The development of biosensors for analytical purposes has attracted a great deal of attention in recent years. A biosensor is defined as an analytical device consisting of a biological component (e.g., enzyme, antibody, entire cell, DNA) and a physical transducer (e.g., electrode, optical device). Biosensors are mostly designed for routine analysis, such as clinical diagnosis, quality control of food, in-process control of fermentations, and in environmental analysis. Many of these sensors are also suitable for screening purposes in order to find new drugs. Such systems should yield information either about compounds with known bioactivity or about the bioactivity of samples with known or unknown chemical composition. Biosensors intended for the latter purpose are essentially based on whole cells carrying receptors and ion channels at their surfaces. Miniaturization of structures, primarily based on silicon, allows integration of many sensors into arrays, which may be suitable for the screening of natural and chemical products as well as combinatorial libraries. Until now, no commercially available sensors of this kind exist but they are expected in the near future. Different biosensors, based on enzymes, antibodies, cells, artificial membranes and entire animal tissues, which can be used in drug discovery and may lead to efficient screening systems in the future, are described in this review.