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Approval Year

Unknown
149124
Substance Class Protein
Created
by admin
on Wed Apr 02 02:17:01 GMT 2025
Edited
by admin
on Wed Apr 02 02:17:01 GMT 2025
Protein Sub Type
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
SEV29N8JND
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ETHER-A-GO-GO-RELATED GENE POTASSIUM CHANNEL 1
Preferred Name English
POTASSIUM VOLTAGE-GATED CHANNEL SUBFAMILY H MEMBER 2
Common Name English
H-ERG
Common Name English
HERG
Common Name English
HERG-1
Common Name English
Code System Code Type Description
FDA UNII
SEV29N8JND
Created by admin on Wed Apr 02 02:17:01 GMT 2025 , Edited by admin on Wed Apr 02 02:17:01 GMT 2025
PRIMARY
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_598
Related Record Type Details
Structure of N-Desmethylapalutamide
INHIBITOR->OFF-TARGET
Structure of M-3258
NON-INHIBITOR->OFF TARGET
IC50
Structure of Dofetilide H-3
RADIOLIGAND->TARGET
Kd
Structure of BMS-986142
INHIBITOR->OFF-TARGET
Structure of LUXEPTINIB
INHIBITOR->OFF-TARGET
IC50
Structure of PF-05089771
NON-INHIBITOR->OFF TARGET
IC50
Structure of DESMETHYLASTEMIZOLE
INHIBITOR->OFF-TARGET
One of the most potent HERG channel blockers.
BINDING
IC50
Structure of LNP-1892
NON-INHIBITOR->OFF TARGET
4% inhibition 10 micromolar
Structure of MIK-665
NON-INHIBITOR->OFF TARGET
Structure of AVAPRITINIB
INHIBITOR->OFF-TARGET
Structure of BEDAQUILINE
INHIBITOR->OFF-TARGET
IC50
Structure of PF- 06895751
NON-INHIBITOR->OFF TARGET
Structure of BOCIDELPAR
INHIBITOR->OFF-TARGET
Structure of APOMORPHINE
INHIBITOR->OFF-TARGET
Structure of AVANAFIL
INHIBITOR->OFF-TARGET
Avanafil inhibited hERG current in a concentration-dependent manner with IC50 of 15.8 ?M, which corresponded to exposures approximately 290-fold above the unbound Cmax (~26 ng/mL, 0.054 ?M) in human subjects after the maximum recommended single oral dose at 200 mg.
IC50
Structure of Cambritaxestat
INHIBITOR->OFF-TARGET
Inhibited the hERG tail current. Based on the high potency of IOA-289 in human plasma and the relatively high plasma protein binding in human of 99%, these activities are not considered to be a significant safety concern.
IC50
Structure of Pimicotinib
INHIBITOR->OFF-TARGET
Assay done in HEK293 cells. At dosages of 5, 15, and 30 mg/kg had no effect on cardiovascular function, respiratory function and body temperature in conscious cynomolgus monkeys after oral gavage administration
IC50
Structure of ASTEMIZOLE
INHIBITOR->OFF-TARGET
BINDING
IC50
Structure of Lunresertib
NON-INHIBITOR->OFF TARGET
Patch clamp assay
IC50
Structure of LML-134
NON-INHIBITOR->OFF TARGET
6% inhibition at 10 micromolar
IC50
Structure of PF-06273340
NON-INHIBITOR->OFF TARGET
IC50
Structure of ACT-774312
WEAK INHIBITOR->OFF TARGET
IC50
Structure of Apalutamide
INHIBITOR->OFF-TARGET
Structure of EVIFACOTREP
NON-INHIBITOR->OFF TARGET
IC50
Structure of AZD-6703
NON-INHIBITOR->OFF TARGET
Structure of AMIODARONE
INHIBITOR -> TARGET
BINDING
IC50
Structure of POSELTINIB
INHIBITOR->OFF-TARGET
Structure of LY-3522348
NON-INHIBITOR->OFF TARGET
14% inhibition at 10 micromolar
BINDING
Structure of Zgwatinib
INHIBITOR->OFF-TARGET
Structure of MK-8768
WEAK INHIBITOR->OFF TARGET
Structure of LORLATINIB
NON-INHIBITOR->OFF TARGET
did not predict QTc prolongation, by inhibition of the hERG channel at clinically relevant concentrations
Structure of Acalabrutinib
NON-INHIBITOR->OFF TARGET
Structure of VANOXERINE
INHIBITOR -> TARGET
Potent blocker of cardiac hERG, Na and Ca channels; (2) block is strongly frequency-dependent especially for Na and Ca channels;has characteristics of a potentially effective and safe antiarrhythmic.
IC50
Structure of TAFENOQUINE
INHIBITOR -> TARGET
IC50
Structure of TECASTEMIZOLE
INHIBITOR->OFF-TARGET
Structure of LATREPIRDINE
INHIBITOR->OFF-TARGET
Structure of TP-0556351
NON-INHIBITOR->OFF TARGET
Structure of CEP-40783
NON-INHIBITOR->OFF TARGET
Structure of SSR-181507
INHIBITOR->OFF-TARGET
Structure of HYDROXYZINE
INHIBITOR->OFF-TARGET
IC50
Structure of NETARSUDIL
INHIBITOR->OFF-TARGET
Structure of MORPHOTHIADINE
INHIBITOR->OFF-TARGET
IC50
Structure of DOMPERIDONE
INHIBITOR->OFF-TARGET
IC50
Structure of Renzapride
NON-INHIBITOR->OFF TARGET
IC50
Structure of LYS-006
NON-INHIBITOR->OFF TARGET
IC50
Structure of ERVOGASTAT
NON-INHIBITOR->OFF TARGET
Structure of E-4031
INHIBITOR -> TARGET
Structure of BETRIXABAN
INHIBITOR->OFF-TARGET
Structure of GLPG-2737
NON-INHIBITOR->OFF TARGET
Structure of JTE-151
INHIBITOR->OFF-TARGET
IC50
Structure of MIK-665
NON-INHIBITOR->OFF-TARGET
Structure of W-18
INHIBITOR -> TARGET
Structure of BN-104
OFF-TARGET->NON-INHIBITOR
IC50
Structure of MK-8189
WEAK INHIBITOR->OFF TARGET
Structure of PACRITINIB
INHIBITOR->OFF-TARGET
IC50
Structure of OTESECONAZOLE
INHIBITOR->OFF-TARGET
Cloned hERG Potassium Channels Expressed in Human Embryonic Kidney Cells
IC50
Structure of Migoprotafib
INHIBITOR->OFF-TARGET
IC50
Structure of ASTEMIZOLE
INHIBITOR -> TARGET
control substance
BINDING
IC50
Structure of Paltusotine
INHIBITOR->OFF-TARGET
Patch-clamp hERG assay
IC50
Structure of SOTORASIB
INHIBITOR->OFF-TARGET
Weak Inhibitor
Structure of Tuspetinib
INHIBITOR->OFF-TARGET
Structure of Idrebormilast
INHIBITOR->OFF-TARGET
IC50
Structure of INCB-3284
INHIBITOR->OFF-TARGET
Structure of Nuvisertib
NON-INHIBITOR->OFF TARGET
IC50
Structure of LY-3381916
NON-INHIBITOR->OFF-TARGET
Structure of HRO-761
NON-INHIBITOR->OFF TARGET
IC50
Structure of Taragarestrant
NON-INHIBITOR->OFF TARGET
Structure of Resmetirom
INHIBITOR->OFF-TARGET
IC50
Structure of AZD-1390
INHIBITOR->OFF-TARGET
IC50
Structure of Risdiplam
NON-INHIBITOR->OFF TARGET
Structure of VEBRELTINIB
INHIBITOR->OFF-TARGET
Structure of IRUPLINALKIB
NON-INHIBITOR->OFF TARGET
Structure of N-MONODESMETHYL BEDAQUILINE
INHIBITOR->OFF-TARGET
MAY BE RESPONSIBLE FOR QT PROLONGATION
IC50
Structure of TD-2749
NON-INHIBITOR->OFF TARGET
9% inhibition at 3 MICROMOLAR
IC50
Structure of PF-04634817
NON-INHIBITOR->OFF TARGET
Structure of IBUTILIDE
INHIBITOR -> TARGET
Structure of ZUCLOPENTHIXOL
INHIBITOR->OFF-TARGET
IC50
Structure of GIREDESTRANT
INHIBITOR->OFF-TARGET
Structure of RMC-5552
NON-INHIBITOR->OFF TARGET
16% inhibition at 10 micromolar
Structure of BOSUTINIB
INHIBITOR->OFF-TARGET
Structure of PL-8177
NON-INHIBITOR->OFF TARGET
IC50
Structure of Desmethyl-sudapyridine
INHIBITOR->OFF-TARGET
Structure of SUN-1334
NON-INHIBITOR->OFF TARGET
IC50
Structure of Mevrometostat
NON-INHIBITOR->OFF TARGET
Structure of VIMSELTINIB
INHIBITOR->OFF-TARGET
IC50
Structure of Risovalisib
NON-INHIBITOR->OFF TARGET
Structure of Fudapirine
NON-INHIBITOR->OFF TARGET
Structure of VERUBECESTAT
INHIBITOR->OFF-TARGET
Structure of CIFENLINE
INHIBITOR -> TARGET
IC50
Structure of Tapinarof
INHIBITOR->OFF-TARGET
IC50
Structure of TERFENADINE
INHIBITOR -> TARGET
BINDING
IC50
Structure of Simnotrelvir
NON-INHIBITOR->OFF TARGET
Structure of ERVOGASTAT
NON-INHIBITOR -> TRANSPORTER
Structure of Zgwatinib monodeuterated
INHIBITOR->OFF-TARGET
Deuterium substitution reduced HERG inhibition substantially
IC50
Structure of MITAPIVAT
INHIBITOR->OFF-TARGET
IC50
Structure of INE-963
INHIBITOR->OFF-TARGET
IC50
Structure of SOTALOL
INHIBITOR -> TARGET
Structure of PF-07258669
WEAK INHIBITOR->OFF TARGET

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID SUBSTITUTION [1_243] [1_283] [1_284] [1_320] [1_351] [1_871] [1_874] [1_1137] DEXFOSFOSERINE VI4F0K069V
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
Molecular Formula CHEMICAL
NIH
NCATS
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