Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.

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Altmann E, Cowan-Jacob SW, Missbach M

Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.

J Med Chem. 2004 Nov 18;47(24):5833-6.

PubMed ID

15537340 [ View in PubMed

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Abstract

Starting from the high-throughput screening hit 1a, novel cathepsin K inhibitors have been developed based on a purine scaffold. High-resolution X-ray structures of several derivatives have revealed the binding mode of these unique cysteine protease inhibitors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
6-(cyclohexylamino)-9-[2-(4-methylpiperazin-1-yl)-ethyl]-9H-purine-2-carbonitrile	Cathepsin K	IC 50 (nM)	6	N/A	N/A	Details
9-CYCLOPENTYL-6-[2-(3-IMIDAZOL-1-YL-PROPOXY)-PHENYLAMINO]-9H-PURINE-2-CARBONITRILE	Cathepsin K	IC 50 (nM)	3.5	N/A	N/A	Details