Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T73724 | ||||
Target Name | Neuronal acetylcholine receptor beta-4 (CHRNB4) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol | Drug Info | IC50 = 8600 nM | [4] | |
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol | Drug Info | IC50 = 8900 nM | [4] | ||
CYTISINE | Drug Info | Ki = 1560 nM | [3] | ||
GCCSNPVCHLEHSNLC* | Drug Info | IC50 = 8 nM | [1] | ||
HOMOEPIBATIDINE | Drug Info | Ki = 0.925 nM | [2] | ||
References | |||||
REF 1 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. J Med Chem. 2005 Jul 28;48(15):4705-45. | ||||
REF 2 | Epibatidine isomers and analogues: structure-activity relationships. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. | ||||
REF 3 | Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2316-9. | ||||
REF 4 | Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. J Med Chem. 2010 Jun 24;53(12):4731-48. | ||||
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