Brand  (β version)

PDB ID: 3U6J

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Ligands
Code Name Style Show Link
03X N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide PoSSuM
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Structure summary

Code : 3U6J   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Crystal structure of the VEGFR2 kinase domain in complex with a pyrazolone inhibitor
Release Data : 2012-02-22
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, Protein-tyrosine kinase receptor flk-1
ec: 2.7.10.1
fragment: unp residues 815-1171
mutation: V916T, E990V
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Trichoplusia ni  (taxid:7111)
gene: FLK1, KDR
expression_system_vector_type: baculovirus
Authors : Whittington, D.A., Long, A., Rose, P., Gu, Y., Zhao, H.
Keywords : KDR, Flk-1, angiogenesis, phosphotransferase, cancer, vascular endothelial growth factor, TRANSFERASE/TRANSFERASE INHIBITOR, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.1500 Å )
Citation :

Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.

Norman, M.H.,Liu, L.,Lee, M.  et al.
(2012)  J.Med.Chem.  55 : 1858 - 1867

PubMed: 22320343
DOI: 10.1021/jm201330u

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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