Structure of PDB 5iu2 Chain A

Receptor sequence
>5iu2A (length=312) Species: 9606 (Homo sapiens) [Search protein sequence]
LSSVRYGTVEDLLAFANHISNFYGQRPQESGILLNMVITPQNGRYQIDSD
VLLIPWKLTYRNGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPS
DVEIQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMRE
FEIIWVTKHVLKGLDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQM
TEDVYFPKDLRGTEIYMSPEVILCRGHSTKADIYSLGATLIHMQTGTPPW
VKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPGMRELIEASLERNPNHRP
RAADLLKHEALN
3D structure
PDB5iu2 Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors.
ChainA
Resolution2.7 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D253 K255 N258 D270 T290
Catalytic site (residue number reindexed from 1) D176 K178 N181 D193 T213
Enzyme Commision number 2.7.11.25: mitogen-activated protein kinase kinase 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 6DA A W132 L134 F149 V152 A165 K167 M207 A209 G210 G213 E217 S257 V260 V269 D270 W56 L58 F72 V75 A88 K90 M130 A132 G133 G136 E140 S180 V183 V192 D193 PDBbind-CN: -logKd/Ki=7.80,IC50=0.016uM
BindingDB: IC50=16nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

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Molecular Function
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Biological Process
External links
PDB RCSB:5iu2, PDBe:5iu2, PDBj:5iu2
PDBsum5iu2
PubMed27502541
UniProtP41279|M3K8_HUMAN Mitogen-activated protein kinase kinase kinase 8 (Gene Name=MAP3K8)

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