There are two main methods to assess the IC50 shift, dilution method, and non-dilution method. In the dilution method, the compound is preincubated for 30 min with a relatively higher concentration of HLMs (with and without NADPH), and the samples are diluted ten-fold before measuring CYP ...
In contrast, reversible inhibitors exhibited a rightward IC50 shift or no changes in IC50 after pre-incubation with NADPH. Similar IC50 alterations were observed by the co-incubation approach coupled with the 30-minute pre-incubation in the presence of NADPH, suggesting that the IC50 shift ...
Weaker correlation was observed for the shifted IC50 (IC50(T=30)) (R(2)=0.61) and the fold-shift in IC50 (R(2)=0.17). 3.Primary mechanism for poor correlation was depletion of active enzyme at concentrations>1M leading to greater than predicted inhibition in the IC50-shift assay. 4....