Structure of PDB 3io7 Chain A

Receptor sequence
>3io7A (length=284) Species: 9606 (Homo sapiens) [Search protein sequence]
TQFEERHLKFLQQLGKGGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLR
DFEREIEILKSLQHDNIVKYKGVCYSRNLKLIMEYLPYGSLRDYLQKHKE
RIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFG
LTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYE
LFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPD
EIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNM
3D structure
PDB3io7 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
ChainA
Resolution2.6 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) M865 D976 A978 R980 N981 D994 S1016
Catalytic site (residue number reindexed from 1) M22 D130 A132 R134 N135 D148 S170
Enzyme Commision number 2.7.10.2: non-specific 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 1P5 A L855 K857 G858 V863 M929 L932 R980 N981 L983 D994 L14 K16 G17 V20 M83 L86 R134 N135 L137 D148 PDBbind-CN: -logKd/Ki=7.77,Ki=0.017uM
BindingDB: Ki=7nM,IC50=>20000nM
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

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Molecular Function
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Biological Process
External links
PDB RCSB:3io7, PDBe:3io7, PDBj:3io7
PDBsum3io7
PubMed19857967
UniProtO60674|JAK2_HUMAN Tyrosine-protein kinase JAK2 (Gene Name=JAK2)

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