Structure of PDB 3nw7 Chain A

Receptor sequence
>3nw7A (length=297) Species: 9606 (Homo sapiens) [Search protein sequence]
YVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVN
EAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGD
LKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDL
AARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGLLPVRWMSPESLKDGVF
TTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPD
MLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK
3D structure
PDB3nw7 Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.
ChainA
Resolution2.11 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1105 R1109 N1110 D1123 E1132
Catalytic site (residue number reindexed from 1) D149 R153 N154 D167 E176
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 LGV A L975 G976 V983 A1001 K1003 M1049 E1050 M1052 G1055 D1056 N1110 M1112 D1123 M1126 L19 G20 V27 A45 K47 M93 E94 M96 G99 D100 N154 M156 D167 M170 MOAD: ic50=5.3nM
PDBbind-CN: -logKd/Ki=8.28,IC50=5.3nM
BindingDB: IC50=5.3nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0004714 transmembrane receptor protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway
Cellular Component
GO:0016020 membrane

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Molecular Function
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Cellular Component
External links
PDB RCSB:3nw7, PDBe:3nw7, PDBj:3nw7
PDBsum3nw7
PubMed20675137
UniProtP08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)

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