Structure of PDB 5e1s Chain A

Receptor sequence
>5e1sA (length=284) Species: 9606 (Homo sapiens) [Search protein sequence]
VYVPDEWEVSREKITLLRELGQGSFGMVYEGNARDIIKGEAETRVAVKTV
NESASLRERIEFLNEASVMKGFTCHHVVRLLGVVSKGQPTLVVMELMAHG
DLKSYLRSLRPEAENNPGRPPPTLQEMIQMAAEIADGMAYLNAKKFVHRN
LAARNCMVAHDFTVKIGDFGMLPVRWMAPESLKDGVFTTSSDMWSFGVVL
WEITSLAEQPYQGLSNEQVLKFVMDGGYLDQPDNCPERVTDLMRMCWQFN
PKMRPTFLEIVNLLKDDLHPSFPEVSFFHSEENK
3D structure
PDB5e1s BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.
ChainA
Resolution2.264 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) N1132 R1136 N1137 D1150
Catalytic site (residue number reindexed from 1) N150 R154 N155 D168
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 5JA A L1002 G1003 V1010 A1028 M1079 H1081 G1082 M1139 L20 G21 V28 A46 M97 H99 G100 M157 MOAD: Kd=12nM
PDBbind-CN: -logKd/Ki=7.92,Kd=12nM
Gene Ontology
Molecular Function
GO:0004672 protein 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:5e1s, PDBe:5e1s, PDBj:5e1s
PDBsum5e1s
PubMed26438154
UniProtP06213|INSR_HUMAN Insulin receptor (Gene Name=INSR)

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