TABLE 1

IC50 values of SID 26681509 against papain and human cathepsins B, G, K, L, S, and V.


Enzyme

IC50

Selectivity Index

% Identity to Cat L
10 min
30 min
60 min
90 min
μM
Cathepsin L, human liver 0.155 ± 0.012 0.075 ± 0.005 0.056 ± 0.004 0.050 ± 0.003 1 100
Cathepsin V, human, recombinant, NSO cells 1.008 ± 0.146 0.688 ± 0.039 0.618 ± 0.035 0.576 ± 0.024 7-11 78
Cathepsin S, human spleen 1.107 ± 0.134 0.745 ± 0.010 0.724 ± 0.011 0.721 ± 0.029 7-14 55
Papain, C. papaya 6.765 ± 0.367 2.981 ± 0.282 2.600 ± 0.208 1.562 ± 0.314 31-46 48
Cathepsin B, human liver 7.492 ± 0.693 2.983 ± 0.295 2.527 ± 0.073 2.512 ± 0.139 40-50 26
Cathepsin K, human, recombinant, Escherichia coli 17.596 ± 1.040 8.460 ± 0.366 8.442 ± 0.140 6.857 ± 0.063 113-151 58
Cathepsin G, human neutrophil
>50
>50
>50
>50