Structure-activity relationship (SAR) study designs

Structure-Activity Relationship (SAR) is perhaps the most important concept in drug development.

Medicinal chemists can “read” SAR like a travel guide.

Establishing SAR informs precisely those positions on a molecule where one can modify, to improve certain properties, including:

• solubility
• potency
• selectivity
• metabolic stability
• permeability
• toxicity
• pharmacokinetics
• tissue distribution
• in vivo efficacy

and distinguish these positions from others, where one cannot undertake such modifications.