0275 Science Center Drive

San Diego, CA, United States

0275 Science Center Drive

San Diego, CA, United States
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Westaway S.M.,Glaxosmithkline | Preston A.G.S.,Glaxosmithkline | Barker M.D.,Glaxosmithkline | Brown F.,Glaxosmithkline | And 28 more authors.
Journal of Medicinal Chemistry | Year: 2016

Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays. © 2016 American Chemical Society.


Westaway S.M.,Glaxosmithkline | Preston A.G.S.,Glaxosmithkline | Barker M.D.,Glaxosmithkline | Brown F.,Glaxosmithkline | And 34 more authors.
Journal of Medicinal Chemistry | Year: 2016

Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-carboxylic acid 39 that are inhibitors of the KDM4 (JMJD2) family of histone lysine demethylases. Compounds 34 and 39 possess activity, IC50 ≤ 100 nM, in KDM4 family biochemical (RFMS) assays with ≥50-fold selectivity against KDM6B and activity in a mechanistic KDM4C cell imaging assay (IC50 = 6-8 μM). Compounds 34 and 39 are also potent inhibitors of KDM5C (JARID1C) (RFMS IC50 = 100-125 nM). © 2016 American Chemical Society.


Kanouni T.,0275 Science Center Drive | Dong Q.,0275 Science Center Drive | Abelovski B.,0275 Science Center Drive | Wallace M.B.,0275 Science Center Drive
Tetrahedron Letters | Year: 2011

A novel, efficient route for the synthesis of 1,8-naphthyridine-2,5-dione compounds is reported. The synthetic scheme allows for diversification at the 4-position of the core, and it was utilized to develop a series of inhibitors for MEK kinase. © 2010 Elsevier Ltd. All rights reserved.

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