Universiteit Leiden

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Division of Drug Discovery & Safety

Affinity

Designing and synthesizing high-affinity ligands for a given drug target have always been among the more important challenges in the drug discovery process.

We have done that routinely over the years and have been successful on many occasions. It does make sense to have high affinity, next to other design criteria. Administering, as a consequence, low amounts of compound to a patient is often beneficial in terms of side effects, and particularly in metabolic load. Interestingly, compounds with super-high affinity (that is subnanomolar affinity) are rare, and we’re proud that we’ve managed to develop a few for adenosine and cannabinoid receptors (see Figure for a few representative examples).

Related publications

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