Structure of PDB 5hzn Chain A

Receptor sequence
>5hznA (length=296) Species: 9606 (Homo sapiens) [Search protein sequence]
AADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAI
KTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELM
TRGDLKSYLRSLRPAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARN
CMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFT
TYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDM
LFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK
3D structure
PDB5hzn Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.
ChainA
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) D145 R149 N150 D163 E172
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 A G1003 Q1004 G1005 F1007 A1028 K1030 E1047 V1060 M1076 M1079 M1139 G1149 D1150 G24 Q25 G26 F28 A49 K51 E68 V81 M97 M100 M152 G162 D163 MOAD: ic50=0.061uM
PDBbind-CN: -logKd/Ki=7.21,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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