Target Validation Information
TTD ID T83813
Target Name 5-HT 2C receptor (HTR2C)
Type of Target
Successful
Drug Potency against Target Drug Info Ki = 0.1+/-0.09 microM [30]
Mirtazapine Drug Info Ki = 5.5 nM [28]
SR46349B Drug Info Ki = 0.35 nM [29]
Drug Info Ki = 79 nM
Drug Info Ki = 34 nM [7]
Drug Info Ki = 17 nM [22]
Drug Info Ki = 20 nM [16]
Drug Info Ki = 556 nM [13]
Drug Info Ki = 658 nM [13]
Drug Info Ki = 84 nM [4]
Drug Info Ki = 1772 nM [4]
Drug Info IC50 = 8.3 nM [18]
(+/-)-nantenine Drug Info Ki = 1069 nM [21]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info Ki = 0.2 nM [14]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 43 nM [14]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 32 nM [14]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 16 nM [14]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info Ki = 200 nM [10]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info Ki = 4 nM
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 7.9 nM
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 6.3 nM
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info Ki = 63 nM
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 4 nM
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 1 nM
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 3 nM [7]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info Ki = 1.2 nM [7]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info Ki = 1 nM [7]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info Ki = 4.8 nM [7]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info Ki = 3.6 nM [7]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info Ki = 9.6 nM [7]
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 4200 nM [4]
1-(piperazin-1-yl)isoquinoline Drug Info IC50 = 24 nM [20]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 14 nM [4]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info Ki = 8.3 nM [7]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info Ki = 45 nM [20]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info Ki = 7 nM [7]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info Ki = 33 nM [4]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info Ki = 6800 nM [4]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info Ki = 539 nM [4]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 126 nM [4]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info Ki = 125 nM [4]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info Ki = 12.6 nM [4]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [24]
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Drug Info Ki = 755 nM [20]
4-(piperazin-1-yl)furo[3,2-c]pyridine Drug Info Ki = 22 nM [20]
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine Drug Info Ki = 127 nM [20]
4-(piperazin-1-yl)thieno[3,2-c]pyridine Drug Info Ki = 14 nM [20]
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 113 nM [20]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 208 nM [13]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 380 nM [13]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 152 nM [13]
5-MEO-DMT Drug Info Ki = 42 nM [7]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info Ki = 8.8 nM [16]
6-(piperazin-1-yl)-9-propyl-9H-purine Drug Info Ki = 378 nM [20]
6-bromo-2'-de-N-methylaplysinopsin Drug Info Ki = 2300 nM [1]
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine Drug Info Ki = 207 nM [20]
6-bromoaplysinopsin Drug Info Ki = 330 nM [1]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info Ki = 50 nM
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine Drug Info Ki = 156 nM [20]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info Ki = 23 nM [16]
Aplysinopsin Drug Info Ki = 14451 nM
BARETTIN Drug Info Ki = 340 nM [9]
Cyclo[(6-bromotryptophan)arginine] Drug Info Ki = 4630 nM [9]
GR-127935 Drug Info Ki = 105 nM [5]
M100907 Drug Info Ki = 13 nM [23]
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide Drug Info IC50 = 542 nM [17]
N-(pyridin-3-yl)indoline-1-carboxamide Drug Info Ki = 1259 nM
N-3'-ethylaplysinopsin Drug Info Ki = 3500 nM [1]
NELOTANSERIN Drug Info Ki = 110 nM [25]
OCTOCLOTHEPIN Drug Info Ki = 0.57 nM [26]
PG-01037 Drug Info Ki = 47 nM [11]
PRUVANSERIN Drug Info Ki = 557 nM [8]
PRUVANSERIN Drug Info Ki = 645 nM [25]
Ro-60-0175 Drug Info Ki = 26 nM [14]
SB-271046 Drug Info Ki = 530 nM [15]
SEROTONIN Drug Info Ki = 20 nM [9]
VER-2692 Drug Info Ki = 1.6 nM [6]
VER-3323 Drug Info Ki = 24 nM [2]
VER-5384 Drug Info Ki = 8.7 nM [2]
VER-5593 Drug Info Ki = 3.2 nM [2]
WAY-181187 Drug Info Ki = 124 nM [12]
WAY-208466 Drug Info IC50 = 644 nM [19]
WAY-466 Drug Info Ki = 235 nM [3]
YM-348 Drug Info Ki = 0.89 nM [16]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 84 nM [4]
Action against Disease Model Methysergide Drug Info IC50 on synergistic interaction between arachidonic acid and 5-hydroxytryptamine in h uMan platelets: 5.2nM/L [27]
References
REF 1 New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea. J Nat Prod. 2002 Apr;65(4):476-80.
REF 2 Indoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.
REF 3 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 4 SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.
REF 5 Synthesis of potent and selective serotonin 5-HT1B receptor ligands. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.
REF 6 Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2006 Feb;16(3):677-80.
REF 7 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.
REF 8 A new class of selective, non-basic 5-HT2A receptor antagonists. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3201-4.
REF 9 Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4.
REF 10 2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2643-8.
REF 11 Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46.
REF 12 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 13 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 14 Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor a... Bioorg Med Chem. 2008 Feb 15;16(4):1966-82.
REF 15 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 16 Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. Bioorg Med Chem. 2008 Mar 15;16(6):3309-20.
REF 17 Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3844-7.
REF 18 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 19 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 20 Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71.
REF 21 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 22 Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33.
REF 23 Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
REF 24 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.
REF 25 Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. J Med Chem. 2010 Aug 12;53(15):5696-706.
REF 26 Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adre... J Med Chem. 2010 Oct 14;53(19):7021-34.
REF 27 Synergism interaction between arachidonic acid by 5-hydroxytryptamine in human platelet aggregation is mediated through multiple signalling pathways. Acta Pharmacol Sin. 2003 Oct;24(10):958-64.
REF 28 5-HT(2A) inverse-agonists for the treatment of insomnia. Curr Top Med Chem. 2008;8(11):969-76.
REF 29 (1-(2,5-dimethoxy-4 iodophenyl)-2-aminopropane)-induced head-twitches in the rat are mediated by 5-hydroxytryptamine (5-HT) 2A receptors: modulation by novel 5-HT2A/2C antagonists, D1 antagonists and 5-HT1A agonists. J Pharmacol Exp Ther. 1995 Apr;273(1):101-12.
REF 30 Inhibition of cytochrome P450 by nefazodone in vitro: studies of dextromethorphan O- and N-demethylation. Br J Clin Pharmacol. 1996 Apr;41(4):339-43.

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