Brand  (β version)

PDB ID: 5GMP

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Ligands
Code Name Style Show Link
F62 N-[3-[2-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-5-methyl-7-oxidanylidene-pyrido[2,3-D]pyrimidin-8-yl]phenyl]prop-2-enamide PoSSuM
Non-standard Residues
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Structure summary

Code : 5GMP   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Crystal structure of EGFR 696-1022 T790M in complex with XTF-262
Release Data : 2017-06-28
Compound :
mol_id molecule chains synonym
1 Epidermal growth factor receptor A Proto-oncogene c-ErbB-1,Receptor tyrosine-protein kinase erbB-1
ec: 2.7.10.1
fragment: UNP RESIDUES 696-1022
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: EGFR, ERBB, ERBB1, HER1
expression_system_common: Fall armyworm
expression_system_cell_line: SF9
expression_system_vector_type: BACULOVIRUS
expression_system_vector: pFastBac-HTB
Authors : Yan, X.E., Yun, C.H.
Keywords : EGFR, T790M, XTF-262, inhibitor, TRANSFERASE
Exp. method : X-RAY DIFFRACTION ( 2.797 Å )
Citation :

A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR(L858R/T790M) mutant with improved pharmacokinetic properties.

Yu, L.,Huang, M.,Xu, T.  et al.
(2017)  Eur J Med Chem  126 : 1107 - 1117

PubMed: 28033579
DOI: 10.1016/j.ejmech.2016.12.006

Reaction

Chain : A
UniProt : P00533 (EGFR_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:15374980, PubMed:17349580, PubMed:18046415, PubMed:18227510, PubMed:19560417, PubMed:19563760
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