The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor-Reference-Cited by-同舟云学术

The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor

Published:2014-09-24 Issue:19 Volume:57 Page:8111-8131
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Gosmini Romain¹²,Nguyen Van Loc¹²,Toum Jérôme¹²,Simon Christophe¹²,Brusq Jean-Marie G.¹²,Krysa Gael¹²,Mirguet Olivier¹²,Riou-Eymard Alizon M.¹²,Boursier Eric V.¹²,Trottet Lionel¹²,Bamborough Paul¹²,Clark Hugh¹²,Chung Chun-wa¹²,Cutler Leanne¹²,Demont Emmanuel H.¹²,Kaur Rejbinder¹²,Lewis Antonia J.¹²,Schilling Mark B.¹²,Soden Peter E.¹²,Taylor Simon¹²,Walker Ann L.¹²,Walker Matthew D.¹²,Prinjha Rab K.¹²,Nicodème Edwige¹²

Affiliation:

1. Candidate Discovery, ‡Discovery Biology, §DMPK, GlaxoSmithKline Les Ulis, Centre de Recherches François Hyafil, GlaxoSmithKline R&D, 25 Avenue du Québec, 91140 Villebon-sur-Yvette, France

2. Epinova Discovery Performance Unit, ⊥Computational & Structural Chemistry, #Experimental Medicine Unit, ∇Biological Sciences, ○Exploratory Development Sciences, ◆Discovery Partnerships Medicinal Chemistry, GlaxoSmithKline Stevenage, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm5010539

Reference41 articles.

1. HDL as a target in the treatment of atherosclerotic cardiovascular disease

2. Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

3. Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

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