Target Validation Information
TTD ID T79062
Target Name 5-HT 7 receptor (HTR7)
Type of Target
Clinical trial
Drug Potency against Target (+/-)-nantenine Drug Info Ki = 67 nM [11]
(R)-8-phenyl-N,N-dipropylchroman-3-amine Drug Info Ki = 3.38 nM [12]
1-naphthylpiperazine Drug Info Ki = 83 nM [1]
2-(2'-methyl-biphenyl-3-yl)-ethylamine Drug Info Ki = 7.5 nM [3]
2-(2-Bromophenoxy)-N,N-dimethylethanamine Drug Info Ki = 2663 nM [12]
2-(2-Bromophenylthio)-N,N-dimethylethanamine Drug Info Ki = 4110 nM [12]
2-(Biphenyl-2-yloxy)-N,N-dimethylethanamine Drug Info Ki = 156 nM [12]
2-(Biphenyl-2-ylthio)-N,N-dimethylethanamine Drug Info Ki = 553 nM [12]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [13]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 294 nM [5]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 793 nM [5]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 97.4 nM [5]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 15.9 nM [5]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 8.2 nM [5]
Disulergine Drug Info Ki = 18 nM [1]
MESULERGINE Drug Info IC50 = 120 nM [9]
METHIOTHEPIN Drug Info IC50 = 3.1 nM [7]
N,N-dimethyl-2-(2'-methylbiphenyl-3-yl)ethanamine Drug Info Ki = 7.6 nM [12]
SB-258719 Drug Info Ki = 32 nM [1]
SB-258741 Drug Info Ki = 3 nM [1]
SB-271046 Drug Info Ki = 260 nM [6]
SB-656104 Drug Info Ki = 2 nM [1]
SEROTONIN Drug Info IC50 = 1.5 nM [8]
UCM-5600 Drug Info Ki = 89 nM [9]
WAY-181187 Drug Info Ki = 679 nM [4]
WAY-208466 Drug Info IC50 = 4764 nM [10]
WAY-466 Drug Info Ki = 329 nM [2]
[3H]spiperone Drug Info Ki = 110 nM [1]
References
REF 1 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
REF 2 Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.
REF 3 Novel aminoethylbiphenyls as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22.
REF 4 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. J Med Chem. 2007 Nov 15;50(23):5535-8.
REF 5 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
REF 6 Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43.
REF 7 Novel quinazolinone derivatives as 5-HT7 receptor ligands. Bioorg Med Chem. 2008 Mar 1;16(5):2570-8.
REF 8 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.
REF 9 Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. J Med Chem. 2009 Apr 23;52(8):2384-92.
REF 10 Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. Bioorg Med Chem. 2009 Jul 15;17(14):5153-63.
REF 11 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 12 SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. Bioorg Med Chem. 2010 Mar 1;18(5):1958-67.
REF 13 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.

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