Structure of PDB 5fxq Chain A

Receptor sequence
>5fxqA (length=302) Species: 9606 (Homo sapiens) [Search protein sequence]
SYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPET
RVAIKTVEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIM
ELMTRGDLKSYLRSLRPEMNPVLAPPSLSKMIQMAGEIADGMAYLNANKF
VHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGLLPVRWMSPESL
KDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKP
DNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEE
NK
3D structure
PDB5fxq Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
ChainA
Resolution2.3 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1135 R1139 N1140 D1153 E1162
Catalytic site (residue number reindexed from 1) D154 R158 N159 D172 E181
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 GD5 A V1013 A1031 M1079 M1082 T1083 G1085 M1142 D1153 V35 A53 M100 M103 T104 G106 M161 D172 PDBbind-CN: -logKd/Ki=7.85,IC50=0.014uM
BindingDB: IC50=55nM
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:5fxq, PDBe:5fxq, PDBj:5fxq
PDBsum5fxq
PubMed27078757
UniProtP08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)

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