| Assay Method Information | |
| | Determination of Related Protease Inhibition |
| Description: | In vitro inhibition of related proteases was determined using an (C50 assay 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 enzymes 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 the accumulation of liberated fluorescence from the substrate over 5 mi at 25′C. The linear rate of fluorescence increase per minute was expressed as 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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