Target Validation Information
Target ID T55815
Target Name Neuronal acetylcholinereceptor subunit alpha-2
Target Type
Successful
Drug Potency against Target 5-(1-Methyl-pyrrolidin-2-yl)-2-phenethyl-pyridine Drug Info Ki = 1200 nM [527574]
2-Pyridin-3-yl-7-aza-bicyclo[2.2.1]heptane Drug Info Ki = 3.3 nM [527015]
1,1-Dimethyl-4-phenyl-piperazin-1-ium iodide Drug Info Ki = 1300 nM [527014]
1-(piperidin-4-ylmethyl)pyridin-2(1H)-one Drug Info Ki = 3600 nM [528157]
Carbachol Drug Info Ki = 728 nM [552407]
Tubocurarine Drug Info Ki = 7770 nM [552407]
(S)-3-(azetidin-2-ylmethoxy)-2-fluoropyridine Drug Info Ki = 180 nM [530178]
CYTISINE Drug Info Ki = 5.41 nM [528157]
CHOLINE Drug Info Ki = 18000 nM [527014]
3-((S)-Azetidin-2-yloxy)-5-iodo-pyridine Drug Info Ki = 47 nM [527014]
1-(piperidin-3-ylmethyl)pyridin-2(1H)-one Drug Info Ki = 4630 nM [528157]
References
Ref 527574Bioorg Med Chem Lett. 2005 Jul 1;15(13):3237-40.6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.
Ref 527015Bioorg Med Chem Lett. 2004 Apr 19;14(8):1889-96.Epibatidine structure-activity relationships.
Ref 527014Bioorg Med Chem Lett. 2004 Apr 19;14(8):1845-8.Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Ref 528157J Med Chem. 2006 May 4;49(9):2673-6.Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Ref 552407Receptor binding thermodynamics at the neuronal nicotinic receptor. Curr Top Med Chem. 2004;4(3):361-8.
Ref 552407Receptor binding thermodynamics at the neuronal nicotinic receptor. Curr Top Med Chem. 2004;4(3):361-8.
Ref 530178Bioorg Med Chem. 2009 Jul 1;17(13):4367-77. Epub 2009 May 15.Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.
Ref 528157J Med Chem. 2006 May 4;49(9):2673-6.Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Ref 527014Bioorg Med Chem Lett. 2004 Apr 19;14(8):1845-8.Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Ref 527014Bioorg Med Chem Lett. 2004 Apr 19;14(8):1845-8.Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Ref 528157J Med Chem. 2006 May 4;49(9):2673-6.Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.

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