AbstractMore and more studies report on the roles that galectins play in numerous types of cancer. These roles can be varied, as has been shown particularly for galectin‐3. These studies have created the need for inhibitors that can block unwanted effects, and the need to detect galectins in tissues, in order to better understand their role, and aid in diagnosis and prognosis. Since galectins bind β‐galactosides, monovalent galactose‐derived inhibitors have been prepared but also peptidic ones have appeared. Since galectins often induce crosslinking and partake in aggregation phenomena, multivalency has been a successful design element in inhibitor development. Currently, there are no cheap and convenient solutions available for the detection of, ideally multiple, galectins in tissue samples, although antibody‐based methods such as ELISA and Western blot analysis are being used. Besides these, a chemical probe‐based method also shows potential as an alternative.