2VWV

ephB4 kinase domain inhibitor complex

2VWV の概要

• エントリーDOI: 10.2210/pdb2vwv/pdb
• 関連するPDBエントリー: 2BBA 2VWU 2VWW 2VWX 2VWY 2VWZ 2VX0 2VX1
• 分子名称: EPHRIN TYPE-B RECEPTOR 4, N'-(3-CHLORO-4-METHOXY-PHENYL)-N-(3,4,5-TRIMETHOXYPHENYL)-1,3,5-TRIAZINE-2,4-DIAMINE (3 entities in total)
• 機能のキーワード: tyrosine-protein kinase, receptor tyrosine kinase, kinase, mutant, membrane, receptor, transferase, atp-binding, polymorphism, glycoprotein, transmembrane, phosphoprotein, unphosphorylated, nucleotide-binding
• 由来する生物種: HOMO SAPIENS (HUMAN)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34352.66

構造登録者

Read, J.,Brassington, C.A.,Green, I.,McCall, E.J.,Valentine, A.L.,Kettle, J.G.,Leach, A.G. (登録日: 2008-06-27, 公開日: 2008-07-08, 最終更新日: 2023-12-13)

主引用文献

Bardelle, C.,Cross, D.,Davenport, S.,Kettle, J.G.,Ko, E.J.,Leach, A.G.,Mortlock, A.,Read, J.,Roberts, N.J.,Robins, P.,Williams, E.J.
Inhibitors of the Tyrosine Kinase Ephb4. Part 1: Structure-Based Design and Optimization of a Series of 2,4-Bis-Anilinopyrimidines
Bioorg.Med.Chem.Lett., 18:2776-, 2008

PubMed Abstract: A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.

PubMed: 18434142
DOI: 10.1016/J.BMCL.2008.04.015

実験手法

X-RAY DIFFRACTION (1.9 Å)