Structure of PDB 3tcp Chain A

Receptor sequence
>3tcpA (length=256) Species: 9606 (Homo sapiens) [Search protein sequence]
LEDVVIDRNLLILGKILGSVMEGNLKQEDGTSLKVAVKTMKLDNSSQREI
EEFLSEAACMKDFSHPNVIRLLGVCIEPKPMVILPFMKYGDLHTYLLYSR
LETGPKHIPLQTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMTV
CVADFPVKWIAIESLADRVYTSKSDVWAFGVTMWEIATRGMTPYPGVQNH
EMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTDPLDRPTFSVLRLQLEKL
LESLPD
3D structure
PDB3tcp Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
ChainA
Resolution2.69 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) D136 A138 R140 N141 D154
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 CKJ A V601 A617 F673 M674 K675 R727 M730 V20 A36 F86 M87 K88 R140 M143 PDBbind-CN: -logKd/Ki=8.37,Ki=4.3nM
BindingDB: IC50=2.9nM,Ki=4.3nM
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:3tcp, PDBe:3tcp, PDBj:3tcp
PDBsum3tcp
PubMed22662287
UniProtQ12866|MERTK_HUMAN Tyrosine-protein kinase Mer (Gene Name=MERTK)

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