| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T70967 | ||||
| Target Name | Neuronal acetylcholine receptor protein, alpha-4 chain | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Pentolinium | Drug Info | IC50 = 3400 nM | [553193] | |
| CYTISINE | Drug Info | Ki = 2.59 nM | [528394] | ||
| BOLDINE | Drug Info | Ki = 3000 nM | [528761] | ||
| N,N-dimethyl-4-(pyridin-3-yl)but-3-yn-1-amine | Drug Info | Ki = 510 nM | [527965] | ||
| N,N-dimethyl(pyridin-3-yl)methanamine | Drug Info | Ki = 540 nM | [527965] | ||
| N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine | Drug Info | Ki = 113 nM | [527965] | ||
| N-ethyl-N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine | Drug Info | Ki = 1770 nM | [527965] | ||
| Varenicline | Drug Info | EC50 = 2300 nM | [552606] | ||
| Sofinicline | Drug Info | EC50 = 40 nM | [530093] | ||
| N,N-dimethyl-2-(pyridin-3-yloxy)ethanamine | Drug Info | Ki = 21 nM | [527965] | ||
| N-methyl-2-(pyridin-3-yloxy)ethanamine | Drug Info | Ki = 35 nM | [527965] | ||
| 3-[2-(N,N,N-trimethylammonium)ethoxy]pyridine | Drug Info | Ki = 0.5 nM | [528245] | ||
| (2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol | Drug Info | IC50 = 6400 nM | [530946] | ||
| 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [531079] | ||
| HOMOEPIBATIDINE | Drug Info | Ki = 0.127 nM | [528394] | ||
| N-methyl-N-(pyridin-3-ylmethyl)ethanamine | Drug Info | Ki = 28 nM | [527965] | ||
| Predicentrine methiodide | Drug Info | Ki = 970 nM | [528761] | ||
| (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol | Drug Info | IC50 = 6000 nM | [530946] | ||
| Trimethaphan | Drug Info | IC50 = 12500 nM | [553193] | ||
| 6'-methylepibatidine | Drug Info | Ki = 256 nM | [529145] | ||
| References | |||||
| Ref 553193 | Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists. Pflugers Arch. 1995 Jan;429(3):449-51. | ||||
| Ref 528394 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships. | ||||
| Ref 528761 | Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 552606 | Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. | ||||
| Ref 530093 | J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. Epub 2009 Apr 23.In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 528245 | Bioorg Med Chem Lett. 2006 Aug 15;16(16):4283-6. Epub 2006 Jun 9.Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors. | ||||
| Ref 530946 | J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. | ||||
| Ref 531079 | 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 528394 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships. | ||||
| Ref 527965 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. | ||||
| Ref 528761 | Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. | ||||
| Ref 530946 | J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. | ||||
| Ref 553193 | Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists. Pflugers Arch. 1995 Jan;429(3):449-51. | ||||
| Ref 529145 | J Med Chem. 2007 Dec 13;50(25):6383-91. Epub 2007 Nov 10.Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine. | ||||
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