Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DTD0BMQ)

• DTP Name: Voltage-gated potassium channel Kv11.1 (KCNH2)
• Gene Name: KCNH2
• UniProt ID: Q12809 (KCNH2_HUMAN)
• VARIDT ID: DTD0510
• 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; Kv11.1; LQT2; SQT1; Potassium voltage-gated channel subfamily H member 2; hERG-1; hERG1; Voltage-gated potassium channel subunit Kv11.1
• DTP Family: Voltage-Gated Ion Channel (VIC) Superfamily
• Tissue Specificity: Highly expressed in heart and brain. IsoformsUSO are frequently overexpressed in cancer cells.
• Sequence:
  MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
  QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
  AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
  RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
  PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
  RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
  PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
  TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
  EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
  RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
  GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
  AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
  PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
  FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
  VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
  QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
  PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
  SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
  VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
  QLGALTSQPLHRHGSDPGS
• Function: This transporter 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. Channel properties are modulated by cAMP and subunit assembly.
• Endogenous Substrate(s): Potassium ions
• TCDB ID: 1.A.1.20.1
• Gene ID: 3757
• Reactome Pathway:
  Phase 3 - rapid repolarisation (R-HSA-5576890)
  Voltage gated Potassium channels (R-HSA-1296072)

The Drug Therapeutic Target (DTT) Role of This DTP

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

1 Approved Drug(s) Targeting This DTP

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 DTP

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 DTP

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 DTP

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 DTP

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]

References

• [1] Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2773-5.
• [2] Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
• [3] 9-Dihydroerythromycin ethers as motilin agonists--developing structure-activity relationships for potency and safety. Bioorg Med Chem. 2010 Nov 1;18(21):7651-8.
• [4] Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80.
• [5] Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.
• [6] Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for ... J Med Chem. 2009 Mar 12;52(5):1408-15.
• [7] The sigma-2 (-2) receptor: a review of recent patent applications: 2013-2018.Expert Opin Ther Pat. 2018 Sep;28(9):655-663.
• [8] Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2016 Aug;26(8):933-46.
• [9] P2X7 receptor antagonists: a patent review (2010-2015).Expert Opin Ther Pat. 2017 Mar;27(3):257-267.
• [10] Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches. Bioorg Med Chem Lett. 2003 May 19;13(10):1829-35.
• [11] Bertosamil blocks HERG potassium channels in their open and inactivated states. Br J Pharmacol. 2002 Sep;137(2):221-8.
• [12] Analogs of MK-499 are differentially affected by a mutation in the S6 domain of the hERG K+ channel.Biochem Pharmacol.2009 May 15;77(10):1602-11.
• [13] Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new ... J Med Chem. 2009 Jul 23;52(14):4266-76.
• [14] Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4.
• [15] 2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2643-8.
• [16] Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
• [17] In vitro studies on a class of quinoline containing histamine H3 antagonists. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3295-300.
• [18] Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
• [19] A binary QSAR model for classification of hERG potassium channel blockers. Bioorg Med Chem. 2008 Apr 1;16(7):4107-19.
• [20] Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. J Med Chem. 2010 Jun 24;53(12):4803-7.
• [21] Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reduc... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92.
• [22] Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7.
• [23] 3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists. J Med Chem. 2001 May 10;44(10):1603-14.
• [24] Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
• [25] Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6062-6.
• [26] Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. J Med Chem. 2009 Jul 9;52(13):3892-901.
• [27] Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1168-72.
• [28] Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-pipe... J Med Chem. 2008 Oct 9;51(19):5893-6.
• [29] Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) b... J Med Chem. 2009 Sep 24;52(18):5685-702.
• [30] 4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists. J Med Chem. 2002 Jan 17;45(2):492-503.
• [31] SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10.
• [32] Electrophysiologic characterization of a novel hERG channel activator. Biochem Pharmacol. 2009 Apr 15;77(8):1383-90.
• [33] Quinazoline and benzimidazole MCH-1R antagonists. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7.
• [34] Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]t... Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9.
• [35] Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol. 1999 Jun;10(6):836-43.
• [36] Ginsenoside Rg(3) decelerates hERG K(+) channel deactivation through Ser631 residue interaction. Eur J Pharmacol. 2011 Aug 1;663(1-3):59-67.
• [37] Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concen... J Med Chem. 2009 Apr 9;52(7):2076-89.
• [38] Pharmacological removal of human ether- -go-go-related gene potassium channel inactivation by 3-nitro-N-(4-phenoxyphenyl) benzamide (ICA-105574). Mol Pharmacol. 2010 Jan;77(1):58-68.
• [39] The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur J Pharmacol. 2010 Apr 25;632(1-3):52-9.
• [40] Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4729-32.
• [41] Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetr... J Med Chem. 2007 Feb 22;50(4):807-19.
• [42] Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carbox... J Med Chem. 2010 May 27;53(10):4028-37.
• [43] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 572).
• [44] Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity. Mol Pharmacol. 2005 Sep;68(3):876-84.
• [45] 2-[2-(3,4-dichloro-phenyl)-2,3-dihydro-1H-isoindol-5-ylamino]-nicotinic acid (PD-307243) causes instantaneous current through human ether-a-go-go-r... Mol Pharmacol. 2008 Mar;73(3):639-51.
• [46] Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia. J Med Chem. 2009 Sep 10;52(17):5307-10.
• [47] Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005 Mar;67(3):827-36.
• [48] Identification and characterization of a compound that protects cardiac tissue from human Ether- -go-go-related gene (hERG)-related drug-induced arrhythmias. J Biol Chem. 2012 Nov 16;287(47):39613-25.