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Target Report Card

Target Name and Classification

Target ID CHEMBL4128
Target Type SINGLE PROTEIN
Preferred Name Tyrosine-protein kinase TIE-2
Synonyms Angiopoietin-1 receptor | CD_antigen=CD202b | Endothelial tyrosine kinase | TEK | TIE2 | Tunica interna endothelial cell kinase | Tyrosine kinase with Ig and EGF homology domains-2 | Tyrosine-protein kinase receptor TEK | Tyrosine-protein kinase receptor TIE-2 | VMCM | VMCM1 | hTIE2 | p140 TEK
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase tie family

Target Components

Component Description Relationship Accession
Angiopoietin-1 receptor SINGLE PROTEIN Q02763

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111375 Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2) SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL24828 VANDETANIB Tyrosine-protein kinase TIE-2 inhibitor 4 DailyMed
CHEMBL1946170 REGORAFENIB Tyrosine-protein kinase TIE-2 inhibitor 4 Expert
CHEMBL254760 MGCD-265 Tyrosine-protein kinase TIE-2 inhibitor 2 Other PubMed
CHEMBL1230609 FORETINIB Tyrosine-protein kinase TIE-2 inhibitor 2 Other PubMed
CHEMBL2010872 CEP-11981 Tyrosine-protein kinase TIE-2 inhibitor 1 PubMed
CHEMBL3545120 CE-245677 Tyrosine-protein kinase TIE-2 inhibitor 1 Other
CHEMBL3545297 PEXMETINIB Tyrosine-protein kinase TIE-2 inhibitor 1 Other Other
CHEMBL3545365 ALTIRATINIB Tyrosine-protein kinase TIE-2 inhibitor 1 Other PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000120156
Ensembl ENSG00000120156
GO Cellular Component GO:0001725 (stress fiber)
GO:0005576 (extracellular region)
GO:0005737 (cytoplasm)
GO:0005815 (microtubule organizing center)
GO:0005856 (cytoskeleton)
GO:0005884 (actin filament)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005902 (microvillus)
GO:0005911 (cell-cell junction)
GO:0005925 (focal adhesion)
GO:0009925 (basal plasma membrane)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016323 (basolateral plasma membrane)
GO:0016324 (apical plasma membrane)
GO:0030054 (cell junction)
GO:0045121 (membrane raft)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019838 (growth factor binding)
GO:0038023 (signaling receptor activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0001525 (angiogenesis)
GO:0001666 (response to hypoxia)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0001935 (endothelial cell proliferation)
GO:0001938 (positive regulation of endothelial cell proliferation)
GO:0001958 (endochondral ossification)
GO:0002040 (sprouting angiogenesis)
GO:0006468 (protein phosphorylation)
GO:0007165 (signal transduction)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007267 (cell-cell signaling)
GO:0007507 (heart development)
GO:0010033 (response to organic substance)
GO:0010595 (positive regulation of endothelial cell migration)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0016525 (negative regulation of angiogenesis)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0032878 (regulation of establishment or maintenance of cell polarity)
GO:0034446 (substrate adhesion-dependent cell spreading)
GO:0035556 (intracellular signal transduction)
GO:0043066 (negative regulation of apoptotic process)
GO:0043114 (regulation of vascular permeability)
GO:0043434 (response to peptide hormone)
GO:0043552 (positive regulation of phosphatidylinositol 3-kinase activity)
GO:0043627 (response to estrogen)
GO:0045766 (positive regulation of angiogenesis)
GO:0046777 (protein autophosphorylation)
GO:0048014 (Tie signaling pathway)
GO:0050728 (negative regulation of inflammatory response)
GO:0050900 (leukocyte migration)
GO:0051259 (protein oligomerization)
GO:0051591 (response to cAMP)
GO:0051894 (positive regulation of focal adhesion assembly)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0060216 (definitive hemopoiesis)
GO:0060347 (heart trabecula formation)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0072012 (glomerulus vasculature development)
GO:1902533 (positive regulation of intracellular signal transduction)
GO:2000251 (positive regulation of actin cytoskeleton reorganization)
GO:2000351 (regulation of endothelial cell apoptotic process)
GO:2000352 (negative regulation of endothelial cell apoptotic process)
Wikipedia TEK_tyrosine_kinase

Target Cross References - Protein

canSAR Q02763
CGD Venous malformations, multiple cutaneous and mucosal
Human Protein Atlas ENSG00000120156
IntAct Q02763
Guide to Pharmacology 1842
Open Targets ENSG00000120156
PharmGKB PA36441
Pharos Q02763 (Tclin)
Reactome R-HSA-210993 (Tie2 Signaling.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
UniProt A8K6W0 B4DH20 B4DHD3 D3DRK5 E7EWI2 Q02763 Q5TCU2 Q8IV34

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR000742 (EGF-like_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR003961 (FN3_dom.)
IPR007110 (Ig-like_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR013032 (EGF-like_CS.)
IPR013783 (Ig-like_fold.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR018941 (Tyr_kin_Tie2_Ig-like_dom-1_N.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR036116 (FN3_sf.)
IPR036179 (Ig-like_dom_sf.)
Pfam PF00041 (fn3)
PF07714 (Pkinase_Tyr)
PF10430 (Ig_Tie2_1)

Target Cross References - Structure

PDBe 1FVR 2GY5 2GY7 2OO8 2OSC 2P4I 2WQB 3BEA 3L8P 4K0V 4X3J 5MYA 5MYB 5UTK
CREDO 1FVR 2GY5 2GY7 2OO8 2OSC 2P4I 2WQB 3BEA 3L8P 4K0V 4X3J 5MYA 5MYB 5UTK
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