Services

Consulting in the area of Lead Discovery

The progression HTS hits → HTS actives → lead series → drug candidate → launched drug has shifted the focus from good quality candidate drugs, to good quality leads [3-5].

The screening attrition rate in the current pharmaceutical discovery protocol suggests that one marketed drug emerges from approximately 1 million HTS screened compounds. The estimates in the figure are illustrative, as exact figures are difficult to average across entire industry.

The ChemGPS projection for 176 leads (red), 186 “leadrugs” (yellow) and 532 drugs (blue), illustrates the overlap between these three categories. “Leadrugs” are chemicals that are both launched drugs, and chemical leads.

Using extensive knowledge related to the nature of chemical leads [3-5], as well as on methods related to the simultaneous optimization of pharmacokinetic and pharmacodynamic properties [6, 7], SMDL can assist with the choice of high quality leads. Contact us for more information.