Trends in Pharmacological Sciences
PrinciplesThe Cheng-Prusoff relationship: something lost in the translation
References (7)
- et al.
Life Sci.
(1989) - et al.
Br. J. Pharmacol.
(1959)
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2022, European Journal of PharmacologyCitation Excerpt :Receptor binding isotherms and concentration/dose-response curves were analysed by nonlinear regression using Origin 6.0 (OriginLab Corp., Northampton, MA), Prism 5.0 (GraphPad Software Inc., La Jolla, CA, USA) or Statistica 8 (Dell) software; all programs gave identical results. From the IC50 values, inhibition constants (Ki) were calculated by the Cheng-Prusoff equation (Cheng and Prusoff, 1973); antagonist affinity (KB) values were calculated according to the formula described by Craig (1993). For [35S] GTPγS binding, raw data were first converted to specific binding, then stimulation % above basal values.
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2015, European Journal of Medicinal ChemistryCitation Excerpt :Data from the binding experiments were fitted to the equation % Bound = 100% Bound/(1+([L]/IC50)n). Since the concentrations of [3H]epibatidine used in the binding experiments were lower than the KD values determined for the radioligands the respective receptors, it was deduced from the Cheng–Prusoff equation [44] that the Ki values for the compounds were similar to the obtained IC50 values. The concentration-response curves for agonists and concentration–inhibition curves for antagonists in the FLIPR Membrane Potential Blue assay were constructed based on the differences in the fluorescence units (△FU) between the maximal fluorescence levels recorded before and after addition of eight different concentrations of the various ligands.