Fig. 1: RXFP2 agonist screening and SAR study.
From: Discovery of small molecule agonists of the Relaxin Family Peptide Receptor 2
a Schematic representation of SAR study showing the initial hit and active enantiomer configuration that led to the final 4 compounds, including the lead compound 6641. b Ranking of the RXFP2 agonist activity by HTRF cAMP assay in HEK-RXFP2 cells. The cAMP response induced by the compounds was normalized to the cAMP response induced by 100 nM INSL3 as 100% efficacy and the cAMP response induced by DMSO vehicle as 0% efficacy. Emax and EC50 were calculated using four parameter nonlinear fit dose-response stimulation curves. Results are expressed as mean ± SEM of 3 independent experiments. aThe EC50 is expressed in micromolar and is the concentration necessary to reach 50% of maximum cAMP signal. Molecular weight (MW).
