Drug discovery relies on massive screening of compound libraries with in vitro cell-based target assays. These pharmacological screens have been well accepted. For in vitro toxicological screening, this privilege has only been obtained for the Ames, chromosomal aberration and eye irritation tests. At the moment, a number of cellular assays for cytotoxicity, genotoxicity, embryotoxicity, cellular metabolic activation processes and endocrine disruption await general acceptance. From that point onwards, tools will become available to identify unwanted pharmacological or toxicological effects at a much earlier stage in the drug development process.