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Target Report Card

Target Name and Classification

Target ID CHEMBL4128
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: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:0004872 (receptor 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 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:0031100 (organ regeneration)
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:0043547 (positive regulation of GTPase activity)
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: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.)
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.)
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