Structure of PDB 5k0x Chain A

Receptor sequence
>5k0xA (length=258) Species: 9606 (Homo sapiens) [Search protein sequence]
KLEDVVIDRNLLILGKILGEGSVMEGNLKQEDGTSLKVAVKTMKLDNSSQ
IEEFLSEAACMKDFSHPNVIRLLGVCIEPKPMVILPFMKYGDLHTYLLYS
RLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMT
VCVADFGPVKWIAIESLADRVYTSKSDVWAFGVTMWEIATRGMTPYPGVQ
NHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTDPLDRPTFSVLRLQLE
KLLESLPD
3D structure
PDB5k0x Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors.
ChainA
Resolution2.231 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D723 A725 R727 N728 D741
Catalytic site (residue number reindexed from 1) D137 A139 R141 N142 D155
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 K0X A L593 A617 L671 F673 M674 K675 N728 M730 D741 L18 A39 L85 F87 M88 K89 N142 M144 D155 MOAD: ic50=4.4nM
PDBbind-CN: -logKd/Ki=8.36,IC50=4.4nM
BindingDB: IC50=<10nM
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:5k0x, PDBe:5k0x, PDBj:5k0x
PDBsum5k0x
PubMed28032464
UniProtQ12866|MERTK_HUMAN Tyrosine-protein kinase Mer (Gene Name=MERTK)

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