Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.

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Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH Jr, Wright LL

Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3425-9.

PubMed ID

15177446 [ 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 S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(2R)-3-Methyl-1-phenyl-2-butanyl [(2S)-1-oxo-2-hexanyl]carbamate	Cathepsin K	IC 50 (nM)	0.5	N/A	N/A	Details
1-(PHENYLMETHYL)CYCLOPENTYL[(1S)-1-FORMYLPENTYL]CARBAMATE	Cathepsin K	IC 50 (nM)	0.35	N/A	N/A	Details