Fig. 3
From: In-silico guided chemical exploration of KDM4A fragments hits
Activity of 2-(methylcarbamoyl)isonicotinic acid in in-vitro assays. A Structure of 2-(methylcarbamoyl)isonicotinic acid, namely compound 1. B Dose–response curve of compound 1 against KDM4A. Graph depicts mean and standard deviation of six replicates of the obtained percentage of inhibition at each concentration. Data were fitted using a non-linear 4-parameter logistic model. The obtained IC50 ± its standard error is reported as result of the fitting. Analysis was performed by GraphPad Prism 9.0 software (GraphPad Software, Inc., San Diego, CA, United States). C BLI sensorgrams for compound 1 against KDM4A. Binding constant (KD) value was estimated by globally fitting the BLI response intensity (nm) as a function of compound concentration (μM) with the Octet Data Analysis Software, using a 1:1 Langmuir binding model