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Identification of a Novel Series of BET Family Bromodomain Inhibitors: Binding Mode and Profile of I-BET151 (GSK1210151A)

Jonathan Seal, Yann Lamotte, Frédéric Donche, Anne Bouillot, Olivier Mirguet, Françoise Gellibert, Edwige Nicodeme, Gael Krysa, Jorge Kirilovsky, Soren Beinke, Scott McCleary, Inma Rioja, Paul Bamborough, etc.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72.

PMID: 22437115

Abstract:

A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1300031495 GSK1210151A GSK1210151A 1300031-49-5 Price
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