Target Validation Information
TTD ID T31204
Target Name 5-HT 2B receptor (HTR2B)
Type of Target
Successful
Drug Potency against Target Minaprine Drug Info Ki = 17000 nM [14]
(+/-)-nantenine Drug Info Ki = 543 nM [10]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 7.5 nM [4]
(5-methoxy-1H-indol-3-yl)methanamine Drug Info Ki = 1617 nM [13]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 35 nM [4]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 8.1 nM [4]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info Ki = 3.8 nM [4]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info Ki = 1.7 nM [4]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info Ki = 6 nM [4]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info Ki = 8.7 nM [4]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info Ki = 15 nM [4]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 5.8 nM [2]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info Ki = 7.8 nM [4]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info Ki = 13 nM [4]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info Ki = 38 nM [2]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info Ki = 6300 nM [2]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 745 nM [2]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info Ki = 423 nM [2]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 98 nM [2]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info Ki = 1242 nM [2]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info Ki = 1242 nM [2]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [12]
5-MEO-DMT Drug Info Ki = 52 nM [4]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info Ki = 100 nM [7]
6-Fluoromelatonin Drug Info Ki = 2495 nM [13]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info Ki = 34 nM [7]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info Ki = 90 nM [7]
ADRENOGLOMERULOTROPIN Drug Info Ki = 491 nM [13]
ADS-103253 Drug Info IC50 = 1900 nM [5]
ADS-103274 Drug Info IC50 = 1500 nM [5]
AR-129330 Drug Info IC50 = 9.66 nM [9]
BP-897 Drug Info Ki = 33.1 nM [13]
CHLOROPHENYLPIPERAZINE Drug Info Ki = 24 nM [11]
FENDILINE Drug Info Ki = 3217 nM [13]
Racemic DOI Drug Info IC50 = 3.5 nM [8]
Ro-60-0175 Drug Info Ki = 5.1 nM [3]
SEROTONIN Drug Info Ki = 12 nM [3]
VER-2692 Drug Info Ki = 12 nM [3]
VER-3323 Drug Info Ki = 46 nM [1]
VER-5384 Drug Info Ki = 49 nM [1]
VER-5593 Drug Info Ki = 21 nM [1]
WAY-181187 Drug Info Ki = 458 nM [6]
YM-348 Drug Info Ki = 2.5 nM [7]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 8.39 nM [2]
Action against Disease Model Triflupromazine Drug Info IC50 on pancreatic beta-cell ATP-sensitive potassi uM channels: 4000nM [15]
References
REF 1 Indoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.
REF 2 SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.
REF 3 Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2006 Feb;16(3):677-80.
REF 4 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 5 Quinazoline and benzimidazole MCH-1R antagonists. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7.
REF 6 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 7 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 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... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 9 Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71.
REF 10 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 11 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 12 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 13 Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify no... J Med Chem. 2010 Nov 11;53(21):7573-86.
REF 14 Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
REF 15 Chlorpromazine and related phenothiazines inhibit the ATP-sensitive K+ channel. Eur J Pharmacol. 1991 May 30;198(1):101-4.

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