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Assays & screens

Cell-based prediction of the fraction of free, unbound compound in brain tissue

A high throughput, cell-based assay could predict what fraction of a compound would be free and nonspecifically bound in brain tissue. Membrane dialysis followed by mass spectrometric analysis simultaneously measured the non-protein-bound fractions of multiple compounds in human embryonic kidney cell line homogenates and then used the results to calculate predicted values for the fraction of each compound that would remain unbound in brain tissue. For 40 of 46 compounds tested, the assay results were comparable to values reported in the literature for the fraction of unbound compound in animal brains. Ongoing work includes applying the method to drug development.

SciBX 7(12); doi:10.1038/scibx.2014.354
Published online March 27, 2014

Unpatented; licensing status not applicable

Mateus, A. et al. J. Med. Chem.; published online March 6, 2014;
Contact: Per Artursson, Uppsala University, Uppsala, Sweden