TABLE 1.

Functional activity and signaling bias of 16-Ethynyl SalA and 16-Bromo SalA in cAMP inhibition and β-arrestin recruitment assays.

	Inhibition of forskolin-induced cAMP accumulation			β-arrestin2 recruitment
Compound	EC50 (nM)	logEC50 ± SEM	Emax ± SEM	EC50 (nM)	logEC50 ± SEM	Emax ± SEM	Bias factor
U50,488	0.111	−9.96 ± 0.073	100	84.9	−7.07 ± 0.084	100	1
16-Bromo SalA	0.035	−10.5 ± 0.059****	98.8 ± 1.84	212	−6.67 ± 0.298	102 ± 13.7	7.7 G
16-Ethynyl SalA	0.011	−11.0 ± 0.082****	101 ± 1.79	7.35	−8.13 ± 0.076***	89.0 ± 2.2	1.0

***p < 0.001, ****p < 0.0001 for comparisons to U50,488, analyzed using one-way ANOVA with Bonferroni post-tests.