| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T34429 | ||||
| Target Name | Neuronal acetylcholine receptor protein, alpha-7 chain | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | TOXIFERINE | Drug Info | IC50 = 9500 nM | [1] | |
| GCCSNPVCHLEHSNLC* | Drug Info | IC50 = 8 nM | [2] | ||
| ALCURONIUM | Drug Info | IC50 = 4100 nM | [1] | ||
| CYTISINE | Drug Info | Ki = 1420 nM | [3] | ||
| PH-709829 | Drug Info | Ki = 9 nM | [4] | ||
| CP-810123 | Drug Info | Ki = 16.4 nM | [5] | ||
| GCCSHPACAGNNQHIC* | Drug Info | IC50 = 1.1 nM | [2] | ||
| References | |||||
| REF 1 | J Med Chem. 2007 Sep 20;50(19):4616-29. Epub 2007 Aug 28.Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor. | ||||
| REF 2 | J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. | ||||
| REF 3 | Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97.3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. | ||||
| REF 4 | Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5. Epub 2008 May 1.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: in vitro and in vivo activity. | ||||
| REF 5 | J Med Chem. 2010 Feb 11;53(3):1222-37.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 agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models. | ||||
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