3VO3

Crystal Structure of the Kinase domain of Human VEGFR2 with imidazo[1,2-b]pyridazine derivative

Summary for 3VO3

• Entry DOI: 10.2210/pdb3vo3/pdb
• Related: 3VHE
• Descriptor: Vascular endothelial growth factor receptor 2, N-[3-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide, 1,2-ETHANEDIOL, ... (4 entities in total)
• Functional Keywords: vegfr2, kinase domain, tyrosin-protein kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Isoform 1: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted (Probable). Isoform 3: Secreted: P35968
• Total number of polymer chains: 1
• Total formula weight: 36846.39

Authors

Oki, H.,Okada, K. (deposition date: 2012-01-19, release date: 2013-03-06, Last modification date: 2024-03-20)

• Primary citation: Miyamoto, N.,Sakai, N.,Hirayama, T.,Miwa, K.,Oguro, Y.,Oki, H.,Okada, K.,Takagi, T.,Iwata, H.,Awazu, Y.,Yamasaki, S.,Takeuchi, T.,Miki, H.,Hori, A.,Imamura, S.; Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor; Bioorg.Med.Chem., 21:2333-2345, 2013; PubMed: 23498918; DOI: 10.1016/j.bmc.2013.01.074

Experimental method

X-RAY DIFFRACTION (1.52 Å)