Target Validation Information
Target ID T84040
Target Name Transient receptor potential cation channel subfamily A member 1
Target Type
Successful
Drug Potency against Target 2-methyl-1-(pyridin-3-yl)pent-1-en-3-one oxime Drug Info IC50 = 17000 nM
2-methyl-1-(pyridin-4-yl)pent-1-en-3-one oxime Drug Info IC50 = 8610 nM
2-methyl-1-(thiophen-2-yl)pent-1-en-3-one oxime Drug Info IC50 = 11000 nM
2-methyl-1-(thiophen-3-yl)pent-1-en-3-one oxime Drug Info IC50 = 1320 nM
AMG-9090 Drug Info IC50 = 7 nM
AMG-2504 Drug Info IC50 = 105 nM
AMG-7160 Drug Info IC50 = 28 nM
AP18 5 Drug Info IC50 = 4500 nM
AMG-5445 Drug Info IC50 = 29 nM
3-Methyl-4-phenylbut-3-en-2-one oxime Drug Info IC50 = 2700 nM [530546]
References
Ref 530546Bioorg Med Chem Lett. 2010 Jan 1;20(1):276-9. Epub 2009 Oct 30.Oxime derivatives related to AP18: Agonists and antagonists of the TRPA1 receptor.

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