN107 indeed suggest that subtle differences in the mode of binding to Abl and a better topological fit to the Abl protein account for the greater potency of the drug (Weisberg et al, 2005).
The greater potency of the second-generation drugs is likely the result of a combination of greater in vitro potency and superior pharmacokinetics.
The greater potency of the newer drugs in SCID-hu Thy/Liv mice is consistent with their observed greater potency in HIV-1-infected individuals.
The EC50 values for BR-AEA were at least five-fold lower than for salbutamol, showing the greater potency of the former.
The Ki values from competitive binding assays that employed the MSH 7 -based probe were generally lower than the Ki values obtained when the probe based on NDP-α-MSH 7 -basedoyed, which is consistent with the greater probecy of the latter probe.
Our results likely reflect the greater potency of the HicA toxin when expressed in E. coli.
It is also intriguing to consider the possibility that the greater potency for inhibition of 2-AG oxygenation exhibited by certain NSAIDs against purified protein has implications for understanding the pharmacological properties of these compounds in vivo.
Consequently then, the greater potency of SB203850 - at the level of gene expression - would not necessarily translate into a greater inhibition of the effects of anti-IgM on the cell cycle.
Higher blood cyanide levels in male vs. female mice and in MAN- vs. AN-treated mice may explain the gender-related differences in the toxicity of these chemicals and the greater potency of MAN vs. AN.
The lack of correlation with previous studies may be attributed to the increased sensitivity of flow cytometry and the greater potency of panobinostat compared with other HDAC inhibitors.
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com