Brand  (β version)

PDB ID: 4AP7

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Ligands
Code Name Style Show Link
F47 4-[[6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-B][1,2,4]triazin-3-yl]methyl]phenol PoSSuM
Non-standard Residues
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Structure summary

Code : 4AP7   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Crystal structure of C-MET kinase domain in complex with 4-((6-(4- fluorophenyl)-(1,2,4)triazolo(4,3-B)(1,2,4)triazin-3-yl)methyl)phenol
Release Data : 2012-09-26
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: TYROSINE KINASE DOMAIN, UNP RESIDUES 1051-1348
Source :
mol_id organism_scientific organism_common expression_system
1 HOMO SAPIENS  (taxid:9606) HUMAN SPODOPTERA FRUGIPERDA  (taxid:7108)
expression_system_common: FALL ARMYWORM
expression_system_cell_line: SF9
expression_system_vector_type: BACULOVIRUS
expression_system_plasmid: PFASTBAC1
Authors : McTigue, M., Wickersham, J.
Keywords : TRANSFERASE
Exp. method : X-RAY DIFFRACTION ( 1.80 Å )
Citation :

Discovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (C-met) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2-(4-(1-(Quinolin-6-Ylmethyl)-1H-[1,2, 3]Triazolo[4,5-B]Pyrazin-6-Yl)-1H-Pyrazol-1-Yl)Ethanol (Pf-04217903) for the Treatment of Cancer.

Cui, J.J.,Mctigue, M.,Nambu, M.  et al.
(2012)  J.Med.Chem.  55 : 8091

PubMed: 22924734
DOI: 10.1021/JM300967G

Reaction

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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