| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T73724 | ||||
| Target Name | Neuronal acetylcholine receptor protein, beta-4 chain | ||||
| Target Type | Discontinued |
||||
| Drug Potency against Target | GCCSNPVCHLEHSNLC* | Drug Info | IC50 = 8 nM | [527644] | |
| (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol | Drug Info | IC50 = 8600 nM | [530946] | ||
| CYTISINE | Drug Info | Ki = 1560 nM | [529383] | ||
| HOMOEPIBATIDINE | Drug Info | Ki = 0.925 nM | [528394] | ||
| (2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol | Drug Info | IC50 = 8900 nM | [530946] | ||
| References | |||||
| Ref 527644 | J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. | ||||
| 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 529383 | Bioorg Med Chem Lett. 2008 Apr 1;18(7):2316-9. Epub 2008 Mar 6.Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine. | ||||
| 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 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. | ||||
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