Details of the Target

General Information of Target

Target ID LDTP05657
Target Name Potassium voltage-gated channel subfamily H member 2 (KCNH2)
Gene Name KCNH2
Gene ID 3757
Synonyms
ERG; ERG1; HERG; Potassium voltage-gated channel subfamily H member 2; Eag homolog; Ether-a-go-go-related gene potassium channel 1; ERG-1; Eag-related protein 1; Ether-a-go-go-related protein 1; H-ERG; hERG-1; hERG1; Voltage-gated potassium channel subunit Kv11.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
QLGALTSQPLHRHGSDPGS
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Potassium channel family, H (Eag) (TC 1.A.1.20) subfamily, Kv11.1/KCNH2 sub-subfamily
Subcellular location
Cell membrane
Function
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr).; [Isoform A-USO]: Has no channel activity by itself, but modulates channel characteristics by forming heterotetramers with other isoforms which are retained intracellularly and undergo ubiquitin-dependent degradation.; [Isoform B-USO]: Has no channel activity by itself, but modulates channel characteristics by forming heterotetramers with other isoforms which are retained intracellularly and undergo ubiquitin-dependent degradation.
TTD ID
T20251
Uniprot ID
Q12809
DrugMap ID
TTQ6VDM
Ensemble ID
ENST00000262186.10
HGNC ID
HGNC:6251
ChEMBL ID
CHEMBL240

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 Deletion: p.G149AfsTer17 .
AN3CA Deletion: p.T152PfsTer14
SNV: p.L155P		 .
CAL51 Deletion: p.L200Ter .
CCK81 SNV: p.L401M .
COLO320 SNV: p.Q676Ter; p.T1062N .
COLO829 SNV: p.L468F .
DEL SNV: p.R696C .
HT115 SNV: p.D712N .
IM95 SNV: p.Q11P .
JURKAT Deletion: p.G965EfsTer9; p.L987CfsTer70 .
LS180 Deletion: p.T152PfsTer14
SNV: p.C265Y		 .
MELJUSO SNV: p.H485P .
MEWO SNV: p.P1121L .
NCIH1666 SNV: p.A536P; p.N733K .
NCIH196 SNV: p.R894G .
NCIH2172 SNV: p.L1073M .
NCIH716 SNV: p.A565T .
RVH421 Substitution: p.P334L .
SKMEL24 SNV: p.E214K .
SNU1 SNV: p.Y667C .
SUPT1 SNV: p.Y812H .
TOV21G SNV: p.H254Q .
WM793 SNV: p.M579I .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C265(10.00)  LDD2157  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Caveolin-1 (CAV1) Caveolin family Q03135
Potassium voltage-gated channel subfamily H member 2 (KCNH2) Potassium channel family Q12809
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
FERM domain-containing protein 8 (FRMD8) . Q9BZ67

The Drug(s) Related To This Target

Approved
Click To Hide/Show 53 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amiodarone Small molecular drug DB01118
Amitriptyline Small molecular drug DB00321
Amsacrine Small molecular drug DB00276
Astemizole Small molecular drug DB00637
Bepridil Small molecular drug DB01244
Betrixaban Small molecular drug DB12364
Carvedilol Small molecular drug DB01136
Chlorpromazine Small molecular drug DB00477
Ciprofloxacin Small molecular drug DB00537
Cisapride Small molecular drug DB00604
Clarithromycin Small molecular drug DB01211
Disopyramide Small molecular drug DB00280
Dofetilide Small molecular drug DB00204
Doxazosin Small molecular drug DB00590
Doxepin Small molecular drug DB01142
Dronedarone Small molecular drug DB04855
Enflurane Small molecular drug DB00228
Erythromycin Small molecular drug DB00199
Flecainide Small molecular drug DB01195
Fluoxetine Small molecular drug DB00472
Fluvoxamine Small molecular drug DB00176
Halofantrine Small molecular drug DB01218
Hydroxyzine Small molecular drug DB00557
Ibutilide Small molecular drug DB00308
Imipramine Small molecular drug DB00458
Isavuconazole Small molecular drug DB11633
Ketoconazole Small molecular drug DB01026
Loperamide Small molecular drug DB00836
Loratadine Small molecular drug DB00455
Miconazole Small molecular drug DB01110
Nefazodone Small molecular drug DB01149
Perhexiline Small molecular drug DB01074
Phenytoin Small molecular drug DB00252
Pimozide Small molecular drug DB01100
Pitolisant Small molecular drug DB11642
Prazosin Small molecular drug DB00457
Procainamide Small molecular drug DB01035
Promethazine Small molecular drug DB01069
Propafenone Small molecular drug DB01182
Quinidine Small molecular drug DB00908
Sertindole Small molecular drug DB06144
Silodosin Small molecular drug DB06207
Sotalol Small molecular drug DB00489
Tamoxifen Small molecular drug DB00675
Terazosin Small molecular drug DB01162
Terfenadine Small molecular drug DB00342
Thioridazine Small molecular drug DB00679
Verapamil Small molecular drug DB00661
Vernakalant Small molecular drug DB06217
Vesnarinone Small molecular drug D0L0ZF
Chlorobutanol . DB11386
Pentoxyverine . DB11186
Potassium Nitrate . DB11090
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
M100907 Small molecular drug D0HZ2E
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abt-229 Small molecular drug D07MKL
Hp-184 Small molecular drug D02TIK
Nitd609 Small molecular drug D0LI1C
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isoquine Small molecular drug D03GNI
Investigative
Click To Hide/Show 74 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(1r,5r)-30-oxo-19-oxa-2,6,10,12-tetraazahexacyclo[18.6.2.1^{2,5}.1^{14,18}.0^{8,12}.0^{23,27}]Triaconta-8,10,14(29),15,17,20(28),21,23(27)-octaene-17-carbonitrile (Structural Mix) Small molecular drug D0DM6F
(2r)-n-(6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2h-pyrano[2,3-b]Pyridin-4-yl)-2-hydroxypropanamide (Enantiomeric Mix) Small molecular drug D01MCD
(E)-2-(4-fluorostyryl)-5-(Phenylsulfinyl)Pyridine Small molecular drug D08JCU
(R)-3-(Naphthalen-2-ylmethoxy)Pyrrolidine Small molecular drug D0XF5P
(R)-6-(2-(2-methylpyrrolidin-1-yl)Ethyl)Quinoline Small molecular drug D06NXK
(R)-n-isobutyl-n-(Pyrrolidin-3-yl)-2-naphthamide Small molecular drug D01JYY
(R)-ondansetron Small molecular drug D09GZH
(S)-3-(Naphthalen-2-ylmethoxy)Pyrrolidine Small molecular drug D0E3DM
1,6-bis(4-(3-chlorophenyl)Piperazin-1-yl)Hexane Small molecular drug D03XKL
1,6-bis(4-(3-methoxyphenyl)Piperazin-1-yl)Hexane Small molecular drug D03PIP
1,6-bis(4-m-tolylpiperazin-1-yl)Hexane Small molecular drug D00CCV
1,6-bis(4-phenylpiperazin-1-yl)Hexane Small molecular drug D0C6BP
1-(1-(2-fluorophenyl)-2-(2-(Trifluoromethoxy)Phenyl)Ethyl)Piperazine (Enantiomeric Mix) Small molecular drug D0GG2J
1-(1-(4-fluorophenyl)-2-(2-(Trifluoromethoxy)Phenyl)Ethyl)Piperazine (Enantiomeric Mix) Small molecular drug D08EKQ
1-(1-phenyl-2-(2-propoxyphenyl)Ethyl)Piperazine Small molecular drug D01ABR
1-(2-(2-(Difluoromethoxy)Phenyl)-1-phenylethyl)Piperazine (Enantiomeric Mix) Small molecular drug D09FIC
1-(2-(6-fluoronaphthalen-2-yl)Ethyl)Piperazine Small molecular drug D0S9AY
1-(4-p-tolyl-butyl)-piperidine Small molecular drug D0I0UW
2-phenyl-3-piperidin-3-yl-1h-indole Small molecular drug D0RC9T
2-phenyl-3-piperidin-4-yl-1h-indole Small molecular drug D08CZT
2-[4-(2-piperidin-1-ylethyl)Phenoxy]Benzothiazole Small molecular drug D0Q8LS
3 9-dihydro-n-desmethyl-n-isopropylerythromycin A Small molecular drug D03PSY
3-(1-benzyl-piperidin-3-yl)-2-phenyl-1h-indole Small molecular drug D0FL1D
3-(1-methyl-piperidin-2-yl)-2-phenyl-1h-indole Small molecular drug D0ND5D
3-(1-methyl-piperidin-3-yl)-2-phenyl-1h-indole Small molecular drug D07ETF
3-(1-phenethyl-piperidin-3-yl)-2-phenyl-1h-indole Small molecular drug D01PYU
3-(1-phenethyl-piperidin-4-yl)-2-phenyl-1h-indole Small molecular drug D07GBV
3-(1h-indol-3-yl)-n-methyl-3-phenylpropan-1-amine Small molecular drug D0BW0V
3-(Benzo[B]Thiophen-5-yl)-3-benzylpyrrolidine Small molecular drug D07LFR
3-(Dimethylamino)-1-(4-heptylphenyl)Propan-1-one Small molecular drug D07MAF
4-((Naphthalen-2-yloxy)Methyl)Piperidine Small molecular drug D01FFX
4-(2-thienyl)Benzene-1,2-diamine Small molecular drug D08ZIS
4-(3-thienyl)Benzene-1,2-diamine) Small molecular drug D00FAY
4-(P-tolyl)Spiro[Chromene-2,4'-piperidine] Small molecular drug D0H3GI
4-(Spiro[Chromene-2,4'-piperidine]-4-yl)Benzamide Small molecular drug D0L9YP
4-(Spiro[Chromene-2,4'-piperidine]-4-yl)Phenol Small molecular drug D02EIB
4-benzenesulfonyl-1-(3-phenyl-propyl)-piperidine Small molecular drug D03NRJ
4-benzenesulfonyl-1-phenethyl-piperidine Small molecular drug D0G7LE
4-phenylspiro[Chromene-2,4'-piperidine] Small molecular drug D0N2DN
5-(3-(4-fluorobenzyl)Pyrrolidin-3-yl)-1h-indole Small molecular drug D02DCM
5-(3-benzylpyrrolidin-3-yl)-1-methyl-1h-indole Small molecular drug D0I2UC
5-(3-benzylpyrrolidin-3-yl)-1h-indole (Structural Mix) Small molecular drug D0ZC3Q
5-(3-butylpyrrolidin-3-yl)-1h-indole Small molecular drug D0S1XC
5-chloro-3-ethyl-1-(4-fluoro-phenyl)-1h-indole Small molecular drug D01PIU
6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-n-(Hydroxymethyl)-1,2,2-trimethyl-1,2,3,4-tetrahydro-1,8-naphthyridine-4-carboxamide (Enantiomeric Mix) Small molecular drug D0OQ5H
7-(Piperidin-4-ylmethoxy)-2-naphthonitrile Small molecular drug D06QIQ
8-azabicyclo[3.2.1]Octan-3-yloxy-benzamide Small molecular drug D03RBD
A-935142 Small molecular drug D0NM7S
Ads-103253 Small molecular drug D0N6OL
Azimilide Small molecular drug DB04957
Bms-645737 Small molecular drug D0Z7TM
Desmethylastemizole Small molecular drug D0C9UF
Desmethylolanzapine Small molecular drug D05KUM
Ginsenoside Rg3 Small molecular drug D01BKS
Gw803430 Small molecular drug D00AWM
Ica-105574 Small molecular drug D0XH1N
Jnj-10392980 Small molecular drug D00UIN
Kb-130015 Small molecular drug D01WVE
Mdl-74156 Small molecular drug D01IWD
Mk-1925 Small molecular drug D08QBS
N-(4-(Benzyloxy)Phenethyl)Pyridin-4-amine Small molecular drug D07SGS
N-(6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2h-pyrano[2,3-b]Pyridin-4-yl)-3-hydroxypropanamide (Enantiomeric Mix) Small molecular drug D0FJ1I
N-(Piperidin-4-yl)-n-propyl-2-naphthamide Small molecular drug D0A7GW
N-[6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2h-pyrano[2,3-b]Pyridine-4-yl]-4,4,4-trifluoro-3-hydroxybutanamide (Diastereomeric Mix) Small molecular drug D06NXC
Ns-1643 Small molecular drug D0JY2K
Pd-118057 Small molecular drug D09ICL
Pd-307243 Small molecular drug D06EGM
Pf-526014 Small molecular drug D0U7OD
R-dimethindene Small molecular drug D0H8XV
Rpr260243 Small molecular drug D0LM5H
Vanoxerine Small molecular drug DB03701
Vu0405601 Small molecular drug D03WAE
[1-(4-p-tolyl-butyl)-piperidin-4-yl]-methanol Small molecular drug D04MLU
Tecastemizole . DB06457
Patented
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isoindoline Derivative 1 Small molecular drug D0S3ON
Isoindoline Derivative 2 Small molecular drug D0F8XU
Isoindoline Derivative 3 Small molecular drug D06FNA
Isoindoline Derivative 4 Small molecular drug D0EK3Z
Isoindoline Derivative 5 Small molecular drug D02NPB
Pyrido[3,2-e][1,2,4]Triazolo[4,3-a]Pyrazine Derivative 1 Small molecular drug D01LSP
Pyrido[3,2-e][1,2,4]Triazolo[4,3-a]Pyrazine Derivative 2 Small molecular drug D0T8WU
Quinoline Derivative 11 Small molecular drug D0L2KM
Quinoline Derivative 12 Small molecular drug D01EBW
Quinoline Derivative 13 Small molecular drug D0B7KM
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bertosamil Small molecular drug D0AX4E
L-702958 Small molecular drug D00YQZ
Mk-499 Small molecular drug D02NGR

References

1 From chemoproteomic-detected amino acids to genomic coordinates: insights into precise multi-omic data integration. Mol Syst Biol. 2021 Feb;17(2):e9840. doi: 10.15252/msb.20209840.
Mass spectrometry data entry: PXD022151