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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