Target Validation Information
Target ID T64591
Target Name 5-hydroxytryptamine receptor 3A
Target Type
Successful
Drug Potency against Target ATI-17000 Drug Info Ki = 2.3 nM [552880]
2-(4-Methyl-piperazin-1-yl)-quinoline Drug Info Ki = 3 nM [525484]
3-(2-Amino-ethyl)-2-methyl-1H-indol-5-ol Drug Info Ki = 1217 nM [532034]
BRL-24682 Drug Info Ki = 41.8 nM [526544]
3alpha-(1'-Methyl-2'-Indolecarbonyloxy)-tropane Drug Info IC50 = 18 nM [530355]
2-(4-Benzyl-piperazin-1-yl)-benzothiazole Drug Info IC50 = 3300 nM [533917]
PH-709829 Drug Info Ki = 350 nM [529479]
Norcisapride Drug Info IC50 = 1600 nM [530330]
Tropisetron Drug Info Ki = 5.3 nM [527799]
1-(biphenyl-4-yl)-3-(4-(piperidin-1-yl)butyl)urea Drug Info IC50 = 7900 nM [530912]
MESULERGINE Drug Info IC50 = 2.13 nM [534503]
2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole Drug Info Ki = 0.99 nM [532034]
6-(4-Methyl-piperazin-1-yl)-phenanthridine Drug Info Ki = 1.9 nM [525484]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 172 nM [529148]
4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane Drug Info Ki = 13 nM [530609]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info Ki = 311 nM [530012]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info Ki = 404 nM [530012]
(R)-zacopride Drug Info Ki = 0.7 nM
3alpha-(2'-Indolecarbonyloxy)-nortropane Drug Info IC50 = 32 nM [530355]
CP-810123 Drug Info Ki = 269 nM [530609]
QUIPAZINE Drug Info Ki = 0.96 nM [530451]
SEROTONIN Drug Info Ki = 120 nM [525484]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 1051 nM [529148]
(4-Quinolin-2-ylpiperazin-1-yl)acetic Acid Drug Info Ki = 11.2 nM [530114]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
References
Ref 552880The ORL-1 receptor system: are there opportunities for antagonists in pain therapy? Curr Top Med Chem. 2008;8(16):1442-51.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 532034J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
Ref 526544J Med Chem. 2003 Feb 27;46(5):702-15.Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
Ref 530355Bioorg Med Chem. 2009 Oct 1;17(19):6872-8. Epub 2009 Aug 20.Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.
Ref 533917J Med Chem. 1994 Apr 29;37(9):1320-5.Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
Ref 529479Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5. Epub 2008 May 1.Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.
Ref 530330Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83. Epub 2009 Aug 8.mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 530912J Med Chem. 2010 Jun 10;53(11):4379-89.Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Ref 534503J Med Chem. 1997 Oct 24;40(22):3670-8.Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
Ref 532034J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 529148Bioorg 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 530609J Med Chem. 2010 Feb 11;53(3):1222-37.Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
Ref 530012Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. Epub 2009 Feb 20.Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
Ref 530012Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. Epub 2009 Feb 20.Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
Ref 530355Bioorg Med Chem. 2009 Oct 1;17(19):6872-8. Epub 2009 Aug 20.Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.
Ref 530609J Med Chem. 2010 Feb 11;53(3):1222-37.Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
Ref 530451J Med Chem. 2009 Nov 12;52(21):6946-50.Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 529148Bioorg 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 530114J Med Chem. 2009 Jun 11;52(11):3548-62.Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
Ref 531079J 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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