Target Information
Target General Infomation | |||||
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Target ID |
T20251
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Former ID |
TTDS00147
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Target Name |
Potassium voltage-gated channel subfamily H member 2
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Gene Name |
KCNH2
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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
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Target Type |
Successful
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Disease | Angina pectoris [ICD9: 413; ICD10: I20] | ||||
Cardiac failure [ICD10: I50] | |||||
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49] | |||||
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).
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BioChemical Class |
Voltage-gated ion channel
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Target Validation |
T20251
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UniProt ID | |||||
Sequence |
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG QLGALTSQPLHRHGSDPGS |
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Structure |
1BYW; 1UJL; 2L0W; 2L1M; 2L4R; 2LE7; 4HP9; 4HQA
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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 522480 | ClinicalTrials.gov (NCT00788515) Comparison of Volinanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties. U.S. National Institutes of Health. | ||||
Ref 526414 | Bertosamil blocks HERG potassium channels in their open and inactivated states. Br J Pharmacol. 2002 Sep;137(2):221-8. | ||||
Ref 528285 | A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2. | ||||
Ref 530085 | Neurogastroenterol 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 532126 | Antimalarial 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 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 545293 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002728) | ||||
Ref 545349 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002963) | ||||
Ref 526043 | J 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 526242 | J Med Chem. 2002 Jan 17;45(2):492-503.4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists. | ||||
Ref 526414 | Bertosamil blocks HERG potassium channels in their open and inactivated states. Br J Pharmacol. 2002 Sep;137(2):221-8. | ||||
Ref 526620 | Bioorg 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 526678 | Bioorg Med Chem Lett. 2003 Aug 18;13(16):2773-5.Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. | ||||
Ref 527605 | 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. Epub 2005 Jun 23. | ||||
Ref 528581 | Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists. | ||||
Ref 528635 | J 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 528690 | Bioorg 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 529181 | 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-related gene potassium channels. Mol Pharmacol. 2008 Mar;73(3):639-51. Epub 2007 Nov 27. | ||||
Ref 529281 | Bioorg 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 529409 | Bioorg 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 529569 | J 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 529689 | J 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 529777 | Bioorg 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 529917 | Bioorg 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 529965 | J 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 530012 | Bioorg 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 530026 | J 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 530115 | Electrophysiologic characterization of a novel hERG channel activator. Biochem Pharmacol. 2009 Apr 15;77(8):1383-90. | ||||
Ref 530166 | J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. | ||||
Ref 530215 | J 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 530242 | Bioorg 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 530299 | Bioorg 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 530300 | J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia. | ||||
Ref 530324 | J 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 530367 | 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. | ||||
Ref 530426 | 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. | ||||
Ref 530653 | The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur J Pharmacol. 2010 Apr 25;632(1-3):52-9. | ||||
Ref 530871 | J 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 530904 | Bioorg 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 530918 | Bioorg 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 530927 | J 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 530929 | Bioorg 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 530936 | Bioorg 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 531109 | Bioorg 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 531146 | Science. 2010 Sep 3;329(5996):1175-80.Spiroindolones, a potent compound class for the treatment of malaria. | ||||
Ref 531177 | Bioorg 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 531483 | Ginsenoside Rg(3) decelerates hERG K(+) channel deactivation through Ser631 residue interaction. Eur J Pharmacol. 2011 Aug 1;663(1-3):59-67. | ||||
Ref 532066 | 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. | ||||
Ref 534874 | Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol. 1999 Jun;10(6):836-43. |
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