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. Author manuscript; available in PMC: 2017 Oct 18.
Published in final edited form as: Chem Commun (Camb). 2016 Oct 18;52(85):12590–12593. doi: 10.1039/c6cc07083c

Table 1.

Thermodynamic and kinetic parameters for inhibition of cathepsin L by CLIK-148, CLIK-181 and 1-4a

Compound Ki (⍰M) kinact (s−1) kinact/Ki (M−1 s−1)
CLIK-148 1.4 ± 0.7 0.015 ± 0.005 11000 ± 3000
CLIK-181 1.3 ± 0.1 0.020 ± 0.003 15000 ± 2000
1 0.77 ± 0.27 0.011 ± 0.005 13000 ± 2800
2 1.6 ± 0.2 0.015 ± 0.001 9400 ± 1000
3 (dark) 1.0 ± 0.2 0.016 ± 0.002 15000 ± 2000
4 (dark) 14 ± 4 0.008 ± 0.002 570 ± 60
a

Inhibition data were acquired using cathepsin L (4 nM), Z-Phe-Arg-AMC (10 μM), and inhibitor (0.1–2.5 μM) in 0.4 M acetate buffer, pH 5.5, <1% DMSO, 4 mM EDTA, 0.01% Triton X-100, DTT = 8 at 25 °C. Data are averages of 3 independent experiments with errors equal to standard deviations. Data for 3 and 4 were collected under dark conditions. See SI for more details.