STAGES OF DRUG DISCOVERY-IDENTIFICATION OF LEAD
A chemical lead is defined as a synthetically stable, feasible, and drug like molecule active in primary and secondary assays with acceptable specificity, affinity and selectivity for the target receptor. This requires definition of the structure activity relationship as well as determination of synthetic
feasibility and preliminary evidence of in vivo efficacy and target engagement. Characteristics of a chemical lead are: SAR defined Drug ability (preliminary toxicity, hERG) Synthetic feasibility Select mechanistic assays In vitro assessment of drug resistance and efflux potential Evidence of in vivo efficacy of chemical class PK/Toxicity of chemical class known based on preliminary toxicity or in silico studies In order to decrease the number of compounds that fail in the drug development process, a drug ability assessment is often conducted.
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