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Assay Method Information

Assay Name:  Inhibition Assay
Description:  The biological activity of the compounds of general formula (I) towards the cholinesterase inhibition was evaluated using Ellman's method (Ellman, G. L.; Courtney, K. D.; Anders, B.; Featherstone, R. M. Biochem. Pharmacol. 1961, 7, 88-95).This method of evaluation of the cholinesterase inhibitors activity is based on the fact that acetyl/butyrylcholinesterase interacts with the inhibitor, which prevents the acetyl/butyrylcholine hydrolysis. The inhibitor causes the enzyme activity drop which is dependent on the inhibitor concentration. The enzyme unbound with the inhibitor is able to hydrolyze acetyl/butyrylthiocholine (ASCh/BSCh). The amount of the hydrolyzed ASCh/BSCh is measured indirectly, by quantification of the product of its reaction with DTNB (5,5 -dithio-bis-2-nitrobenzoic acid). Ellman's method relies therefore on the spectrophotometric quantification of product of the reaction between acylthiocholine and DTNB.
Affinity data for this assay
 

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Last update November 1, 2007
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