Target Validation Information
TTD ID	T59679
Target Name	5-HT 4 receptor (HTR4)
Type of Target	Successful
Drug Potency against Target	Tegaserod	Drug Info	EC50 ~= 5 nM
	1-((S)-2-aminopropyl)-1H-indazol-6-ol	Drug Info	Ki = 515 nM	[1]
	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Drug Info	Ki < 1000 nM	[5]
	BARETTIN	Drug Info	Ki = 1910 nM	[2]
	GR-113808	Drug Info	Ki = 0.7 nM	[3]
	Norcisapride	Drug Info	IC50 = 19 nM	[4]
	SB-207710	Drug Info	Ki = 2.2 nM	[6]
	SEROTONIN	Drug Info	Ki = 500 nM	[2]
Action against Disease Model	Tegaserod	Drug Info	EC50 on Afferent nerve activity to rectal distension in cats: 700000ng/kg
References
REF 1	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 2	Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4.
REF 3	Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers. J Med Chem. 2007 Sep 6;50(18):4482-92.
REF 4	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 5	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 6	Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for ... J Med Chem. 2010 Oct 14;53(19):7035-47.

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