Dual inhibitor experiments were performed essentially as before45. Briefly, GM6001 (0–800 nM) was incubated with ADAMTS-5 in the presence and absence of a fixed concentration (10 μM) of compound 4b and QF peptide cleavage assays were run as above. IC50 values were determined in the absence (IC50) and in the presence of 4b (IC50+). In the latter condition, the activity measured in the presence of 4b and ADAMTS-5 alone was taken as 100%.

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