Structure of PDB 5fxs Chain A

Receptor sequence
>5fxsA (length=308) Species: 9606 (Homo sapiens) [Search protein sequence]
SYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPET
RVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVI
MELMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNA
NKFVHRDLAARNCMVAEDFTVKIGDFGMTRAIYETDYYRKGGKGLLPVRW
MSPESLKDGVFTTYSDVWSFGVVLWEIATLAEEPYQGLSNEQVLRFVMEG
GLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVS
FYYSEENK
3D structure
PDB5fxs 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
Resolution1.9 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) D157 R161 N162 D175 E184
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 OZN A L1005 V1013 A1031 M1079 M1082 G1085 M1142 M1156 L27 V35 A53 M101 M104 G107 M164 M178 PDBbind-CN: -logKd/Ki=8.05,IC50=0.009uM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:5fxs, PDBe:5fxs, PDBj:5fxs
PDBsum5fxs
PubMed27078757
UniProtP08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)

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