Abstract
Compound library derived from solution-phase synthesis via amide or 1,3-dipolar cycloaddition coupled with an in-situ enzymatic screening has yielded a fast discovery of several potent inhibitors. Novel compounds against hydrolases including exo- and endo hydrolases and transferases has been found by using the probing substrates such as chromophore-, fluorophore- and FRETtagged compounds, or indirect sensing methods such as fluorescence. The dilution method minimize the disturbing effects arisen from residual reagents thereby making the assay attractive to the medicinal chemistry. Aspects regarding chemical reaction, solvent effect, and probing methods are briefly reviewed.