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044 N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}-1-[(2r)-2-hydroxypropyl]-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide
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Code : 3U6I   PDBj   RCSB PDB   PDBe
Header : transferase/transferase inhibitor
Title : Crystal structure of C-Met in complex with pyrazolone inhibitor 58a
Release Data : 2012-02-22
Compound :
mol_id molecule chains synonym
1 Hepatocyte growth factor receptor A HGF receptor, HGF/SF receptor, Proto-oncogene c-Met, Scatter factor receptor, SF receptor, Tyrosine-protein kinase Met
ec: 2.7.10.1
fragment: unp residues 1048-1315
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Trichoplusia ni  (taxid:7111)
gene: MET
expression_system_vector_type: baculovirus
expression_system_plasmid: pFastBac1
Authors : Bellon, S.F., Whittington, D.A., Long, A.L.
Keywords : kinase domain, phosphotransferase, cancer, hepatocyte growth factor, transferase-transferase inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.10 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

Chain : A
UniProt : P08581 (MET_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.1 PROSITE-ProRule:PRU10028
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