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The specificity of the assay has been evaluated by Bhhlmann Laboratories AG and all measured compounds show less than 0.05% cross-reactivity.
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Some recent studies have shown the importance of highly selective chromatographic separation for the accurate quantitation of measured compounds [ 22, 24, 34].
10 Owing to the enormous specificity and sensitivity of the MS analyser for deuterated substances (requiring as little as 0.5 ng/mL of analyte), urine samples are readily measured for target compounds showing prolonged elimination times and, thus, might support expanded detection windows and retrospectivity.
Both compounds show a decrease in EC50 value with W261A TAS2R16.
Some of these compounds show as iNOS inhibition percentage near of 100% at a concentration of 50 μM, and the IC50 values measured for the more potent compounds are in a range of 20 40 μM.
Curve class 1 compounds show complete response, whereas curve class 2 compounds show partial response.
Both compounds showed noncompetitive inhibition kinetics when measured against tryptamine at saturating concentrations of SAM.
In this study, lipophilicity (measured by a similar parameter, clogD) for drugs, metabolites and library compounds showed that the distribution of library compounds is similar to that of drugs, but differ markedly from metabolites and that metabolites are more hydrophilic than both drugs and library compounds.
Both compounds showed significant inhibition of E2-stimulated ERα transcriptional activity in the two cell lines as measured by the luminescence signal.
Representative compounds showing activity at the CB2R were also assessed for activity at the CB1R again using a complementation immunoassay measuring levels of β-galactosidase (β-gal) labelled cAMP, analogous to the assay used to measure CB2R activity.
The compounds showed no toxic effects.
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