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.