The druggable genome

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An assessment of the number of molecular targets that represent an opportunity for therapeutic intervention is crucial to the development of post-genomic research strategies within the pharmaceutical industry. Now that we know the size of the human genome, it is interesting to consider just how many molecular targets this opportunity represents. We start from the position that we understand the properties that are required for a good drug, and therefore must be able to understand what makes a good drug target.

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Figure 1: Drug-target families.
Figure 2: Number of drug targets.
Figure 3: Novel drug launches.
Figure 4: Marketed small-molecule drug targets by biochemical class.
Figure 5: Exploitation of the genome, as measured by known leads.


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We are indebted to J. P. Overington (Inpharmatica, London), A. Alex and L. Beeley for their contributions to the ideas on the physico-chemical limits for protein-binding sites. We also thank R. W. Spencer and C. Lipinski (Pfizer, Groton, Connecticut, USA) for much stimulating discussion.

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Correspondence to Colin R. Groom.

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Protein Data Bank

Proteome Analysis Database

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