4-methyl-N-[(2S)-1-oxo-3-phenyl-1-[[(3S)-1-phenyl-5-(phenylmethoxysulfamoyl)pentan-3-yl]amino]propan-2-yl]piperazine-1-carboxamide

4-Methyl-N-[(2S)-1-oxo-3-phenyl-1-[[(3S)-1-phenyl-5-(phenylmethoxysulfamoyl)pentan-3-yl]amino]propan-2-yl]piperazine-1-carboxamide is a potent and selective small molecule inhibitor of **cathepsin K**, a cysteine protease primarily expressed in osteoclasts and a key mediator of bone resorption. Developed by **Bristol Myers Squibb** as part of a research program targeting metabolic bone diseases, the compound is a peptidomimetic featuring a 4-methylpiperazine-1-carboxamide N-terminal cap and a unique phenylmethoxysulfamoyl (N-benzyloxysulfamoyl) moiety. This moiety serves as a potent binding element that interacts with the S1' subsite of the cathepsin K active site. The compound was identified as a lead in the discovery of clinical candidates for the treatment of **osteoporosis**, demonstrating high potency against the target enzyme and selectivity over other cathepsins such as cathepsin L and cathepsin S.

Other names

Example 101Example101Example-1014-methyl-N-[(1S)-1-benzyl-2-[[(1S)-1-(2-phenylethyl)-3-(benzyloxysulfamoyl)propyl]amino]-2-oxo-ethyl]piperazine-1-carboxamide