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W545:Strelow:The Application Of Mechanism Of Action Studies For Enzyme In Early Drug Discovery

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The Application of Mechanism of Action Studies for Enzymes in Early Drug Discovery

John Strelow, Yan Zhai, Karen Huss, Chan-Hsin Chang, Nathan Fite, James McGee, Neal Roehm

Quantitative and Structural Biology, Eli Lilly and Company, Indianapolis, IN


Enzymatic mechanism of action (MoA) studies determine the binding location of an inhibitor relative to the substrate or cofactor used by the enzyme. In some cases, the kinetics can be evaluated to determine the residence time of the inhibitor on the enzyme. This information can provide important guidance for the selection and optimization of screening actives, hits, and leads with the highest probability of advancing to achieve clinical success. In this poster, we present our methodology for performing these studies in a consistent and robust manner for enzyme targets. We have used this methodology to perform over 1,600 MoA studies. We summarize our observations and their implications for the utility of enzymatic MoA studies in early drug discovery.

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