Target Validation Information
TTD ID T16691
Target Name 5-HT 6 receptor (HTR6)
Type of Target
Clinical trial
Drug Potency against Target SB-742457 Drug Info Ki = 0.25 nM [30]
Drug Info Ki = 400 nM [1]
(+/-)-nantenine Drug Info Ki = 257 nM [25]
1-(2-Methoxy-phenyl)-piperazine Drug Info Ki = 1.2 nM [5]
1-(3-(benzyloxy)-2-methylphenyl)piperazine Drug Info Ki = 1.3 nM [21]
1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole Drug Info Ki = 1 nM [10]
1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole Drug Info Ki = 1 nM [9]
1-Benzenesulfonyl-3-piperidin-4-yl-1H-indole Drug Info IC50 = 19.5 nM [3]
1-naphthylpiperazine Drug Info Ki = 100 nM [5]
1-phenylthio-N,N-dimethyltryptamine Drug Info Ki = 90 nM [18]
2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine Drug Info Ki = 10 nM [15]
2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine Drug Info Ki = 3 nM [20]
2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine Drug Info Ki = 6 nM [20]
2-(1-tosyl-1H-indol-3-yl)ethanamine Drug Info Ki = 8 nM [15]
2-(3-(phenylsulfonyl)-1H-indol-1-yl)ethanamine Drug Info Ki = 25 nM [22]
2-(3-benzenesulfonyl)phenyl-1-aminoethane Drug Info Ki = 50 nM [12]
2-(3-phenylthio)phenyl)-1-aminoethane Drug Info Ki = 115 nM [12]
2-(4-(benzenesulfonyl)phenyl)-1-aminoethane Drug Info Ki = 37 nM [12]
2-Benzyl-4-piperazin-1-yl-1H-benzimidazole Drug Info Ki = 31 nM [26]
2-Ethyl-5-methoxy-3-piperidin-4-yl-1H-indole Drug Info IC50 = 300 nM [8]
3-(phenylsulfonyl)-1-(piperidin-3-yl)-1H-indole Drug Info Ki = 13 nM [27]
3-(phenylsulfonyl)-1-(piperidin-4-yl)-1H-indole Drug Info Ki = 91 nM [27]
3-(phenylsulfonyl)-1-(pyrrolidin-3-yl)-1H-indole Drug Info Ki = 5 nM [27]
4-((1H-indol-1-yl)methyl)benzenamine Drug Info Ki = 8200 nM [14]
4-(1H-Inden-1-ylmethyl)-phenylamine Drug Info Ki = 4470 nM [7]
4-(1H-indol-1-ylsulfonyl)benzenamine Drug Info Ki = 10 nM [10]
4-(1H-Indol-3-ylmethyl)-phenylamine Drug Info Ki = 2530 nM [7]
4-(2-benzenesulfonylphenyl)piperazine Drug Info Ki = 4000 nM [12]
4-(3-benzenesulfonamidophenyl)piperazine Drug Info Ki = 62 nM [12]
4-(3-benzenesulfonylphenyl)piperazine Drug Info Ki = 1.2 nM [12]
4-(3-Methyl-indole-1-sulfonyl)-phenylamine Drug Info Ki = 12 nM [5]
4-(3H-Inden-1-ylmethyl)-phenylamine Drug Info Ki = 11800 nM [7]
4-(4,6-dinitro-1H-indol-1-ylsulfonyl)benzenamine Drug Info Ki = 980 nM [10]
4-(4-benzenesulfonamidophenyl)piperazine Drug Info Ki = 85 nM [12]
4-(4-benzenesulfonylphenyl)piperazine Drug Info Ki = 6.9 nM [12]
4-(4-methoxy-1H-indol-1-ylsulfonyl)benzenamine Drug Info Ki = 3.3 nM [11]
4-(6-methoxy-1H-indol-1-ylsulfonyl)benzenamine Drug Info Ki = 1.8 nM [11]
4-(Indan-1-ylsulfanyl)-phenylamine Drug Info Ki = 4200 nM [7]
4-(Indane-1-sulfonyl)-phenylamine Drug Info Ki = 740 nM [7]
4-(Naphthalene-1-sulfonyl)-phenylamine Drug Info Ki = 34 nM [5]
4-(piperazin-1-yl)-1H-indole Drug Info Ki = 2700 nM [10]
4-(piperazin-1-yl)-3-tosyl-1H-indazole Drug Info Ki = 134 nM [29]
4-Indan-1-ylmethyl-phenylamine Drug Info Ki = 6100 nM [7]
4-Inden-(1E)-ylidenemethyl-phenylamine Drug Info Ki = 640 nM [7]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 1157 nM [16]
5-(4-Methylpiperazin-1-yl)-3-tosyl-1H-indazole Drug Info IC50 = 112 nM [29]
5-MEO-DMT Drug Info Ki = 13 nM [13]
5-METHOXYTRYPTAMINE Drug Info Ki < 50 nM [6]
6-(piperazin-1-yl)-3-tosyl-1H-indazole Drug Info Ki = 27 nM [29]
6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole Drug Info Ki = 29 nM [19]
CHLOROPHENYLPIPERAZINE Drug Info Ki = 2300 nM [1]
DIMEBOLIN Drug Info Ki = 26 nM [24]
E-6837 Drug Info Ki = 0.7 nM [20]
EDMT Drug Info Ki = 16 nM [20]
METHIOTHEPIN Drug Info IC50 = 2.4 nM [28]
N,N-diethyl-2-(1H-indol-3-yl)ethanamine Drug Info Ki = 575 nM [13]
N,N-dimethyl-2-(1-tosyl-1H-indol-3-yl)ethanamine Drug Info Ki = 2.5 nM [14]
N-(3-(2-aminoethyl)phenyl)benzenesulfonamide Drug Info Ki = 21 nM [12]
N-(3-(3-aminopropyl)phenyl)benzenesulfonamide Drug Info Ki = 230 nM [12]
N-(3-(aminomethyl)phenyl)benzenesulfonamide Drug Info Ki = 290 nM [12]
N-(3-aminophenyl)benzenesulfonamide Drug Info Ki = 2840 nM [12]
N-(4-(2-aminoethyl)phenyl)benzenesulfonamide Drug Info Ki = 38 nM [12]
N-phenyl-3-(2-aminoethyl)benzenesulfonamide Drug Info Ki = 70 nM [12]
OCTOCLOTHEPIN Drug Info Ki < 50 nM [6]
QUIPAZINE Drug Info Ki = 3600 nM [1]
Ro-04-6790 Drug Info Ki = 47 nM [20]
SB-271046 Drug Info Ki = 0.66 nM [21]
SB-357134 Drug Info Ki = 3 nM [17]
SEROTONIN Drug Info IC50 = 27.5 nM [28]
WAY-181187 Drug Info Ki = 2 nM [23]
WAY-208466 Drug Info Ki = 4.8 nM [22]
WAY-466 Drug Info Ki = 1 nM [4]
[2-(3-Benzyl-3H-inden-1-yl)-ethyl]-methyl-amine Drug Info Ki = 3 nM [7]
[2-(3-Benzyl-3H-indol-1-yl)-ethyl]-dimethyl-amine Drug Info Ki = 6 nM [2]
[2-(3-Benzyl-indol-1-yl)-ethyl]-dimethyl-amine Drug Info Ki = 32 nM [7]
[2-(3H-Indol-1-yl)-ethyl]-dimethyl-amine Drug Info Ki = 1900 nM [2]
[3H]Ro 63-0563 Drug Info Ki = 512 nM [17]
[3H]spiperone Drug Info Ki = 1595 nM [1]
Action against Disease Model SB-742457 Drug Info The effect of a selective 5-HT(6) receptor antagonist SB-742457 to reverse sub-chronic phencyclidine (PCP)-induced cognitive deficits in female rats was examined. The PCP-induced selective reversal learning deficit was significantly improved by SB-742457. [31]
References
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REF 2 Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4569-73.
REF 3 N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2005 Jan 17;15(2):379-83.
REF 4 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 5 1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1707-11.
REF 6 Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J Med Chem. 2005 Mar 24;48(6):1781-95.
REF 7 Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1987-91.
REF 8 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4.
REF 9 Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4780-5.
REF 10 Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5298-302.
REF 11 Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3793-6.
REF 12 Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. J Med Chem. 2006 Aug 24;49(17):5217-25.
REF 13 Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5832-5.
REF 14 Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1691-4.
REF 15 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 16 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 17 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 18 Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. J Med Chem. 2008 Feb 14;51(3):603-11.
REF 19 A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3929-31.
REF 20 Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. J Med Chem. 2009 Feb 12;52(3):675-87.
REF 21 Synthesis and SAR of tolylamine 5-HT6 antagonists. Bioorg Med Chem Lett. 2009 May 1;19(9):2409-12.
REF 22 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 23 Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists. J Med Chem. 2009 Oct 8;52(19):6153-7.
REF 24 8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. Eur J Med Chem. 2010 Feb;45(2):782-9.
REF 25 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 26 Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation. J Med Chem. 2010 Feb 11;53(3):1357-69.
REF 27 3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1657-60.
REF 28 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. J Med Chem. 2010 Mar 25;53(6):2521-7.
REF 29 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. J Med Chem. 2010 Nov 11;53(21):7639-46.
REF 30 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics. 2008 Jul;5(3):458-69.
REF 31 Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms. Psychopharmacology (Berl). 2010 Jan;208(1):23-36.

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