Answers are grounded in this paper and cite their sources.
An iterative analogue library synthesis strategy rapidly developed comprehensive SAR data for a novel series of M4 positive allosteric modulators (PAMs). This effort identified key moieties that improved microsomal stability and physiochemical properties. Moreover, this series displayed an order of magnitude greater potency for human versus rat M4, providing compounds with EC50 values in the 100 nM range.
No takes yet. Share an insight, caveat, or question.
Kennedy et al. (2009) studied this question.
Synapse has enriched 10 related papers. Consider them for comparative context: