Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00104
Target Name5-hydroxytryptamine 2B receptor    
Type of TargetSuccessful target    
Drug Potency against TargetMinaprineKi = 17000 nM[1]
ADS-103274IC50 = 1500 nM[2]
ADS-103253IC50 = 1900 nM[2]
(+/-)DOIIC50 = 3.5 nM[3]
ATC-0175IC50 = 9.66 nM[4]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi < 1000 nM[5]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-olKi = 1.7 nM[6]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepineKi = 100 nM[7]
SEROTONINKi = 12 nM[8]
VER-2692Ki = 12 nM[8]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-olKi = 1242 nM[9]
3-Dimethylaminomethyl-1H-indol-4-olKi = 1242 nM[9]
5-hydroxy-alpha-methyltryptamineKi = 13 nM[6]
1-(2-aminoethyl)-1H-indazol-6-olKi = 15 nM[6]
(5-methoxy-1H-indol-3-yl)methanamineKi = 1617 nM[10]
YM-348Ki = 2.5 nM[7]
VER-5593Ki = 21 nM[11]
CHLOROPHENYLPIPERAZINEKi = 24 nM[12]
6-FluoromelatoninKi = 2495 nM[10]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-olKi = 3.8 nM[6]
FENDILINEKi = 3217 nM[10]
BP-897Ki = 33.1 nM[10]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepineKi = 34 nM[7]
1-((R)-2-aminopropyl)-1H-indazol-6-olKi = 35 nM[6]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-olKi = 38 nM[9]
SB-206553Ki = 4.3 nM[10]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-olKi = 423 nM[9]
WAY-181187Ki = 458 nM[13]
VER-3323Ki = 46 nM[11]
VER-5384Ki = 49 nM[11]
ADRENOGLOMERULOTROPINKi = 491 nM[10]
Ro-60-0175;Ro-600175Ki = 5.1 nM[8]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-olKi = 5.8 nM[9]
5-MEO-DMTKi = 52 nM[6]
(+/-)-nantenineKi = 543 nM[14]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-olKi = 6 nM[6]
3-(2-Dimethylamino-ethyl)-1H-indol-6-olKi = 6300 nM[9]
(S)-2-(6-methoxyindazol-1-yl)-1-methylethylamineKi = 7.5 nM[6]
5-methoxy-alpha-methyltryptamineKi = 7.8 nM[6]
3-(2-Dimethylamino-propyl)-1H-indol-4-olKi = 745 nM[9]
1-((S)-2-aminopropyl)-1H-indazol-6-olKi = 8.1 nM[6]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amineKi = 8.39 nM[9]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-olKi = 8.7 nM[6]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepineKi = 90 nM[7]
3-(3-Dimethylamino-propyl)-1H-indol-4-olKi = 98 nM[9]
Action against Disease ModelTriflupromazineIC50 on pancreatic beta-cell ATP-sensitive potassi uM channels: 4000nM[15]
Ref 1Mini Rev Med Chem. 2007 Nov;7(11):1108-19.Privileged structures: a useful concept for the rational design of new lead drug candidates. To Reference
Ref 2Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists. To Reference
Ref 3J 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. To Reference
Ref 4Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. Epub 2009 Sep 6.Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. To Reference
Ref 5J 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. To Reference
Ref 6J 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. To Reference
Ref 7Bioorg 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. To Reference
Ref 8Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. To Reference
Ref 9Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. To Reference
Ref 10J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs. To Reference
Ref 11Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists. To Reference
Ref 12Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. Epub 2009 Dec 6.Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. To Reference
Ref 13J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.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. To Reference
Ref 14Bioorg 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. To Reference
Ref 15Eur J Pharmacol. 1991 May 30;198(1):101-4.Chlorpromazine and related phenothiazines inhibit the ATP-sensitive K+ channel. To Reference



 

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Professor in Department of Pharmacy
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