3HC8

Investigation of Aminopyridiopyrazinones as PDE5 Inhibitors: Evaluation of Modifications to the Central Ring System.

3HC8 の概要

• エントリーDOI: 10.2210/pdb3hc8/pdb
• 関連するPDBエントリー: 1uho 2chm 2h40 2h42 2h44 3HDZ 3bjc
• 分子名称: cGMP-specific 3',5'-cyclic phosphodiesterase,cAMP-specific 3',5'-cyclic phosphodiesterase 4A, 6-(6-methoxypyridin-3-yl)-2-[(2-morpholin-4-ylethyl)amino]-4-(2-propoxyethyl)pyrido[2,3-b]pyrazin-3(4H)-one, ZINC ION, ... (5 entities in total)
• 機能のキーワード: pde5, pde-5, inhibition, alternative splicing, camp, hydrolase, phosphoprotein, polymorphism allosteric enzyme, cgmp, cgmp-binding, magnesium, metal-binding, nucleotide-binding, zinc
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 37934.56

構造登録者

Hughes, R.O.,Stallings, W.C.,Cubbage, J.W.,Williams, J.M. (登録日: 2009-05-05, 公開日: 2009-07-07, 最終更新日: 2024-05-22)

主引用文献

Hughes, R.O.,Walker, J.K.,Cubbage, J.W.,Fobian, Y.M.,Rogier, D.J.,Heasley, S.E.,Blevis-Bal, R.M.,Benson, A.G.,Owen, D.R.,Jacobsen, E.J.,Freskos, J.N.,Molyneaux, J.M.,Brown, D.L.,Stallings, W.C.,Acker, B.A.,Maddux, T.M.,Tollefson, M.B.,Williams, J.M.,Moon, J.B.,Mischke, B.V.,Rumsey, J.M.,Zheng, Y.,Macinnes, A.,Bond, B.R.,Yu, Y.
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.
Bioorg.Med.Chem.Lett., 19:4092-4096, 2009

PubMed Abstract: Efforts to improve the potency and physical properties of the aminopyridiopyrazinone class of PDE5 inhibitors through modification of the core ring system are described. Five new ring systems are evaluated and features that impart improved potency and improved solubility are delineated.

PubMed: 19539468
DOI: 10.1016/j.bmcl.2009.06.004

実験手法

X-RAY DIFFRACTION (1.79 Å)