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 [1]
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 [2]
WAY-466 Drug Info Ki = 235 nM [3]
VER-5384 Drug Info Ki = 8.7 nM [4]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 3 nM [2]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 32 nM [5]
VOLINANSERIN Drug Info Ki = 13 nM [6]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info Ki = 1 nM [2]
CHLOROPHENYLPIPERAZINE Drug Info Ki = 17 nM [7]
BARETTIN Drug Info Ki = 340 nM [8]
PRUVANSERIN Drug Info Ki = 557 nM [9]
6-bromoaplysinopsin Drug Info Ki = 330 nM [10]
4-(piperazin-1-yl)furo[3,2-c]pyridine Drug Info Ki = 22 nM [11]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info Ki = 9.6 nM [2]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info Ki = 125 nM [12]
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Drug Info Ki = 755 nM [11]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info Ki = 4.8 nM [2]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info Ki = 1.2 nM [2]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info Ki = 45 nM [11]
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine Drug Info Ki = 127 nM [11]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info Ki = 539 nM [12]
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine Drug Info Ki = 207 nM [11]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 152 nM [13]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 126 nM [12]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 208 nM [13]
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine Drug Info Ki = 156 nM [11]
Ro-60-0175 Drug Info Ki = 26 nM [5]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info Ki = 20 nM [14]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info Ki = 12.6 nM [12]
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 113 nM [11]
YM-348 Drug Info Ki = 0.89 nM [14]
NELOTANSERIN Drug Info Ki = 110 nM [15]
WAY-181187 Drug Info Ki = 124 nM [16]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 4 nM
WAY-208466 Drug Info IC50 = 644 nM [17]
SR46349B Drug Info Ki = 0.35 nM [18]
GR-127935 Drug Info Ki = 105 nM [19]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 16 nM [5]
(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 [13]
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide Drug Info IC50 = 542 nM [20]
(+/-)-nantenine Drug Info Ki = 1069 nM [21]
6-bromo-2'-de-N-methylaplysinopsin Drug Info Ki = 2300 nM [10]
Mirtazapine Drug Info Ki = 5.5 nM [22]
N-3'-ethylaplysinopsin Drug Info Ki = 3500 nM [10]
Cyclo[(6-bromotryptophan)arginine] Drug Info Ki = 4630 nM [8]
SEROTONIN Drug Info Ki = 20 nM [8]
VER-5593 Drug Info Ki = 3.2 nM [4]
VER-3323 Drug Info Ki = 24 nM [4]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 658 nM [13]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info Ki = 200 nM [23]
APLYSINOPSIN Drug Info Ki = 14451 nM
OCTOCLOTHEPIN Drug Info Ki = 0.57 nM [24]
4-(piperazin-1-yl)thieno[3,2-c]pyridine Drug Info Ki = 14 nM [11]
1-(piperazin-1-yl)isoquinoline Drug Info IC50 = 24 nM [11]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [25]
VER-2692 Drug Info Ki = 1.6 nM [26]
SB-271046 Drug Info Ki = 530 nM [27]
5-MEO-DMT Drug Info Ki = 42 nM [2]
PRUVANSERIN Drug Info Ki = 645 nM [15]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info Ki = 8.3 nM [2]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info Ki = 3.6 nM [2]
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 [12]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 14 nM [12]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 84 nM [12]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 380 nM [13]
6-(piperazin-1-yl)-9-propyl-9H-purine Drug Info Ki = 378 nM [11]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info Ki = 0.2 nM [5]
PG-01037 Drug Info Ki = 47 nM [28]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info Ki = 1772 nM [12]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 43 nM [5]
(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 [14]
RS-102,221 Drug Info IC50 = 8.3 nM [29]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info Ki = 6800 nM [12]
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 4200 nM [12]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info Ki = 7 nM [2]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info Ki = 33 nM [12]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info Ki = 8.8 nM [14]
Action against Disease Model Methysergide IC50 on synergistic interaction between arachidonic acid and 5-hydroxytryptamine in h uMan platelets: 5.2nM/L [30] Drug Info
References
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REF 2J 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.
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REF 17Bioorg 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.
REF 18(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 19Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
REF 20Bioorg Med Chem Lett. 2008 Jul 15;18(14):3844-7. Epub 2008 Jun 21.Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.
REF 21Bioorg 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.
REF 225-HT(2A) inverse-agonists for the treatment of insomnia. Curr Top Med Chem. 2008;8(11):969-76.
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REF 24J 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.
REF 25J 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.
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