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Enzymes generally make excellent targets for small molecule ligand discovery because

  • they are pre-organized to carry out a reaction and thus have destabilizing unsatisfied residues that are available for ligand binding
  • there is often a chemical starting point available in the form of the endogenous ligand
  • there is hope that interfering with catalysis will have an effect because a bound ligand directly competes with the natrual substrate.

Back to targets.