3Q3B

6-Amino-4-(pyrimidin-4-yl)pyridones: Novel Glycogen Synthase Kinase-3 Inhibitors

3Q3B の概要

• エントリーDOI: 10.2210/pdb3q3b/pdb
• 関連するPDBエントリー: 1PYX 1Q3D 1Q41 1Q4L
• 分子名称: Glycogen synthase kinase-3 beta, 4-(4-hydroxy-3-methylphenyl)-6-phenylpyrimidin-2(5H)-one (3 entities in total)
• 機能のキーワード: kinase, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm : P49841
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 94719.56

構造登録者

Pandit, J. (登録日: 2010-12-21, 公開日: 2011-06-15, 最終更新日: 2024-02-21)

主引用文献

Coffman, K.,Brodney, M.,Cook, J.,Lanyon, L.,Pandit, J.,Sakya, S.,Schachter, J.,Tseng-Lovering, E.,Wessel, M.
6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors
Bioorg.Med.Chem.Lett., 21:1429-1433, 2011

PubMed Abstract: The synthesis and structure-activity relationships for a novel series of 6-amino-4-(pyrimidin-4-yl)pyridones derived from a high throughput screening hit are discussed. Optimization of lead matter afforded compounds with good potency, selectivity and central nervous system (CNS) exposure.

PubMed: 21295469
DOI: 10.1016/j.bmcl.2011.01.017

実験手法

X-RAY DIFFRACTION (2.7 Å)