Therapeutic Targets Database
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Target Validation Information
TTD IDTTDR00157
Target Name5-hydroxytryptamine 7 receptor    
Type of TargetResearch target    
Drug Potency against TargetSEROTONINIC50 = 1.5 nM[1]
MESULERGINEIC50 = 120 nM[2]
METHIOTHEPINIC50 = 3.1 nM[3]
WAY-208466IC50 = 4764 nM[4]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi < 1000 nM[5]
SB-269970Ki = 1.2 nM[6]
SB-269970Ki = 1.3 nM[7]
SPIPERONEKi = 110 nM[7]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amineKi = 15.9 nM[8]
2-(Biphenyl-2-yloxy)-N,N-dimethylethanamineKi = 156 nM[9]
DisulergineKi = 18 nM[7]
SB-656104Ki = 2 nM[7]
L-745870Ki = 226.3 nM[10]
SB-271046Ki = 260 nM[11]
2-(2-Bromophenoxy)-N,N-dimethylethanamineKi = 2663 nM[9]
5,6-dichloro-3,4-dihydroquinazolin-2-amineKi = 294 nM[8]
SB-258741Ki = 3 nM[7]
(R)-8-phenyl-N,N-dipropylchroman-3-amineKi = 3.38 nM[9]
SB-258719Ki = 32 nM[7]
WAY-466Ki = 329 nM[12]
2-(2-Bromophenylthio)-N,N-dimethylethanamineKi = 4110 nM[9]
2-(Biphenyl-2-ylthio)-N,N-dimethylethanamineKi = 553 nM[9]
(+/-)-nantenineKi = 67 nM[13]
WAY-181187Ki = 679 nM[14]
2-(2'-methyl-biphenyl-3-yl)-ethylamineKi = 7.5 nM[15]
N,N-dimethyl-2-(2'-methylbiphenyl-3-yl)ethanamineKi = 7.6 nM[9]
5-chloro-3,4-dihydroquinazolin-2-amineKi = 793 nM[8]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amineKi = 8.2 nM[8]
1-Naphthalen-1-yl-piperazineKi = 83 nM[7]
UCM-5600Ki = 89 nM[2]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amineKi = 97.4 nM[8]
Ref 1J 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. To Reference
Ref 2J Med Chem. 2009 Apr 23;52(8):2384-92.Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. To Reference
Ref 3Bioorg Med Chem. 2008 Mar 1;16(5):2570-8. Epub 2007 Nov 22.Novel quinazolinone derivatives as 5-HT7 receptor ligands. To Reference
Ref 4Bioorg Med Chem. 2009 Jul 15;17(14):5153-63. Epub 2009 May 29.Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. To Reference
Ref 5J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 6Bioorg Med Chem Lett. 2009 Aug 15;19(16):4827-31. Epub 2009 Jun 13.Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands. To Reference
Ref 7J Med Chem. 2003 Jul 3;46(14):2795-812.Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). To Reference
Ref 8Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. To Reference
Ref 9Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. Epub 2010 Jan 18.SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. To Reference
Ref 10Bioorg Med Chem Lett. 2001 Jun 4;11(11):1375-7.Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. To Reference
Ref 11Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. To Reference
Ref 12J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. To Reference
Ref 13Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. To Reference
Ref 14J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist. To Reference
Ref 15Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22. Epub 2007 Mar 23.Novel aminoethylbiphenyls as 5-HT7 receptor ligands. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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