3EWH

Crystal structure of the VEGFR2 kinase domain in complex with a pyridyl-pyrimidine benzimidazole inhibitor

Summary for 3EWH

• Entry DOI: 10.2210/pdb3ewh/pdb
• Related: 3EFW
• Descriptor: vascular endothelial growth factor receptor 2, N-[4-({3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl}oxy)naphthalen-1-yl]-6-(trifluoromethyl)-1H-benzimidazol-2-amine, 1,2-ETHANEDIOL, ... (4 entities in total)
• Functional Keywords: angiogenesis, receptor tyrosine kinase, dfg-out, transferase
• Biological source: Homo sapiens; More
• Cellular location: Cell junction . Isoform 1: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted . Isoform 3: Secreted: P35968
• Total number of polymer chains: 1
• Total formula weight: 36714.20

Authors

Whittington, D.A.,Long, A.M.,Rose, P.,Gu, Y.,Zhao, H. (deposition date: 2008-10-15, release date: 2009-08-25, Last modification date: 2023-12-27)

• Primary citation: Cee, V.J.,Cheng, A.C.,Romero, K.,Bellon, S.,Mohr, C.,Whittington, D.A.,Bak, A.,Bready, J.,Caenepeel, S.,Coxon, A.,Deak, H.L.,Fretland, J.,Gu, Y.,Hodous, B.L.,Huang, X.,Kim, J.L.,Lin, J.,Long, A.M.,Nguyen, H.,Olivieri, P.R.,Patel, V.F.,Wang, L.,Zhou, Y.,Hughes, P.,Geuns-Meyer, S.; Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.; Bioorg.Med.Chem.Lett., 19:424-427, 2009; PubMed: 19062275; DOI: 10.1016/j.bmcl.2008.11.056

Experimental method

X-RAY DIFFRACTION (1.6 Å)