ABSTRACT

The drug discovery process lies at the interface of biology and chemistry and can be divided into two main phases, namely the pre-clinical and the clinical phase. This chapter reviews the main processes in pre-clinical drug discovery, including target identification, assay development, compound screening, Hit identification and properties of a Lead series and Candidate compound. Compound screening activities of drug targets against compound libraries is now a mature and validated approach to identifying the chemical starting points of drugs. There are broadly two main screening types, namely phenotypic and target-based approaches. The most widely utilised method for the screening of biological targets considered to be suitable for therapeutic intervention in drug discovery efforts uses microtiter plate based assays that conform to the Society of Biomolecular Screening plate standard. The chapter also presents a summary of the attributes of a typical Lead compound.