We send this reference out to our clients and contacts more than any other paper. It describes the rationale, strategies and methodologies for in vitro pharmacological profiling at four major pharmaceutical companies (AstraZeneca, GlaxoSmithKline, Novartis and Pfizer), and illustrates, with examples of their impact, on the drug discovery process. For the first time there was a disclosed a list of proteins, that small molecule interaction has been linked to undesired side effects in patients. Such effects led to discontinuation of the drug at obvious high cost. The knowledge of this list, coupled with early in-vitro screening, is a must have for medicinal chemistry.
Reducing safety-related drug attrition: the use of in vitro pharmacological profiling.