Associating Cellular Effects with Target Enzyme Inhibition

Note These data highlight the need for making comparisons of inhibitor selectivity on the basis of dissociation constants, rather than IC50 values. 

5 ASSOCIATING CELLULAR EFFECTS WITH TARGET ENZYME INHIBITION 

The ultimate goal of lead optimization is to produce compounds that will elicit the desired cellular and organismal phenotype when dosed at appropriate concentrations. During the course of lead optimization activities it is common for pharmacologists to evaluate compounds not only using in vitro enzyme activity assays but also in cell-based assays as well. A question that often arises at this stage of drug discov- 

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