The Drug-Discovery Process cannot be

1 The Drug-Discovery Process cannot be Simplified to a Single Blueprint 

The ability to generate large collections of compounds and evaluate them for activity is a positive feature that cannot be underestimated. Instead of collecting data on 

4 Combinatorial Chemistry is about Making the Compounds that Fit Your Needs, not How They are Made 

In the synthesis of combinatorial libraries, there is a raft of tactical issues that need to be tackled. Will the library be made of mixtures or discrete compounds Prepared by solid-phase or solution-phase Screened in solution or attached to beads What level of purification and characterization is needed Will hits be identified by deconvolution, encoding techniques, or other means These are aU crucial operational aspects of combinatorial chemistry but it is equally important not to concentrate on them to the extent of missing the big picture. At the end of the day, neither a biological assay nor a medicinal chemist care how a compound was made. It is vital, though, that the tactical decisions do not prevent one from making the right compounds. Combinatorial synthesis is a means to an end, not an end in itself. 

SpaUer, M.T. Burger, M. Fardis and P.A. Bartlett, Curr. Opin. Chem. Biol, 1997,1, 47-53. 

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