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In many of the transformations hERG inhibition follows the expected qualitative trends: decreasing lipophilicity, decreasing basicity, and increasing acidity all decrease the potency of hERG blockers.
According to Dr. Woodford, if coca leaves are left out in the sun for too long after being harvested, they can dry out and decrease the potency of cocaine before the drug even hits the market.
Compounds 32 (analog of compound 23) and 33 (analog of compound 28) had poorer MIC profiles than did their lipophilic counterparts, which again confirms the observation that polar groups, particularly groups with hydrogen bond donors such as compound 32, tend to decrease the potency of the AMCs against resistant organisms (Table 3).
Don't skimp on this step adding the alcohol while the mixture is too hot will greatly decrease the potency of the drink!
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The acute stress also selectively decreased the potency of GABA to modulate GABAA receptor-mediated chloride uptake in group-housed females.
One widespread factor that may affect the safety of any medication is environmental exposure to chemicals that have the potential for interactions, including increasing or decreasing the potency of a given drug dose or changing the rate at which the drug is metabolized.
Mutation of Val-349 to Ala enlarges the pocket and increases the potency of indomethacin 3-fold, whereas mutation to Leu reduces the pocket size and decreases the potency of the inhibitor by 16-fold.
In the assessment of VUF 10085, mutation of Ile-2796.59 decreased the potency of VUF 10085 twofold while mutation of Y3087.43 decreased the efficacy to such an extent that no IC50 value could be calculated (Table 2).
The introduction of the human α1 2′Val residue into RDL subunits hugely decreases the potency of the compounds, and Drosophila carrying a 2′ mutation are resistant to ginkgolides, while the introduction of the insect 2′Ala residue into the human α1 subunit results in increased susceptibility.
Similarly compound 5g having p-fluoro substitution decreased the potency, while substitution of phenyl ring with p-nitro group (5k) slightly enhanced the potency.
Partial disruption of the bridge, resulting from mutation of the serine or acidic residue, significantly decreased the potency (i.e., affinity) of clinically relevant quinolones for the enzyme but had relatively little effect on drug efficacy (i.e., maximal drug-induced cleavage).
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com