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Target Report Card

Target Name and Classification

Target ID CHEMBL1824
Target Type SINGLE PROTEIN
Preferred Name Receptor protein-tyrosine kinase erbB-2
Synonyms CD_antigen=CD340 | ERBB2 | HER2 | MLN 19 | MLN19 | Metastatic lymph node gene 19 protein | NEU | NGL | Proto-oncogene Neu | Proto-oncogene c-ErbB-2 | Receptor tyrosine-protein kinase erbB-2 | Tyrosine kinase-type cell surface receptor HER2 | p185erbB2
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase egfr family

Target Components

Component Description Relationship Accession
Receptor tyrosine-protein kinase erbB-2 SINGLE PROTEIN P04626

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2363049 Epidermal growth factor receptor PROTEIN FAMILY
CHEMBL2111431 Epidermal growth factor receptor and ErbB2 (HER1 and HER2) PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1201179 LAPATINIB DITOSYLATE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 DailyMed
CHEMBL1201585 TRASTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 DailyMed
CHEMBL1743082 TRASTUZUMAB EMTANSINE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 DailyMed DailyMed PubMed PubMed
CHEMBL2007641 PERTUZUMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 4 DailyMed
CHEMBL2105712 AFATINIB DIMALEATE Receptor protein-tyrosine kinase erbB-2 inhibitor 4 DailyMed
CHEMBL180022 NERATINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 3 PubMed PubMed
CHEMBL545315 CANERTINIB DIHYDROCHLORIDE Receptor protein-tyrosine kinase erbB-2 inhibitor 3 PubMed PubMed
CHEMBL2105719 DACOMITINIB HYDRATE Receptor protein-tyrosine kinase erbB-2 inhibitor 3 Other PubMed
CHEMBL2364649 MARGETUXIMAB Receptor protein-tyrosine kinase erbB-2 inhibitor 3 Other
CHEMBL483321 CP-724714 Receptor protein-tyrosine kinase erbB-2 inhibitor 2 PubMed PubMed
CHEMBL587723 AEE-788 Receptor protein-tyrosine kinase erbB-2 inhibitor 2 PubMed
CHEMBL2103842 VARLITINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 2 Other Other
CHEMBL2108029 ERTUMAXOMAB Receptor protein-tyrosine kinase erbB-2 other 2 PubMed
CHEMBL2109271 MDX-210 Receptor protein-tyrosine kinase erbB-2 other 2 PubMed
CHEMBL2408045 SAPITINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 2 PubMed PubMed
CHEMBL3544956 Pyrotinib Receptor protein-tyrosine kinase erbB-2 inhibitor 2 Other
CHEMBL3544983 TESEVATINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 2 Other PubMed PubMed
CHEMBL3545025 INSM-18 Receptor protein-tyrosine kinase erbB-2 inhibitor 2 PubMed PubMed
CHEMBL3545396 BMS-690514 Receptor protein-tyrosine kinase erbB-2 inhibitor 2 PubMed PubMed
CHEMBL598797 CUDC-101 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 PubMed
CHEMBL1614707 MUBRITINIB Receptor protein-tyrosine kinase erbB-2 inhibitor 1 PubMed PubMed PubMed
CHEMBL1614725 TAK-285 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 DOI PubMed
CHEMBL1645462 AC-480 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 PubMed PubMed
CHEMBL3545002 MP-412 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 PubMed PubMed
CHEMBL3545111 Hemay-022 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 ClinicalTrials
CHEMBL3545133 JNJ-26483327 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 DOI PubMed
CHEMBL3545200 S-222611 Receptor protein-tyrosine kinase erbB-2 inhibitor 1 PubMed PubMed
CHEMBL3545244 Allitinib Receptor protein-tyrosine kinase erbB-2 inhibitor 1 PubMed
CHEMBL3545380 Irbinitinib Receptor protein-tyrosine kinase erbB-2 inhibitor 1 Other Other
CHEMBL3833344 MM-302 Receptor protein-tyrosine kinase erbB-2 binding agent 0 PubMed PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000141736
Ensembl ENSG00000141736
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0010008 (endosome membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016323 (basolateral plasma membrane)
GO:0016324 (apical plasma membrane)
GO:0031410 (cytoplasmic vesicle)
GO:0043209 (myelin sheath)
GO:0043235 (receptor complex)
GO:0048471 (perinuclear region of cytoplasm)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0001042 (RNA polymerase I core binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0004716 (receptor signaling protein tyrosine kinase activity)
GO:0004888 (transmembrane signaling receptor activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008022 (protein C-terminus binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019838 (growth factor binding)
GO:0019903 (protein phosphatase binding)
GO:0042802 (identical protein binding)
GO:0043125 (ErbB-3 class receptor binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO:0046982 (protein heterodimerization activity)
GO:0046983 (protein dimerization activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0007165 (signal transduction)
GO:0007166 (cell surface receptor signaling pathway)
GO:0007167 (enzyme linked receptor protein signaling pathway)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007399 (nervous system development)
GO:0007422 (peripheral nervous system development)
GO:0007507 (heart development)
GO:0007528 (neuromuscular junction development)
GO:0008045 (motor neuron axon guidance)
GO:0008283 (cell proliferation)
GO:0014065 (phosphatidylinositol 3-kinase signaling)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0030307 (positive regulation of cell growth)
GO:0032886 (regulation of microtubule-based process)
GO:0033088 (negative regulation of immature T cell proliferation in thymus)
GO:0038128 (ERBB2 signaling pathway)
GO:0042060 (wound healing)
GO:0042552 (myelination)
GO:0043406 (positive regulation of MAP kinase activity)
GO:0043547 (positive regulation of GTPase activity)
GO:0045727 (positive regulation of translation)
GO:0045765 (regulation of angiogenesis)
GO:0045785 (positive regulation of cell adhesion)
GO:0045943 (positive regulation of transcription from RNA polymerase I promoter)
GO:0045945 (positive regulation of transcription from RNA polymerase III promoter)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048709 (oligodendrocyte differentiation)
GO:0050679 (positive regulation of epithelial cell proliferation)
GO:0070372 (regulation of ERK1 and ERK2 cascade)
GO:0071363 (cellular response to growth factor stimulus)
GO:0090314 (positive regulation of protein targeting to membrane)
GO:2000145 (regulation of cell motility)
Wikipedia HER2/neu

Target Cross References - Protein

canSAR P04626
Human Protein Atlas ENSG00000141736
IntAct P04626
Guide to Pharmacology 2019
MICAD NBK23144 (Human epidermal growth factor receptor 2 (HER2))
Open Targets ENSG00000141736
PharmGKB PA27844
Pharos P04626 (Tclin)
Reactome R-HSA-1227986 (Signaling by ERBB2.)
R-HSA-1250196 (SHC1 events in ERBB2 signaling.)
R-HSA-1251932 (PLCG1 events in ERBB2 signaling.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-1306955 (GRB7 events in ERBB2 signaling.)
R-HSA-1358803 (Downregulation of ERBB2:ERBB3 signaling.)
R-HSA-1963640 (GRB2 events in ERBB2 signaling.)
R-HSA-1963642 (PI3K events in ERBB2 signaling.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-416572 (Sema4D induced cell migration and growth-cone collapse.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6785631 (ERBB2 Regulates Cell Motility.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8847993 (ERBB2 Activates PTK6 Signaling.)
R-HSA-8863795 (Downregulation of ERBB2 signaling.)
R-HSA-8866910 (TFAP2 (AP-2) family regulates transcription of growth factors and their receptors.)
UniProt B2RZG3 B4DHN3 P04626 Q14256 Q6LDV1 Q9UMK4 X5D2V5

Target Cross References - Domain

InterPro IPR000494 (Rcpt_L-dom.)
IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR006211 (Furin-like_Cys-rich_dom.)
IPR006212 (Furin_repeat.)
IPR008266 (Tyr_kinase_AS.)
IPR009030 (Growth_fac_rcpt_.)
IPR011009 (Kinase-like_dom.)
IPR016245 (Tyr_kinase_EGF/ERB/XmrK_rcpt.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR032675 (L_dom-like.)
IPR032778 (GF_recep_IV.)
Pfam PF00757 (Furin-like)
PF01030 (Recep_L_domain)
PF07714 (Pkinase_Tyr)
PF14843 (GF_recep_IV)

Target Cross References - Structure

PDBe 1MFG 1MFL 1N8Z 1QR1 1S78 2A91 3BE1 3H3B 3MZW 3N85 3PP0 3RCD 3WLW 3WSQ 4GFU 4HRL 4HRM 4HRN
CREDO 1MFG 1MFL 1N8Z 1QR1 1S78 2A91 3BE1 3H3B 3MZW 3N85 3PP0 3RCD 3WLW 3WSQ 4GFU 4HRL 4HRM 4HRN
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