Structure of PDB 5tc0 Chain A

Receptor sequence
>5tc0A (length=238) Species: 9606 (Homo sapiens) [Search protein sequence]
EDVVIDRNLLILGKILGEGEFGSVMEGNLKQEDGTSLKVAVKTMKDFSHP
NVMRLLGVCIEMSSQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPL
QTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMTVCVADFMPVKW
IAIETSKSDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPE
DCLDELYEIMYSCWRTDPLDRPTFSVLRLQLEKLLESL
3D structure
PDB5tc0 Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.
ChainA
Resolution2.24 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 M762
Catalytic site (residue number reindexed from 1) D126 A128 R130 N131 D144 M146
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 79Y A A617 K619 L671 P672 F673 M674 G677 N728 M730 A740 D741 A40 K42 L74 P75 F76 M77 G80 N131 M133 A143 D144 MOAD: ic50=25nM
PDBbind-CN: -logKd/Ki=7.60,IC50=25nM
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:5tc0, PDBe:5tc0, PDBj:5tc0
PDBsum5tc0
PubMed28082036
UniProtQ12866|MERTK_HUMAN Tyrosine-protein kinase Mer (Gene Name=MERTK)

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