… Azepanone-based compounds were first reported as orally bioavailable and extremely potent
inhibitors of cathepsin K, as shown by the pharmacokinetic studies in the rat [141]. Marquis …

… K and showed an improved selectivity profile against other cathepsins. Structural … (R)-2, a
potent human cathepsin K inhibitor (IC 50 = 3 nM) that is selective versus cathepsins B (IC 50 = …

… Compound 9 is a potent inhibitor of cathepsin K (K i, app = 10 nM), but now exhibits initial
inhibition kinetics (1–30 min) consistent with a rapidly reversible mechanism of …

… Because of the high potency and selectivity for Cathepsin K inhibition, we deemed 4 an
excellent lead for further evaluation in a medicinal chemistry program. Our SAR investigation (…

… Many potent aldehyde inhibitors have also been isolated from … most potent catB inhibitors,
with an IC50 of 9.2 ng/mL (21.5 nM) [94]. Another potent inhibitor of catB and also cathepsin L (…

… SID 26681509), a potent inhibitor of human cathepsin L (EC 3.4.22.15… with cathepsin L, this
compound became even more potent, … and slowly reversible competitive inhibitor. Through a …

… is not fatal, as demonstrated by cathepsin L gene knockout mice, which are viable and live
… human and parasitic cysteine proteases for the design and synthesis of potent inhibitors as …

… been followed to identify potent inhibitors of members of the cathepsin family of … for potent
inhibitors of human cathepsin L. In the search for novel inhibitory peptides of human cathepsin …

… 2 and 3 which are potent inhibitors of human cathepsin K displaying potent … potent inhibitor
of human cathepsin K (K i = 0.0048 nM) and a sufficiently potent inhibitor of rat cathepsin K to …

… found to be a potent inhibitor of cathepsins K and L with a K i value of 50 nM for cathepsin
K. … 2 by a 1-cyanoazetidine increased the potency of the inhibitor by 10-fold. This increase in …