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Target Report Card

Target Name and Classification

Target ID CHEMBL3009
Target Type SINGLE PROTEIN
Preferred Name Receptor protein-tyrosine kinase erbB-4
Synonyms 4ICD | E4ICD | ERBB4 intracellular domain | ERBB4 | HER4 | Proto-oncogene-like protein c-ErbB-4 | Receptor tyrosine-protein kinase erbB-4 | Tyrosine kinase-type cell surface receptor HER4 | p180erbB4 | s80HER4
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-4 SINGLE PROTEIN Q15303

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2363049 Epidermal growth factor receptor PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL2105712 AFATINIB DIMALEATE Receptor protein-tyrosine kinase erbB-4 inhibitor 4 DailyMed
CHEMBL545315 CANERTINIB DIHYDROCHLORIDE Receptor protein-tyrosine kinase erbB-4 inhibitor 3 PubMed PubMed
CHEMBL2105719 DACOMITINIB HYDRATE Receptor protein-tyrosine kinase erbB-4 inhibitor 3 Other PubMed
CHEMBL3545396 BMS-690514 Receptor protein-tyrosine kinase erbB-4 inhibitor 2 PubMed PubMed
CHEMBL1645462 AC-480 Receptor protein-tyrosine kinase erbB-4 inhibitor 1 PubMed PubMed
CHEMBL3545133 JNJ-26483327 Receptor protein-tyrosine kinase erbB-4 inhibitor 1 DOI PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000178568
Ensembl ENSG00000178568
GO Cellular Component GO:0005576 (extracellular region)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005739 (mitochondrion)
GO:0005759 (mitochondrial matrix)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016323 (basolateral plasma membrane)
GO:0043235 (receptor complex)
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:0004716 (receptor signaling protein tyrosine kinase activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005154 (epidermal growth factor receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0042803 (protein homodimerization activity)
GO:0044212 (transcription regulatory region DNA binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0001755 (neural crest cell migration)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0007165 (signal transduction)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007275 (multicellular organism development)
GO:0007399 (nervous system development)
GO:0007507 (heart development)
GO:0007595 (lactation)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0009880 (embryonic pattern specification)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0021551 (central nervous system morphogenesis)
GO:0021889 (olfactory bulb interneuron differentiation)
GO:0030334 (regulation of cell migration)
GO:0038128 (ERBB2 signaling pathway)
GO:0042523 (positive regulation of tyrosine phosphorylation of Stat5 protein)
GO:0043066 (negative regulation of apoptotic process)
GO:0043547 (positive regulation of GTPase activity)
GO:0043552 (positive regulation of phosphatidylinositol 3-kinase activity)
GO:0043653 (mitochondrial fragmentation involved in apoptotic process)
GO:0045165 (cell fate commitment)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0060045 (positive regulation of cardiac muscle cell proliferation)
GO:0060644 (mammary gland epithelial cell differentiation)
GO:0060749 (mammary gland alveolus development)
GO:0061026 (cardiac muscle tissue regeneration)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:2000010 (positive regulation of protein localization to cell surface)
GO:2000145 (regulation of cell motility)
GO:2000366 (positive regulation of STAT protein import into nucleus)
GO:2001223 (negative regulation of neuron migration)
Wikipedia ERBB4

Target Cross References - Protein

canSAR Q15303
Human Protein Atlas ENSG00000178568
IntAct Q15303
Guide to Pharmacology 1799
Open Targets ENSG00000178568
PharmGKB PA27847
Pharos Q15303 (Tclin)
Reactome R-HSA-1227986 (Signaling by ERBB2.)
R-HSA-1236394 (Signaling by ERBB4.)
R-HSA-1250196 (SHC1 events in ERBB2 signaling.)
R-HSA-1250342 (PI3K events in ERBB4 signaling.)
R-HSA-1250347 (SHC1 events in ERBB4 signaling.)
R-HSA-1251985 (Nuclear signaling by ERBB4.)
R-HSA-1253288 (Downregulation of ERBB4 signaling.)
R-HSA-1257604 (PIP3 activates AKT 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-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.)
UniProt B7ZLD7 B7ZLE2 B7ZLE3 Q15303 Q2M1W1 Q59EW4

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 2AHX 2R4B 3BBT 3BBW 3BCE 3U2P 3U7U 3U9U
CREDO 2AHX 2R4B 3BBT 3BBW 3BCE 3U2P 3U7U 3U9U
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