. Author manuscript; available in PMC: 2016 May 23.

Published in final edited form as: J Med Chem. 2013 Nov 11;56(22):9045–9056. doi: 10.1021/jm400904m

Table 2.

SAR of analogs in position one.



R	#	cAMP IC₅₀ µM	Ca²⁺ IC₅₀ µM	ERK IC₅₀ µM
	7	1.7 ± 0.1	0.051 ± 0.008	0.030 ± 0.006
	20a	1.3 ± 0.0	0.032 ± 0.005	0.016 ± 0.001
	20b	2.1 ± 0.2	0.073 ± 0.023	0.016, 0.063^b
	20c	2.1 ± 0.0	0.080 ± 0.013	0.013, 0.028^b
	20d	0.11 ± 0.01	0.0016, <0.0005^a	0.0035, <0.0005^a
	20e	0.045 ± 0.000	0.00096 ± 0.00023	0.0013 ± 0.0007
	20f	0.94 ± 0.08	0.0011, < 0.0005^a	0.015 ± 0.000
	20g	0.71 ± 0.00	0.013 ± 0.002	0.0062 ± 0.0007

The cAMP and Ca²⁺ assay activity is the mean IC₅₀ with SD from two separate experiments, each ran in duplicate. The ERK assay is the mean IC₅₀ with SD from one experiment run in duplicate.

The two replicate IC₅₀s are reported here, one (<0.5 nM) being less than that could be detemined accurately by the assay.

Both IC₅₀ values are reported here as we feel that the standard deviation between the replicates is significant.