Target Validation Information
Target ID T20251
Target Name Potassium voltage-gated channel subfamily H member 2
Target Type
Successful
Drug Potency against Target Propafenone Drug Info IC50 = 13 nM/mL [552254]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info IC50 = 260 nM [531109]
ADS-103253 Drug Info IC50 = 10000 nM [528581]
MDL-74156 Drug Info IC50 = 5230 nM [526678]
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 IC50 = 380 nM [530929]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info Ki = 2200 nM [530927]
VOLINANSERIN Drug Info Ki = 1100 nM [530936]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Drug Info IC50 = 643 nM [529689]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline Drug Info Ki = 10000 nM [530904]
E-4031 Drug Info IC50 = 10.2 nM [527041]
R-dimethindene Drug Info IC50 = 900 nM [530300]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info IC50 = 680 nM [529689]
4-(p-Tolyl)spiro[chromene-2,4'-piperidine] Drug Info IC50 = 462 nM [529689]
TERIKALANT Drug Info IC50 = 6600 nM [526678]
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 IC50 = 2470 nM [530871]
(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 IC50 = 120 nM [530929]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info IC50 = 11589 nM [530324]
AZD-5438 Drug Info IC50 = 3200 nM [529792]
Amiodarone Drug Info IC50 = 2.8 nM/mL [552247]
(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 IC50 = 7000 nM [530215]
N-(4-(benzyloxy)phenethyl)pyridin-4-amine Drug Info IC50 = 130 nM [528635]
(R)-ONDANSETRON Drug Info IC50 = 810 nM [529281]
MK-499 Drug Info IC50 = 34 nM [526620]
5-Chloro-3-ethyl-1-(4-fluoro-phenyl)-1H-indole Drug Info IC50 = 3500 nM [526620]
2-[4-(2-Piperidin-1-ylethyl)phenoxy]benzothiazole Drug Info IC50 = 2000 nM [529569]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info Ki = 8000 nM [530927]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info Ki = 300 nM [530927]
5-(3-(4-fluorobenzyl)pyrrolidin-3-yl)-1H-indole Drug Info IC50 = 9000 nM [529777]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info Ki = 8500 nM [530012]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info Ki = 7000 nM [530367]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info Ki = 2400 nM [530927]
N-(piperidin-4-yl)-N-propyl-2-naphthamide Drug Info Ki = 12700 nM [530367]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info Ki = 15700 nM [530012]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info Ki = 16400 nM [530012]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info IC50 = 15300 nM [530918]
MK-1925 Drug Info IC50 = 9500 nM [530242]
GW-3430 Drug Info IC50 = 1170 nM [530026]
5-(3-butylpyrrolidin-3-yl)-1H-indole Drug Info IC50 = 4400 nM [529777]
PF-526014 Drug Info IC50 = 6950 nM [530918]
4-(3-thienyl)benzene-1,2-diamine) Drug Info IC50 = 1500 nM [529917]
TERIKALANT Drug Info IC50 = 6700 nM [526678]
DESMETHEYLASTEMIZOLE Drug Info IC50 = 9000 nM [526678]
ISOQUINE Drug Info IC50 = 7500 nM [529965]
PRUVANSERIN Drug Info Ki = 1268 nM [528150]
Brivanib Drug Info IC50 = 18000 nM [528103]
BETRIXABAN Drug Info IC50 = 8900 nM [530941]
VESNARINONE Drug Info IC50 = 5960 nM [526678]
2-Phenyl-3-piperidin-3-yl-1H-indole Drug Info Ki = 4900 nM [526043]
5-(3-benzylpyrrolidin-3-yl)-1-methyl-1H-indole Drug Info IC50 = 7000 nM [529777]
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 IC50 = 40 nM [530929]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info Ki = 3800 nM [530012]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info Ki = 3500 nM [530012]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 80 nM [526043]
3-(1-Methyl-piperidin-2-yl)-2-phenyl-1H-indole Drug Info Ki = 7000 nM [526043]
3-(1-Phenethyl-piperidin-3-yl)-2-phenyl-1H-indole Drug Info Ki = 530 nM [526043]
5-(3-BENZYLPYRROLIDIN-3-YL)-1H-INDOLE (STRUCTURAL MIX) Drug Info IC50 = 9000 nM [529777]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info IC50 = 760 nM [530918]
3-(benzo[b]thiophen-5-yl)-3-benzylpyrrolidine Drug Info IC50 = 11000 nM [529777]
1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 10000 nM [529777]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info IC50 = 4950 nM [530918]
4-Benzenesulfonyl-1-(3-phenyl-propyl)-piperidine Drug Info Ki = 2500 nM [526242]
4-Benzenesulfonyl-1-phenethyl-piperidine Drug Info Ki = 1800 nM [526242]
3-(1H-indol-3-yl)-N-methyl-3-phenylpropan-1-amine Drug Info IC50 = 1000 nM [529777]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info IC50 = 5840 nM [530918]
BMS-645737 Drug Info IC50 = 6600 nM [529409]
JNJ-10392980 Drug Info IC50 = 1000 nM [529569]
ISOQUINE Drug Info IC50 = 3900 nM [529965]
N-DESMETHYLCLOZAPINE Drug Info IC50 = 4490 nM [530215]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info Ki = 3900 nM [528690]
DESMETHYLOLANZAPINE Drug Info IC50 = 14200 nM [530215]
3-(1-Methyl-piperidin-3-yl)-2-phenyl-1H-indole Drug Info Ki = 9600 nM [526043]
3-(1-Benzyl-piperidin-3-yl)-2-phenyl-1H-indole Drug Info Ki = 290 nM [526043]
2-Phenyl-3-piperidin-4-yl-1H-indole Drug Info Ki = 5700 nM [526043]
4-(2-thienyl)benzene-1,2-diamine Drug Info IC50 = 1600 nM [529917]
Dofetilide Drug Info IC50 = 0.32 nM/mL [553266]
References
Ref 552254Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel. Naunyn Schmiedebergs Arch Pharmacol. 2001 Apr;363(4):472-80.
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 528581Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists.
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 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 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 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 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 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 527041J Med Chem. 2004 Apr 22;47(9):2318-25.Design, synthesis, and biological evaluation of substituted 2-cyclohexyl-4-phenyl-1H-imidazoles: potent and selective neuropeptide Y Y5-receptor antagonists.
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 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 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 526678Bioorg Med Chem Lett. 2003 Aug 18;13(16):2773-5.Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
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 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 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 529792Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9. Epub 2008 Oct 22.Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.
Ref 552247Short- and long-term effects of amiodarone on the two components of cardiac delayed rectifier K(+) current. Circulation. 2001 Mar 6;103(9):1317-24.
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 526678Bioorg Med Chem Lett. 2003 Aug 18;13(16):2773-5.Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
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 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 528150Bioorg Med Chem Lett. 2006 Jun 15;16(12):3201-4. Epub 2006 May 2.A new class of selective, non-basic 5-HT2A receptor antagonists.
Ref 528103J Med Chem. 2006 Apr 6;49(7):2143-6.Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Ref 530941J Med Chem. 2010 Sep 9;53(17):6243-74.Factor Xa inhibitors: next-generation antithrombotic agents.
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 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 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 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 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 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 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 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 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 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 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 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 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 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 526242J Med Chem. 2002 Jan 17;45(2):492-503.4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-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 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 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 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 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 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 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 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 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 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 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 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 553266Molecular determinants of dofetilide block of HERG K+ channels. Circ Res. 1998 Feb 23;82(3):386-95.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.