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