Nanoscale carriers are of increasing interest for use in anticancer therapy because they can deliver drugs in a targeted way. Ideally, nanocarriers combine passive and active delivery mechanisms, by integrating targeting ligands on the surface of their stealth corona using simple and efficient conjugation chemistry. This feature article summarizes the conventional and newly explored conjugation chemistries that are used to bind ligands in organic nanoparticle systems, providing strategic guidance for the preparation of targeted nanocarriers.