Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQ6VDM)

• DTT Name: Voltage-gated potassium channel Kv11.1 (KCNH2)
• Synonyms: hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
• Gene Name: KCNH2
• DTT Type: Successful target; [1]
• BioChemical Class: Voltage-gated ion channel
• UniProt ID: KCNH2_HUMAN
• TTD ID: T20251
• Sequence:
  MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
  QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
  AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
  RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
  PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
  RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
  PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
  TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
  EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
  RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
  GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
  AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
  PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
  FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
  VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
  QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
  PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
  SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
  VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
  QLGALTSQPLHRHGSDPGS
• Function: Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel.
• Reactome Pathway: Voltage gated Potassium channels (R-HSA-1296072)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
VESNARINONE	DMBKX3C	Cardiac failure	BD10-BD13	Approved	[1]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[2]
ABT-229	DMN3S1B	Pain	MG30-MG3Z	Phase 2	[3]
HP-184	DMNOMV2	Multiple sclerosis	8A40	Phase 2	[4]
NITD609	DMQHBSX	Malaria	1F40-1F45	Phase 2	[5]
ISOQUINE	DMR17YI	Malaria	1F40-1F45	Phase 1	[6]

10 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Isoindoline derivative 1	DMD19QC	N. A.	N. A.	Patented	[7]
Isoindoline derivative 2	DMTE0S3	N. A.	N. A.	Patented	[7]
Isoindoline derivative 3	DM2MYL9	N. A.	N. A.	Patented	[7]
Isoindoline derivative 4	DMP1NKI	N. A.	N. A.	Patented	[7]
Isoindoline derivative 5	DMIUTQW	N. A.	N. A.	Patented	[7]
Pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazine derivative 1	DMC8935	N. A.	N. A.	Patented	[8]
Pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazine derivative 2	DM4CSBD	N. A.	N. A.	Patented	[8]
Quinoline derivative 11	DMH02JL	N. A.	N. A.	Patented	[9]
Quinoline derivative 12	DM9FXE7	N. A.	N. A.	Patented	[9]
Quinoline derivative 13	DMAH4P8	N. A.	N. A.	Patented	[9]

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MK-499	DMVEGW6	Cardiac arrhythmias	BC9Z	Discontinued in Phase 2	[10]
Bertosamil	DM56WD3	Angina pectoris	BA40	Terminated	[11]
L-702958	DMO7GWC	Cardiac arrhythmias	BC9Z	Terminated	[12]

71 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(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)	DMUJ7ZE	Discovery agent	N.A.	Investigative	[13]
(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)	DMXPQU6	Discovery agent	N.A.	Investigative	[14]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine	DMTJI4F	Discovery agent	N.A.	Investigative	[15]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine	DM94B12	Discovery agent	N.A.	Investigative	[16]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline	DM3LQFK	Discovery agent	N.A.	Investigative	[17]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide	DMJFH97	Discovery agent	N.A.	Investigative	[18]
(R)-ONDANSETRON	DMCYD8Q	Discovery agent	N.A.	Investigative	[19]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine	DM5ILK1	Discovery agent	N.A.	Investigative	[16]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane	DMDFU6S	Discovery agent	N.A.	Investigative	[20]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane	DMNLUKS	Discovery agent	N.A.	Investigative	[20]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane	DM5Z6XG	Discovery agent	N.A.	Investigative	[20]
1,6-bis(4-phenylpiperazin-1-yl)hexane	DMD3EUI	Discovery agent	N.A.	Investigative	[20]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX)	DMCSOAV	Discovery agent	N.A.	Investigative	[21]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX)	DMS9PZ7	Discovery agent	N.A.	Investigative	[21]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine	DM54ZKU	Discovery agent	N.A.	Investigative	[21]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX)	DMUJ2WB	Discovery agent	N.A.	Investigative	[21]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine	DMR4DJ1	Discovery agent	N.A.	Investigative	[16]
1-(4-p-Tolyl-butyl)-piperidine	DMFYK6T	Discovery agent	N.A.	Investigative	[22]
2-Phenyl-3-piperidin-3-yl-1H-indole	DMY6NIT	Discovery agent	N.A.	Investigative	[23]
2-Phenyl-3-piperidin-4-yl-1H-indole	DMEXZQ5	Discovery agent	N.A.	Investigative	[23]
2-[4-(2-Piperidin-1-ylethyl)phenoxy]benzothiazole	DMMYJ3R	Discovery agent	N.A.	Investigative	[24]
3 9-DIHYDRO-N-DESMETHYL-N-ISOPROPYLERYTHROMYCIN A	DMOAY8R	Discovery agent	N.A.	Investigative	[3]
3-(1-Benzyl-piperidin-3-yl)-2-phenyl-1H-indole	DMGDN93	Discovery agent	N.A.	Investigative	[23]
3-(1-Methyl-piperidin-2-yl)-2-phenyl-1H-indole	DMK8LHB	Discovery agent	N.A.	Investigative	[23]
3-(1-Methyl-piperidin-3-yl)-2-phenyl-1H-indole	DM4UD8C	Discovery agent	N.A.	Investigative	[23]
3-(1-Phenethyl-piperidin-3-yl)-2-phenyl-1H-indole	DMOQ4ER	Discovery agent	N.A.	Investigative	[23]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole	DM8TH2N	Discovery agent	N.A.	Investigative	[23]
3-(1H-indol-3-yl)-N-methyl-3-phenylpropan-1-amine	DMEV6Q2	Discovery agent	N.A.	Investigative	[25]
3-(benzo[b]thiophen-5-yl)-3-benzylpyrrolidine	DM58GRA	Discovery agent	N.A.	Investigative	[25]
3-(dimethylamino)-1-(4-heptylphenyl)propan-1-one	DMG5VMH	Discovery agent	N.A.	Investigative	[26]
4-((naphthalen-2-yloxy)methyl)piperidine	DMIQHYZ	Discovery agent	N.A.	Investigative	[16]
4-(2-thienyl)benzene-1,2-diamine	DM4YWQN	Discovery agent	N.A.	Investigative	[27]
4-(3-thienyl)benzene-1,2-diamine)	DML4NJU	Discovery agent	N.A.	Investigative	[27]
4-(p-Tolyl)spiro[chromene-2,4'-piperidine]	DMIOQJD	Discovery agent	N.A.	Investigative	[28]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide	DM0XDG6	Discovery agent	N.A.	Investigative	[29]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol	DM8ZRAE	Discovery agent	N.A.	Investigative	[28]
4-Benzenesulfonyl-1-(3-phenyl-propyl)-piperidine	DMACRHS	Discovery agent	N.A.	Investigative	[30]
4-Benzenesulfonyl-1-phenethyl-piperidine	DMCKT3Q	Discovery agent	N.A.	Investigative	[30]
4-Phenylspiro[chromene-2,4'-piperidine]	DMW46K7	Discovery agent	N.A.	Investigative	[28]
5-(3-(4-fluorobenzyl)pyrrolidin-3-yl)-1H-indole	DMR35OM	Discovery agent	N.A.	Investigative	[25]
5-(3-benzylpyrrolidin-3-yl)-1-methyl-1H-indole	DM2ZUFO	Discovery agent	N.A.	Investigative	[25]
5-(3-benzylpyrrolidin-3-yl)-1h-indole (structural mix)	DMZK4AH	Discovery agent	N.A.	Investigative	[25]
5-(3-butylpyrrolidin-3-yl)-1H-indole	DMPKGJC	Discovery agent	N.A.	Investigative	[25]
5-Chloro-3-ethyl-1-(4-fluoro-phenyl)-1H-indole	DM207CQ	Discovery agent	N.A.	Investigative	[10]
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)	DMEJ83H	Ovarian cancer	2C73	Investigative	[14]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile	DM6I5K1	Discovery agent	N.A.	Investigative	[16]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide	DMQMSZR	Discovery agent	N.A.	Investigative	[31]
A-935142	DMBF1OY	Discovery agent	N.A.	Investigative	[32]
ADS-103253	DMH9A4S	Discovery agent	N.A.	Investigative	[33]
BMS-645737	DMBTMO9	Discovery agent	N.A.	Investigative	[34]
Desmethylastemizole	DM58XJN	Discovery agent	N.A.	Investigative	[35]
DESMETHYLOLANZAPINE	DMLKBNR	Discovery agent	N.A.	Investigative	[13]
ginsenoside Rg3	DMFN58T	Discovery agent	N.A.	Investigative	[36]
GW803430	DMWAEJ3	Discovery agent	N.A.	Investigative	[37]
ICA-105574	DMS9H2P	Discovery agent	N.A.	Investigative	[38]
JNJ-10392980	DMZH0K8	Discovery agent	N.A.	Investigative	[24]
KB-130015	DMO72XF	Discovery agent	N.A.	Investigative	[39]
MDL-74156	DMF8VX3	Discovery agent	N.A.	Investigative	[1]
MK-1925	DM3NDWK	Discovery agent	N.A.	Investigative	[40]
N-(4-(benzyloxy)phenethyl)pyridin-4-amine	DMIPKNQ	Discovery agent	N.A.	Investigative	[41]
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)	DMSX5DI	Discovery agent	N.A.	Investigative	[14]
N-(piperidin-4-yl)-N-propyl-2-naphthamide	DM9QIH4	Discovery agent	N.A.	Investigative	[18]
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)	DMVY7RX	Discovery agent	N.A.	Investigative	[42]
NS-1643	DMT97KV	Heart arrhythmia	BC65	Investigative	[43]
PD-118057	DM0E4OW	Discovery agent	N.A.	Investigative	[44]
PD-307243	DMLU9P6	Discovery agent	N.A.	Investigative	[45]
PF-526014	DMD8QOZ	Discovery agent	N.A.	Investigative	[21]
R-dimethindene	DM6FVZW	Discovery agent	N.A.	Investigative	[46]
RPR260243	DM4T2R3	Discovery agent	N.A.	Investigative	[47]
VU0405601	DMLPMAY	Discovery agent	N.A.	Investigative	[48]
[1-(4-p-Tolyl-butyl)-piperidin-4-yl]-methanol	DMAGW3R	Discovery agent	N.A.	Investigative	[22]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Type 2 diabetes	5A11	Liver tissue	8.21E-02	-0.12	-0.91
Liver cancer	2C82	Liver tissue	6.97E-02	-0.25	-1.72
Ovarian cancer	2C82	Ovarian tissue	2.31E-01	0.4	0.61
Schizophrenia	6A20	Pre-frontal cortex	3.26E-02	-0.17	-0.31
Schizophrenia	6A20	Superior temporal cortex	9.12E-01	-0.01	-0.03

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Voltage-gated potassium channel Kv11.1 (KCNH2) DTP Info
• Gene Name: KCNH2

References

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