Structure of PDB 3i81 Chain A

Receptor sequence
>3i81A (length=296) Species: 9606 (Homo sapiens) [Search protein sequence]
DVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKT
VNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTR
GDLKSYLRSLRPEENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRD
LAARNCMVAEDFTVKIGDFGMTRDIYETDYYRLLPVRWMSPESLKDGVFT
TYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDM
LFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK
3D structure
PDB3i81 Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
ChainA
Resolution2.08 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) D150 R154 N155 D168 E177
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 EBI A L975 V983 A1001 M1049 E1050 M1052 T1053 G1055 N1110 M1112 G1122 D1123 M1126 L21 V29 A47 M95 E96 M98 T99 G101 N155 M157 G167 D168 M171 MOAD: ic50=13nM
PDBbind-CN: -logKd/Ki=7.89,IC50=13nM
BindingDB: IC50=2nM
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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Biological Process
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Cellular Component
External links
PDB RCSB:3i81, PDBe:3i81, PDBj:3i81
PDBsum3i81
PubMed19778024
UniProtP08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)

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