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. 2023 Mar 3;66(6):3818–3851. doi: 10.1021/acs.jmedchem.2c01360

Table 1. Kinetic Parameters of Dipeptide Nitriles 1a and 1b and Dipeptide Alkynes 2a and 2b with Respect to Cathepsins B, S, L, and Ka.

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compound R CatB CatS CatL CatK
Ki (μM)
1a F 0.109 ± 0.023 0.406 ± 0.040 0.661 ± 0.011 25.94 ± 0.58
1b H 0.042 ± 0.003 0.046 ± 0.004 0.220 ± 0.004 8.81 ± 0.17
kinact/KI (M–1 s–1)
2a F 22 ± 2 58 ± 1 30 ± 3 3 ± 0,1
2b H 85 ± 3 682 ± 85 281 ± 30 48 ± 5
a

Data shown are mean values ± SEM of three experiments, each performed in duplicate.