Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T83813 | ||||
Target Name | 5-hydroxytryptamine 2C receptor | ||||
Target Type | Successful |
||||
Drug Potency against Target | (R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine | Drug Info | Ki = 63 nM | ||
N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | Ki = 1259 nM | |||
Nefazodone | Drug Info | Ki = 0.1+/-0.09 microM | [553232] | ||
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | Ki = 79 nM | |||
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine | Drug Info | Ki = 4 nM | |||
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine | Drug Info | Ki = 6.3 nM | |||
1-((R)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | Ki = 34 nM | [527952] | ||
WAY-466 | Drug Info | Ki = 235 nM | [527381] | ||
VER-5384 | Drug Info | Ki = 8.7 nM | [527037] | ||
1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | Ki = 3 nM | [527952] | ||
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine | Drug Info | Ki = 32 nM | [529168] | ||
VOLINANSERIN | Drug Info | Ki = 13 nM | [530936] | ||
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol | Drug Info | Ki = 1 nM | [527952] | ||
CHLOROPHENYLPIPERAZINE | Drug Info | Ki = 17 nM | [530589] | ||
BARETTIN | Drug Info | Ki = 340 nM | [528498] | ||
PRUVANSERIN | Drug Info | Ki = 557 nM | [528150] | ||
6-bromoaplysinopsin | Drug Info | Ki = 330 nM | [526321] | ||
4-(piperazin-1-yl)furo[3,2-c]pyridine | Drug Info | Ki = 22 nM | [530516] | ||
1-(2-aminoethyl)-1H-indazol-6-ol | Drug Info | Ki = 9.6 nM | [527952] | ||
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol | Drug Info | Ki = 125 nM | [527668] | ||
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine | Drug Info | Ki = 755 nM | [530516] | ||
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol | Drug Info | Ki = 4.8 nM | [527952] | ||
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol | Drug Info | Ki = 1.2 nM | [527952] | ||
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline | Drug Info | Ki = 45 nM | [530516] | ||
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine | Drug Info | Ki = 127 nM | [530516] | ||
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol | Drug Info | Ki = 539 nM | [527668] | ||
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine | Drug Info | Ki = 207 nM | [530516] | ||
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 152 nM | [529148] | ||
3-(2-Dimethylamino-propyl)-1H-indol-4-ol | Drug Info | Ki = 126 nM | [527668] | ||
5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 208 nM | [529148] | ||
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine | Drug Info | Ki = 156 nM | [530516] | ||
Ro-60-0175 | Drug Info | Ki = 26 nM | [529168] | ||
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine | Drug Info | Ki = 20 nM | [529221] | ||
3-Dimethylaminomethyl-1H-indol-4-ol | Drug Info | Ki = 12.6 nM | [527668] | ||
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine | Drug Info | Ki = 113 nM | [530516] | ||
YM-348 | Drug Info | Ki = 0.89 nM | [529221] | ||
NELOTANSERIN | Drug Info | Ki = 110 nM | [531083] | ||
WAY-181187 | Drug Info | Ki = 124 nM | [529112] | ||
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine | Drug Info | Ki = 4 nM | |||
WAY-208466 | Drug Info | IC50 = 644 nM | [530209] | ||
SR46349B | Drug Info | Ki = 0.35 nM | [553190] | ||
GR-127935 | Drug Info | Ki = 105 nM | [527726] | ||
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine | Drug Info | Ki = 16 nM | [529168] | ||
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine | Drug Info | Ki = 7.9 nM | |||
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 556 nM | [529148] | ||
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide | Drug Info | IC50 = 542 nM | [529582] | ||
(+/-)-nantenine | Drug Info | Ki = 1069 nM | [530558] | ||
6-bromo-2'-de-N-methylaplysinopsin | Drug Info | Ki = 2300 nM | [526321] | ||
Mirtazapine | Drug Info | Ki = 5.5 nM | [552847] | ||
N-3'-ethylaplysinopsin | Drug Info | Ki = 3500 nM | [526321] | ||
Cyclo[(6-bromotryptophan)arginine] | Drug Info | Ki = 4630 nM | [528498] | ||
SEROTONIN | Drug Info | Ki = 20 nM | [528498] | ||
VER-5593 | Drug Info | Ki = 3.2 nM | [527037] | ||
VER-3323 | Drug Info | Ki = 24 nM | [527037] | ||
5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 658 nM | [529148] | ||
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine | Drug Info | Ki = 200 nM | [528690] | ||
APLYSINOPSIN | Drug Info | Ki = 14451 nM | |||
OCTOCLOTHEPIN | Drug Info | Ki = 0.57 nM | [531171] | ||
4-(piperazin-1-yl)thieno[3,2-c]pyridine | Drug Info | Ki = 14 nM | [530516] | ||
1-(piperazin-1-yl)isoquinoline | Drug Info | IC50 = 24 nM | [530516] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [531079] | ||
VER-2692 | Drug Info | Ki = 1.6 nM | [527833] | ||
SB-271046 | Drug Info | Ki = 530 nM | [529191] | ||
5-MEO-DMT | Drug Info | Ki = 42 nM | [527952] | ||
PRUVANSERIN | Drug Info | Ki = 645 nM | [531083] | ||
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | Ki = 8.3 nM | [527952] | ||
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol | Drug Info | Ki = 3.6 nM | [527952] | ||
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | Ki = 50 nM | |||
3-(3-Dimethylamino-propyl)-1H-indol-4-ol | Drug Info | Ki = 84 nM | [527668] | ||
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol | Drug Info | Ki = 14 nM | [527668] | ||
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine | Drug Info | Ki = 84 nM | [527668] | ||
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | Ki = 380 nM | [529148] | ||
6-(piperazin-1-yl)-9-propyl-9H-purine | Drug Info | Ki = 378 nM | [530516] | ||
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine | Drug Info | Ki = 0.2 nM | [529168] | ||
PG-01037 | Drug Info | Ki = 47 nM | [528974] | ||
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol | Drug Info | Ki = 1772 nM | [527668] | ||
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine | Drug Info | Ki = 43 nM | [529168] | ||
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine | Drug Info | Ki = 1 nM | |||
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine | Drug Info | Ki = 23 nM | [529221] | ||
RS-102,221 | Drug Info | IC50 = 8.3 nM | [529789] | ||
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol | Drug Info | Ki = 6800 nM | [527668] | ||
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol | Drug Info | Ki = 4200 nM | [527668] | ||
3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | Ki = 7 nM | [527952] | ||
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol | Drug Info | Ki = 33 nM | [527668] | ||
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine | Drug Info | Ki = 8.8 nM | [529221] | ||
Action against Disease Model | Methysergide | IC50 on synergistic interaction between arachidonic acid and 5-hydroxytryptamine in h uMan platelets: 5.2nM/L | [552384] | Drug Info | |
References | |||||
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Ref 553190 | (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. | ||||
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Ref 530558 | Bioorg 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. | ||||
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Ref 528498 | J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. | ||||
Ref 528498 | J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. | ||||
Ref 527037 | Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists. | ||||
Ref 527037 | Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists. | ||||
Ref 529148 | Bioorg 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. | ||||
Ref 528690 | Bioorg 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 531171 | J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors. | ||||
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Ref 530516 | Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71. Epub 2009 Oct 30.Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. | ||||
Ref 531079 | J 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. | ||||
Ref 527833 | Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. | ||||
Ref 529191 | Bioorg 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. | ||||
Ref 527952 | J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. | ||||
Ref 531083 | J Med Chem. 2010 Aug 12;53(15):5696-706.Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. | ||||
Ref 527952 | J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. | ||||
Ref 527952 | J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 529148 | Bioorg 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. | ||||
Ref 530516 | Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71. Epub 2009 Oct 30.Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. | ||||
Ref 529168 | Bioorg Med Chem. 2008 Feb 15;16(4):1966-82. Epub 2007 Nov 4.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 agonists. | ||||
Ref 528974 | J Med Chem. 2007 Aug 23;50(17):4135-46. Epub 2007 Aug 2.Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 529168 | Bioorg Med Chem. 2008 Feb 15;16(4):1966-82. Epub 2007 Nov 4.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 agonists. | ||||
Ref 529221 | Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. | ||||
Ref 529789 | J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 527952 | J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. | ||||
Ref 527668 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. | ||||
Ref 529221 | Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. |
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