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Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis
Christopher A Willoughby1, Herbert G Bull, Margarita Garcia-Calvo
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. willoughby@merk.com
Bioorganic & Medicinal Chemistry Letters
|July 20, 2002
Abstract:
A novel class of small molecule human granzyme B inhibitors is reported. Compound 20 has a K(i) of 7 nM against human granzyme B and blocks CTL mediated apoptosis with an IC(50) of 3 micromolar.