Target Validation Information
TTD ID	T64591
Target Name	5-HT 3A receptor (HTR3A)
Type of Target	Successful
Drug Potency against Target	Tropisetron	Drug Info	Ki = 5.3 nM	[3]
	ATI-17000	Drug Info	Ki = 2.3 nM	[17]
		Drug Info	Ki = 1217 nM	[14]
	(4-Quinolin-2-ylpiperazin-1-yl)acetic Acid	Drug Info	Ki = 11.2 nM	[7]
	(R)-zacopride	Drug Info	Ki = 0.7 nM
	1-(biphenyl-4-yl)-3-(4-(piperidin-1-yl)butyl)urea	Drug Info	IC50 = 7900 nM	[12]
	2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole	Drug Info	Ki = 0.99 nM	[14]
	2-(4-Benzyl-piperazin-1-yl)-benzothiazole	Drug Info	IC50 = 3300 nM	[15]
	2-(4-Methyl-piperazin-1-yl)-quinoline	Drug Info	Ki = 3 nM	[1]
	3alpha-(1'-Methyl-2'-Indolecarbonyloxy)-tropane	Drug Info	IC50 = 18 nM	[9]
	3alpha-(2'-Indolecarbonyloxy)-nortropane	Drug Info	IC50 = 32 nM	[9]
	4-((naphthalen-2-yloxy)methyl)piperidine	Drug Info	Ki = 311 nM	[6]
	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Drug Info	Ki < 1000 nM	[13]
	4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane	Drug Info	Ki = 13 nM	[11]
	5,6-dichloro-3,4-dihydroquinazolin-2-amine	Drug Info	Ki = 172 nM	[4]
	5-chloro-3,4-dihydroquinazolin-2-amine	Drug Info	Ki = 1051 nM	[4]
	6-(4-Methyl-piperazin-1-yl)-phenanthridine	Drug Info	Ki = 1.9 nM	[1]
	7-(piperidin-4-ylmethoxy)-2-naphthonitrile	Drug Info	Ki = 404 nM	[6]
	BRL-24682	Drug Info	Ki = 41.8 nM	[2]
	CP-810123	Drug Info	Ki = 269 nM	[11]
	MESULERGINE	Drug Info	IC50 = 2.13 nM	[16]
	Norcisapride	Drug Info	IC50 = 1600 nM	[8]
	PH-709829	Drug Info	Ki = 350 nM	[5]
	QUIPAZINE	Drug Info	Ki = 0.96 nM	[10]
	SEROTONIN	Drug Info	Ki = 120 nM	[1]
References
REF 1	Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy ... J Med Chem. 1999 May 6;42(9):1556-75.
REF 2	Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotoni... J Med Chem. 2003 Feb 27;46(5):702-15.
REF 3	Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 4	Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
REF 5	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:... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5.
REF 6	Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
REF 7	Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. J Med Chem. 2009 Jun 11;52(11):3548-62.
REF 8	mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83.
REF 9	Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors. Bioorg Med Chem. 2009 Oct 1;17(19):6872-8.
REF 10	Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.
REF 11	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 ag... J Med Chem. 2010 Feb 11;53(3):1222-37.
REF 12	Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and... J Med Chem. 2010 Jun 10;53(11):4379-89.
REF 13	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 14	Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. J Med Chem. 1990 Jan;33(1):13-6.
REF 15	Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties. J Med Chem. 1994 Apr 29;37(9):1320-5.
REF 16	Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. J Med Chem. 1997 Oct 24;40(22):3670-8.
REF 17	The ORL-1 receptor system: are there opportunities for antagonists in pain therapy Curr Top Med Chem. 2008;8(16):1442-51.

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