Our method has proven to be effective at generating large amounts of crystallographic data but lacks an equally high-throughput and automated means of validating those hits via assays. Here, we still relied upon the purchase of pure compounds (Fig. ), or resynthesis in-house using conventional chemistry, but efforts have been made in measuring Kd from crude reaction mixtures, which may combine efficiently with the novel pulsed injection schemes implemented for the time-resolved kinetic analysis using grating-coupled interferometry. Automated methods will also be needed to systematically analyse and rationalise the data resulting from these increasingly large high-throughput crystallographic screenings.