3NRM

Imidazo[1,2-a]pyrazine-based Aurora Kinase Inhibitors

3NRM の概要

• エントリーDOI: 10.2210/pdb3nrm/pdb
• 分子名称: Serine/threonine-protein kinase 6, N-(3-methylisothiazol-5-yl)-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine (2 entities in total)
• 機能のキーワード: kinase, cell cycle, inhibitor, transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm, cytoskeleton, centrosome: O14965
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 32855.65

構造登録者

Hruza, A. (登録日: 2010-06-30, 公開日: 2010-08-18, 最終更新日: 2023-09-06)

主引用文献

Belanger, D.B.,Curran, P.J.,Hruza, A.,Voigt, J.,Meng, Z.,Mandal, A.K.,Siddiqui, M.A.,Basso, A.D.,Gray, K.
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Bioorg.Med.Chem.Lett., 20:5170-5174, 2010

PubMed Abstract: The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile.

PubMed: 20674350
DOI: 10.1016/j.bmcl.2010.07.008

実験手法

X-RAY DIFFRACTION (3.05 Å)