ChEMBL logo

ChEMBL

spacer
ChEMBL Statistics
  Loading Statistics...
spacer

Target Report Card

Target Name and Classification

Target ID CHEMBL240
Target Type SINGLE PROTEIN
Preferred Name HERG
Synonyms ERG | ERG-1 | ERG1 | Eag homolog | Eag-related protein 1 | Ether-a-go-go-related gene potassium channel 1 | Ether-a-go-go-related protein 1 | H-ERG | HERG | KCNH2 | Potassium voltage-gated channel subfamily H member 2 | Voltage-gated potassium channel subunit Kv11.1 | hERG-1 | hERG1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • ion channel > voltage-gated ion channel > potassium channels > voltage-gated potassium channel

Target Components

Component Description Relationship Accession
Potassium voltage-gated channel subfamily H member 2 SINGLE PROTEIN Q12809

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2362996 Voltage-gated potassium channel PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL473 DOFETILIDE HERG blocker 4 DailyMed
CHEMBL1700 SOTALOL HYDROCHLORIDE HERG blocker 4 DailyMed
CHEMBL1083993 AMIODARONE HYDROCHLORIDE HERG blocker 4 DailyMed
CHEMBL1200564 IBUTILIDE FUMARATE HERG blocker 4 DailyMed PubMed
CHEMBL3545040 AZD7009 HERG blocker 2 PubMed
CHEMBL3545169 AZD1305 HERG blocker 2 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000055118
Ensembl ENSG00000055118
GO Cellular Component GO:0005886 (plasma membrane)
GO:0008076 (voltage-gated potassium channel complex)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0048471 (perinuclear region of cytoplasm)
GO Molecular Function GO:0000155 (phosphorelay sensor kinase activity)
GO:0005216 (ion channel activity)
GO:0005242 (inward rectifier potassium channel activity)
GO:0005244 (voltage-gated ion channel activity)
GO:0005249 (voltage-gated potassium channel activity)
GO:0005251 (delayed rectifier potassium channel activity)
GO:0005267 (potassium channel activity)
GO:0005515 (protein binding)
GO:0031625 (ubiquitin protein ligase binding)
GO:0042802 (identical protein binding)
GO:0042803 (protein homodimerization activity)
GO:0055131 (C3HC4-type RING finger domain binding)
GO:0086008 (voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization)
GO:0097110 (scaffold protein binding)
GO:1902282 (voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization)
GO Biological Process GO:0000160 (phosphorelay signal transduction system)
GO:0003064 (regulation of heart rate by hormone)
GO:0006810 (transport)
GO:0006811 (ion transport)
GO:0006813 (potassium ion transport)
GO:0023014 (signal transduction by protein phosphorylation)
GO:0034765 (regulation of ion transmembrane transport)
GO:0035690 (cellular response to drug)
GO:0042391 (regulation of membrane potential)
GO:0055075 (potassium ion homeostasis)
GO:0055085 (transmembrane transport)
GO:0060048 (cardiac muscle contraction)
GO:0060306 (regulation of membrane repolarization)
GO:0060307 (regulation of ventricular cardiac muscle cell membrane repolarization)
GO:0061337 (cardiac conduction)
GO:0071435 (potassium ion export)
GO:0071805 (potassium ion transmembrane transport)
GO:0086005 (ventricular cardiac muscle cell action potential)
GO:0086010 (membrane depolarization during action potential)
GO:0086011 (membrane repolarization during action potential)
GO:0086013 (membrane repolarization during cardiac muscle cell action potential)
GO:0086091 (regulation of heart rate by cardiac conduction)
GO:0097623 (potassium ion export across plasma membrane)
GO:0098915 (membrane repolarization during ventricular cardiac muscle cell action potential)
GO:1901379 (regulation of potassium ion transmembrane transport)
GO:1901380 (negative regulation of potassium ion transmembrane transport)
GO:1901381 (positive regulation of potassium ion transmembrane transport)
GO:1902303 (negative regulation of potassium ion export)
Wikipedia HERG

Target Cross References - Protein

canSAR Q12809
CGD Long QT syndrome 2; Short QT syndrome 1
Human Protein Atlas ENSG00000055118
IntAct Q12809
Guide to Pharmacology 572
Open Targets ENSG00000055118
PharmGKB PA212
Pharos Q12809 (Tclin)
Reactome R-HSA-1296072 (Voltage gated Potassium channels.)
R-HSA-5576890 (Phase 3 - rapid repolarisation.)
UniProt A5H1P7 C4PFH9 D3DX04 O75418 O75680 Q12809 Q708S9 Q9BT72 Q9BUT7 Q9H3P0

Target Cross References - Domain

InterPro IPR000014 (PAS.)
IPR000595 (cNMP-bd_dom.)
IPR000700 (PAS-assoc_C.)
IPR001610 (PAC.)
IPR003938 (K_chnl_volt-dep_EAG/ELK/ERG.)
IPR003967 (K_chnl_volt-dep_ERG.)
IPR005821 (Ion_trans_dom.)
IPR014710 (RmlC-like_jellyroll.)
IPR018490 (cNMP-bd-like.)
Pfam PF00027 (cNMP_binding)
PF00520 (Ion_trans)
PF13426 (PAS_9)

Target Cross References - Structure

PDBe 1BYW 4HP9 4HQA
CREDO 1BYW 4HP9 4HQA
spacer
spacer