Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.

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Catalano JG, Deaton DN, Furfine ES, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Willard DH Jr, Wright LL

Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):275-8.

PubMed ID

14684342 [ View in PubMed

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Abstract

The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tert-Butyl(1s)-1-Cyclohexyl-2-Oxoethylcarbamate	Cathepsin K	IC 50 (nM)	26	N/A	N/A	Details