| Assay Method Information | |
| | Determination of Related Protease Inhibition |
| Description: | Table 8: In vitro inhibition of related proteases was determined using a single-concentration % inhibition screen and/or IC50 determination at relevant enzymes. Assays were based on standard literature methods (see e.g. Shori et al., Biochem. Pharmacol., 1992,43, 1209; Bouckaert et al., European Journal of Medicinal Chemistry 110 (2016) 181). Human serine protease enzyme Plasma Kallikrein, KLK1, FXa, Plasmin, Thrombin and Trypsin were assayed for enzymatic activity using an appropriate fluorogenic substrate at Km concentration, FXIa at fixed substrate concentration of 100 μM and various concentrations of the test compound. Protease activity was measured by monitoring fluorescence emitted from cleaved substrate over 5 min at 25° C. The linear rate of fluorescence increase per minute was expressed as 10 percentage (%) activity. IC50 values were calculated as the concentration of inhibitor giving 50% inhibition of the uninhibited enzyme activity (100%). |
| Affinity data for this assay | |
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