Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.

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Moss N, Xiong Z, Burke M, Cogan D, Gao DA, Haverty K, Heim-Riether A, Hickey ER, Nagaraja R, Netherton M, O'Shea K, Ramsden P, Schwartz R, Shih DT, Ward Y, Young E, Zhang Q

Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7189-93. doi: 10.1016/j.bmcl.2012.09.054. Epub 2012 Oct 2.

PubMed ID

23084902 [ View in PubMed

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Abstract

This paper details exploration of a class of triazole-based cathepsin S inhibitors originally reported by Ellman and co-workers. SAR studies involving modifications across the whole inhibitor provide a perspective on the strengths and weaknesses of this class of inhibitors. In addition, we put the unique characteristics of this class of compounds into perspective with other classes of cathepsin S inhibitors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
N-[(1S)-2-[(4-cyano-1-methylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-oxoethyl]morpholine-4-carboxamide	Cathepsin S	IC 50 (nM)	1.5	N/A	N/A	Details
N-[(1S)-2-[(4-cyano-1-methylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-oxoethyl]morpholine-4-carboxamide	Cathepsin S	IC 50 (nM)	0.9	N/A	N/A	Details