3U6J

Crystal structure of the VEGFR2 kinase domain in complex with a pyrazolone inhibitor

Summary for 3U6J

Entry DOI	10.2210/pdb3u6j/pdb
Related	3U6H 3U6I
Descriptor	Vascular endothelial growth factor receptor 2, N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (3 entities in total)
Functional Keywords	kdr, flk-1, angiogenesis, phosphotransferase, cancer, vascular endothelial growth factor, transferase/transferase inhibitor, transferase-transferase inhibitor complex
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	36685.23
Authors	Whittington, D.A.,Long, A.,Rose, P.,Gu, Y.,Zhao, H. (deposition date: 2011-10-12, release date: 2012-02-22, Last modification date: 2024-02-28)
Primary citation	Norman, M.H.,Liu, L.,Lee, M.,Xi, N.,Fellows, I.,D'Angelo, N.D.,Dominguez, C.,Rex, K.,Bellon, S.F.,Kim, T.S.,Dussault, I. Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives. J.Med.Chem., 55:1858-1867, 2012 Cited by PubMed: 22320343 DOI: 10.1021/jm201330u PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.15 Å)

Structure validation