3NRM

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

Summary for 3NRM

Entry DOI	10.2210/pdb3nrm/pdb
Descriptor	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)
Functional Keywords	kinase, cell cycle, inhibitor, transferase
Biological source	Homo sapiens (human)
Cellular location	Cytoplasm, cytoskeleton, centrosome: O14965
Total number of polymer chains	1
Total formula weight	32855.65
Authors	Hruza, A. (deposition date: 2010-06-30, release date: 2010-08-18, Last modification date: 2023-09-06)
Primary citation	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 Cited by 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 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (3.05 Å)

Structure validation