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Target Report Card

Target Name and Classification

Target ID CHEMBL2041
Target Type SINGLE PROTEIN
Preferred Name Tyrosine-protein kinase receptor RET
Synonyms CDHF12 | CDHR16 | Cadherin family member 12 | Extracellular cell-membrane anchored RET cadherin 120 kDa fragment | PTC | Proto-oncogene c-Ret | Proto-oncogene tyrosine-protein kinase receptor Ret | RET | RET51 | Soluble RET kinase fragment
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase ret family

Target Components

Component Description Relationship Accession
Proto-oncogene tyrosine-protein kinase receptor Ret SINGLE PROTEIN P07949

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3430888 Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET CHIMERIC PROTEIN

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL24828 VANDETANIB Tyrosine-protein kinase receptor RET inhibitor 4 DailyMed
CHEMBL1567 SUNITINIB MALATE Tyrosine-protein kinase receptor RET inhibitor 4 DailyMed
CHEMBL1200485 SORAFENIB TOSYLATE Tyrosine-protein kinase receptor RET inhibitor 4 FDA
CHEMBL1946170 REGORAFENIB Tyrosine-protein kinase receptor RET inhibitor 4 Expert
CHEMBL3707320 ALECTINIB HYDROCHLORIDE Tyrosine-protein kinase receptor RET inhibitor 4 FDA
CHEMBL572881 MOTESANIB Tyrosine-protein kinase receptor RET inhibitor 3 PubMed
CHEMBL576982 QUIZARTINIB Tyrosine-protein kinase receptor RET inhibitor 3 PubMed PubMed
CHEMBL603469 LESTAURTINIB Tyrosine-protein kinase receptor RET inhibitor 3 PubMed
CHEMBL574738 AST-487 Tyrosine-protein kinase receptor RET inhibitor 1 PubMed
CHEMBL2029988 CEP-32496 Tyrosine-protein kinase receptor RET inhibitor 1 Other
CHEMBL3545332 CEP-2563 Tyrosine-protein kinase receptor RET inhibitor 1 PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000165731
Ensembl ENSG00000165731
GO Cellular Component GO:0005737 (cytoplasm)
GO:0005768 (endosome)
GO:0005769 (early endosome)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0010008 (endosome membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030424 (axon)
GO:0030425 (dendrite)
GO:0043025 (neuronal cell body)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0043235 (receptor complex)
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:0005509 (calcium ion binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0001657 (ureteric bud development)
GO:0001755 (neural crest cell migration)
GO:0001838 (embryonic epithelial tube formation)
GO:0006468 (protein phosphorylation)
GO:0006919 (activation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0007155 (cell adhesion)
GO:0007156 (homophilic cell adhesion via plasma membrane adhesion molecules)
GO:0007158 (neuron cell-cell adhesion)
GO:0007165 (signal transduction)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007399 (nervous system development)
GO:0007497 (posterior midgut development)
GO:0010628 (positive regulation of gene expression)
GO:0010976 (positive regulation of neuron projection development)
GO:0014042 (positive regulation of neuron maturation)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0030155 (regulation of cell adhesion)
GO:0030182 (neuron differentiation)
GO:0030335 (positive regulation of cell migration)
GO:0033619 (membrane protein proteolysis)
GO:0033630 (positive regulation of cell adhesion mediated by integrin)
GO:0035799 (ureter maturation)
GO:0042493 (response to drug)
GO:0042551 (neuron maturation)
GO:0043547 (positive regulation of GTPase activity)
GO:0045793 (positive regulation of cell size)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0048265 (response to pain)
GO:0048484 (enteric nervous system development)
GO:0050770 (regulation of axonogenesis)
GO:0060041 (retina development in camera-type eye)
GO:0060384 (innervation)
GO:0061146 (Peyer's patch morphogenesis)
GO:0071300 (cellular response to retinoic acid)
GO:0072300 (positive regulation of metanephric glomerulus development)
GO:0097021 (lymphocyte migration into lymphoid organs)
GO:1903263 (positive regulation of serine phosphorylation of STAT3 protein)
GO:2001241 (positive regulation of extrinsic apoptotic signaling pathway in absence of ligand)
Wikipedia RET_proto-oncogene

Target Cross References - Protein

canSAR P07949
CGD Multiple endocrine neoplasia, type IIA; Multiple endocrine neoplasia IIB; Medullary thyroid carcinoma, familial; Pheochromocytoma; Hirschsprung disease, susceptibility to
Human Protein Atlas ENSG00000165731
IntAct P07949
Guide to Pharmacology 2185
Open Targets ENSG00000165731
PharmGKB PA34335
Pharos P07949 (Tclin)
Reactome R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-8853659 (RET signaling.)
UniProt A8K6Z2 P07949 Q15250 Q9BTB0 Q9H4A2

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR002126 (Cadherin.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR015919 (Cadherin-like.)
IPR016249 (Tyr_kinase_Ret_rcpt.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
Pfam PF00028 (Cadherin)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 2IVS 2IVT 2IVU 2IVV 2X2K 2X2L 2X2M 2X2U 4CKI 4CKJ 5AMN 5FM2 5FM3
CREDO 2IVS 2IVT 2IVU 2IVV 2X2K 2X2L 2X2M 2X2U 4CKI 4CKJ 5AMN 5FM2 5FM3
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