Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T63967 Target Info
Target Name Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2)
Synonyms
CHRN; nAChR
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Target Type Successful Target
Gene Name CHRNA4-CHRNB2
Biochemical Class Neurotransmitter receptor
UniProt ID
ACHA4_HUMAN; ACHB2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Neuronal acetylcholine receptor alpha-3/beta-4 (CHRNA3/B4) Successful Target
UniProt ID ACHA3_HUMAN-ACHB4_HUMAN
Gene Name CHRNA3-CHRNB4
Synonyms
Neuronal acetylcholine receptor
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Representative Drug(s) Varenicline Drug Info Ki = 74.7 nM Click to Show More [1]
2 Varenicline Drug Info Ki = 240 nM [2]
Co-Target Name Neuronal acetylcholine receptor alpha-7 (CHRNA7) Successful Target
UniProt ID ACHA7_HUMAN
Gene Name CHRNA7
Synonyms
Nicotinic acetylcholine receptor subunit alpha 7; Nicotinic acetylcholine receptor alpha7; CHRNA7; Alpha7 nicotinic receptor; Alpha7 nAChR; Alpha-7 nAChR; Alpha(7) nicotinic receptor
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Representative Drug(s) Varenicline Drug Info Ki = 125 nM [1]
Co-Target Name Neuronal acetylcholine receptor alpha4/beta4 (CHRNA4/CHRNB4) Co-Target
UniProt ID ACHA4_HUMAN; ACHB4_HUMAN
Gene Name CHRNA4; CHRNB4
Representative Drug(s) Varenicline Drug Info Ki = 110 nM [3]
Co-Target Name Acetylcholine receptor alpha-1/beta-1/delta/gamma (CHRNA1/CHRNA1/CHRND/CHRNG) Co-Target
UniProt ID ACHA_HUMAN-ACHB_HUMAN-ACHD_HUMAN-ACHG_HUMAN
Gene Name CHRNA1-CHRNB1-CHRND-CHRNG
Representative Drug(s) Varenicline Drug Info EC50 ~ 1000 nM [3]
References  Top
REF 1 A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4749-52.
REF 2 Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005 May 19;48(10):3474-7.
REF 3 Discovery of highly potent and selective alpha4beta2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II. J Med Chem. 2012 Nov 26;55(22):9998-10009.

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