Brand  (β version)

PDB ID: 3VO3

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Ligands
Code Name Style Show Link
0KF N-[3-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-B]pyridazin-6-yl}oxy)phenyl]-1,3-dimethyl-1h-pyrazole-5-carboxamide PoSSuM
EDO 1,2-ethanediol PoSSuM
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Structure summary

Code : 3VO3   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Crystal Structure of the Kinase domain of Human VEGFR2 with imidazo[1,2-B]pyridazine derivative
Release Data : 2013-03-06
Compound :
mol_id molecule chains synonym
1 Vascular endothelial growth factor receptor 2 A VEGFR-2, Fetal liver kinase 1, FLK-1, Kinase insert domain receptor, KDR, Protein-tyrosine kinase receptor flk-1
ec: 2.7.10.1
fragment: UNP residues 806-1171
mutation: truncated residues 940-989
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: KDR, FLK1, VEGFR2
expression_system_cell_line: Sf9
expression_system_vector_type: Baculovirus
expression_system_plasmid: pFastBac
Authors : Oki, H., Okada, K.
Keywords : vegfr2, kinase domain, Tyrosin-protein kinase, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 1.5200 Å )
Citation :

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

Miyamoto, N.,Sakai, N.,Hirayama, T.  et al.
(2013)  Bioorg.Med.Chem.  21 : 2333 - 2345

PubMed: 23498918
DOI: 10.1016/j.bmc.2013.01.074

Reaction

Chain : A
UniProt : P35968 (VGFR2_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.1 PROSITE-ProRule:PRU10028, PubMed:10037737, PubMed:10102632
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