Structure of PDB 5em5 Chain A

Receptor sequence
>5em5A (length=298) Species: 9606 (Homo sapiens) [Search protein sequence]
EAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKE
TSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLD
YVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQH
VKITDFGRAVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYD
GIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELII
EFSKMARDPQRYLVIQGDERMHLPSPTDSNFYEEDMDDVVDADEYLIP
3D structure
PDB5em5 Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
ChainA
Resolution2.65 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D837 A839 R841 N842 D855
Catalytic site (residue number reindexed from 1) D137 A139 R141 N142 D155
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine kinase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 5Q2 A L718 V726 A743 K745 L788 M790 Q791 M793 G796 L844 L22 V30 A47 K49 L88 M90 Q91 M93 G96 L144 PDBbind-CN: -logKd/Ki=6.58,Ki=0.262uM
BindingDB: Ki=37nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

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Molecular Function

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Biological Process
External links
PDB RCSB:5em5, PDBe:5em5, PDBj:5em5
PDBsum5em5
PubMed26819674
UniProtP00533|EGFR_HUMAN Epidermal growth factor receptor (Gene Name=EGFR)

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