Structure of PDB 5hzn Chain H

Receptor sequence
>5hznH (length=303) Species: 9606 (Homo sapiens) [Search protein sequence]
AADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAI
KTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELM
TRGDLKSYLRSLRPAMANNPVLAPPSLSKMIQMAGEIADGMAYLNANKFV
HRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPE
SLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLD
KPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYS
EEN
3D structure
PDB5hzn Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.
ChainH
Resolution2.2 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1132 R1136 N1137 D1150 E1159
Catalytic site (residue number reindexed from 1) D153 R157 N158 D171 E180
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 66A H L1002 G1003 Q1004 V1010 A1028 K1030 F1044 E1047 A1048 V1060 M1076 M1079 D1083 M1139 G1149 D1150 L23 G24 Q25 V31 A49 K51 F65 E68 A69 V81 M97 M100 D104 M160 G170 D171 MOAD: ic50=0.061uM
BindingDB: IC50=61nM
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:5hzn, PDBe:5hzn, PDBj:5hzn
PDBsum5hzn
PubMed26951750
UniProtP08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)

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