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Ligands
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FZP (4-fluorophenyl)methyl {2-[(1-methyl-1h-pyrazol-3-yl)amino]pyrimidin-4-yl}[3-(propanoylamino)phenyl]carbamate
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Code : 6D8E   PDBj   RCSB PDB   PDBe
Header : Transferase/Transferase Inhibitor
Title : Discovery of a Highly Potent and Broadly Effective EGFR and HER2 Exon 20 Insertion Mutant Inhibitor
Release Data : 2018-07-18
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
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: EGFR, ERBB, ERBB1, HER1
Authors : Park, E., Eck, M.J.
Keywords : EGFR, Inhibitor, SIGNALING PROTEIN, Transferase-Transferase Inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.537 Å )
Citation :

Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.

Jang, J.,Son, J.,Park, E.  et al.
(2018)  Angew. Chem. Int. Ed. Engl.  57 : 11629 - 11633

PubMed: 29978938
DOI: 10.1002/anie.201805187

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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