Target Information

Target General Infomation
Target ID
T20251
Former ID
TTDS00147
Target Name
Potassium voltage-gated channel subfamily H member 2
Gene Name
KCNH2
Synonyms
Eag homolog; Eag related protein 1; Erg1; Ether-a-go-go related gene potassium channel 1; Ether-a-go-go related protein 1; H-ERG; HERG K+ channel; Voltage-gated potassium channel subunit Kv11.1; KCNH2
Target Type
Successful
Disease Angina pectoris [ICD9: 413; ICD10: I20]
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49]
Cardiac failure [ICD10: I50]
Heart arrhythmia [ICD10: I47-I49]
Malaria [ICD10: B54]
Multiple scierosis [ICD9: 340; ICD10: G35]
Ovarian cancer [ICD9: 183; ICD10: C56]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
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).
BioChemical Class
Voltage-gated ion channel
Target Validation
T20251
UniProt ID
Q12809
Sequence
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
QLGALTSQPLHRHGSDPGS
Structure
1BYW; 1UJL; 2L0W; 2L1M; 2L4R; 2LE7; 4HP9; 4HQA
Drugs and Mode of Action
Drug(s) VESNARINONE Drug Info Approved Cardiac failure [551871]
VOLINANSERIN Drug Info Phase 3 Discovery agent [522480], [539159]
ABT-229 Drug Info Phase 2 Pain [530085], [538920]
Desmethylastemizole Drug Info Phase 2 Discovery agent [528285]
HP-184 Drug Info Phase 2 Multiple scierosis [536648]
NITD609 Drug Info Phase 2 Malaria [549327]
ISOQUINE Drug Info Phase 1 Malaria [532126]
MK-499 Drug Info Discontinued in Phase 2 Cardiac arrhythmias [539684], [545349]
Bertosamil Drug Info Terminated Angina pectoris [526414]
L-702958 Drug Info Terminated Cardiac arrhythmias [545293]
Inhibitor (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) Drug Info [530215]
(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) Drug Info [530929]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info [528690]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info [530012]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline Drug Info [530904]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info [530367]
(R)-ONDANSETRON Drug Info [529281]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info [530012]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info [530927]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info [530918]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info [530918]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info [530918]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info [530918]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info [530012]
1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane Drug Info [529777]
1-(4-p-Tolyl-butyl)-piperidine Drug Info [530299]
2-Phenyl-3-piperidin-3-yl-1H-indole Drug Info [526043]
2-Phenyl-3-piperidin-4-yl-1H-indole Drug Info [526043]
2-[4-(2-Piperidin-1-ylethyl)phenoxy]benzothiazole Drug Info [529569]
3 9-DIHYDRO-N-DESMETHYL-N-ISOPROPYLERYTHROMYCIN A Drug Info [531177]
3-(1-Benzyl-piperidin-3-yl)-2-phenyl-1H-indole Drug Info [526043]
3-(1-Methyl-piperidin-2-yl)-2-phenyl-1H-indole Drug Info [526043]
3-(1-Methyl-piperidin-3-yl)-2-phenyl-1H-indole Drug Info [526043]
3-(1-Phenethyl-piperidin-3-yl)-2-phenyl-1H-indole Drug Info [526043]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [526043]
3-(1H-indol-3-yl)-N-methyl-3-phenylpropan-1-amine Drug Info [529777]
3-(benzo[b]thiophen-5-yl)-3-benzylpyrrolidine Drug Info [529777]
3-(dimethylamino)-1-(4-heptylphenyl)propan-1-one Drug Info [530166]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info [530012]
4-(2-thienyl)benzene-1,2-diamine Drug Info [529917]
4-(3-thienyl)benzene-1,2-diamine) Drug Info [529917]
4-(p-Tolyl)spiro[chromene-2,4'-piperidine] Drug Info [529689]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info [530324]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Drug Info [529689]
4-Benzenesulfonyl-1-(3-phenyl-propyl)-piperidine Drug Info [526242]
4-Benzenesulfonyl-1-phenethyl-piperidine Drug Info [526242]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info [529689]
5-(3-(4-fluorobenzyl)pyrrolidin-3-yl)-1H-indole Drug Info [529777]
5-(3-benzylpyrrolidin-3-yl)-1-methyl-1H-indole Drug Info [529777]
5-(3-BENZYLPYRROLIDIN-3-YL)-1H-INDOLE (STRUCTURAL MIX) Drug Info [529777]
5-(3-butylpyrrolidin-3-yl)-1H-indole Drug Info [529777]
5-Chloro-3-ethyl-1-(4-fluoro-phenyl)-1H-indole Drug Info [526620]
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) Drug Info [530929]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info [530012]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info [531109]
ABT-229 Drug Info [531177]
ADS-103253 Drug Info [528581]
BMS-645737 Drug Info [529409]
DESMETHEYLASTEMIZOLE Drug Info [526678]
DESMETHYLOLANZAPINE Drug Info [530215]
GW-3430 Drug Info [530026]
ISOQUINE Drug Info [529965]
JNJ-10392980 Drug Info [529569]
MDL-74156 Drug Info [526678]
MK-1925 Drug Info [530242]
MK-499 Drug Info [526620]
N-(4-(benzyloxy)phenethyl)pyridin-4-amine Drug Info [528635]
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) Drug Info [530929]
N-(piperidin-4-yl)-N-propyl-2-naphthamide Drug Info [530367]
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) Drug Info [530871]
NITD609 Drug Info [531146]
PF-526014 Drug Info [530918]
R-dimethindene Drug Info [530300]
VESNARINONE Drug Info [526678]
VOLINANSERIN Drug Info [530936]
[1-(4-p-Tolyl-butyl)-piperidin-4-yl]-methanol Drug Info [530299]
Activator A-935142 Drug Info [530115]
ginsenoside Rg3 Drug Info [531483]
ICA-105574 Drug Info [530426]
KB-130015 Drug Info [530653]
PD-118057 Drug Info [527605]
PD-307243 Drug Info [529181]
RPR260243 Drug Info [536020]
VU0405601 Drug Info [532066]
Modulator Bertosamil Drug Info [526414]
L-702958 Drug Info
Blocker Desmethylastemizole Drug Info [534874]
HP-184 Drug Info [536648]
Opener NS-1643 Drug Info [543879]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
PathWhiz Pathway Muscle/Heart Contraction
Reactome Voltage gated Potassium channels
WikiPathways SIDS Susceptibility Pathways
Hematopoietic Stem Cell Differentiation
Potassium Channels
References
Ref 522480ClinicalTrials.gov (NCT00788515) Comparison of Volinanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties. U.S. National Institutes of Health.
Ref 526414Bertosamil blocks HERG potassium channels in their open and inactivated states. Br J Pharmacol. 2002 Sep;137(2):221-8.
Ref 528285A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2.
Ref 530085Neurogastroenterol Motil. 2009 Jun;21(6):657-64, e30-1.GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility.
Ref 532126Antimalarial activity of isoquine against Kenyan Plasmodium falciparum clinical isolates and association with polymorphisms in pfcrt and pfmdr1 genes. J Antimicrob Chemother. 2013 Apr;68(4):786-8.
Ref 536648Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80.
Ref 538920(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. (Ligand id: 1444).
Ref 539159(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. (Ligand id: 185).
Ref 539684(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. (Ligand id: 2607).
Ref 545293Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002728)
Ref 545349Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002963)
Ref 549327Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035252)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526043J Med Chem. 2001 May 10;44(10):1603-14.3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Ref 526242J Med Chem. 2002 Jan 17;45(2):492-503.4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Ref 526414Bertosamil blocks HERG potassium channels in their open and inactivated states. Br J Pharmacol. 2002 Sep;137(2):221-8.
Ref 526620Bioorg Med Chem Lett. 2003 May 19;13(10):1829-35.Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches.
Ref 526678Bioorg Med Chem Lett. 2003 Aug 18;13(16):2773-5.Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
Ref 527605Novel 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. Epub 2005 Jun 23.
Ref 528581Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists.
Ref 528635J Med Chem. 2007 Feb 22;50(4):807-19. Epub 2007 Jan 24.Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Ref 528690Bioorg Med Chem Lett. 2007 May 1;17(9):2643-8. Epub 2007 Feb 2.2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.
Ref 5291812-[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-related gene potassium channels. Mol Pharmacol. 2008 Mar;73(3):639-51. Epub 2007 Nov 27.
Ref 529281Bioorg Med Chem. 2008 Apr 1;16(7):4107-19. Epub 2008 Jan 16.A binary QSAR model for classification of hERG potassium channel blockers.
Ref 529409Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. Epub 2008 Mar 22.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]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Ref 529569J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Ref 529689J Med Chem. 2008 Oct 9;51(19):5893-6. Epub 2008 Sep 13.Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Ref 529777Bioorg Med Chem Lett. 2008 Dec 1;18(23):6062-6. Epub 2008 Oct 11.Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
Ref 529917Bioorg Med Chem Lett. 2009 Feb 15;19(4):1168-72. Epub 2008 Dec 25.Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.
Ref 529965J Med Chem. 2009 Mar 12;52(5):1408-15.Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
Ref 530012Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. Epub 2009 Feb 20.Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
Ref 530026J Med Chem. 2009 Apr 9;52(7):2076-89.Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormoneantagonists.
Ref 530115Electrophysiologic characterization of a novel hERG channel activator. Biochem Pharmacol. 2009 Apr 15;77(8):1383-90.
Ref 530166J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.
Ref 530215J Med Chem. 2009 Jul 23;52(14):4266-76.Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.
Ref 530242Bioorg Med Chem Lett. 2009 Aug 15;19(16):4729-32. Epub 2009 Jun 17.Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Ref 530299Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7. Epub 2009 Aug 5.Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Ref 530300J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Ref 530324J Med Chem. 2009 Sep 24;52(18):5685-702.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) benzamide (ADL5747).
Ref 530367Bioorg 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.
Ref 530426Pharmacological 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.
Ref 530653The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur J Pharmacol. 2010 Apr 25;632(1-3):52-9.
Ref 530871J Med Chem. 2010 May 27;53(10):4028-37.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-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Ref 530904Bioorg Med Chem Lett. 2010 Jun 1;20(11):3295-300. Epub 2010 Apr 18.In vitro studies on a class of quinoline containing histamine H3 antagonists.
Ref 530918Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. Epub 2010 Apr 18.Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Ref 530927J Med Chem. 2010 Jun 24;53(12):4803-7.Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
Ref 530929Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. Epub 2010 Apr 21.Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Ref 530936Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12. Epub 2010 Apr 24.Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
Ref 531109Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10. Epub 2010 Aug 3.SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Ref 531146Science. 2010 Sep 3;329(5996):1175-80.Spiroindolones, a potent compound class for the treatment of malaria.
Ref 531177Bioorg Med Chem. 2010 Nov 1;18(21):7651-8. Epub 2010 Aug 19.9-Dihydroerythromycin ethers as motilin agonists--developing structure-activity relationships for potency and safety.
Ref 531483Ginsenoside Rg(3) decelerates hERG K(+) channel deactivation through Ser631 residue interaction. Eur J Pharmacol. 2011 Aug 1;663(1-3):59-67.
Ref 532066Identification 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.
Ref 534874Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol. 1999 Jun;10(6):836-43.
Ref 536020Discovery 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. Epub 2004 Nov 17.
Ref 536648Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80.
Ref 543879(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).

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