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. Author manuscript; available in PMC: 2014 Jan 15.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Dec 1;23(2):412–416. doi: 10.1016/j.bmcl.2012.11.092

Table 2.

Structures and activities of analogs 24a–k attached to the preferred biaryl.

graphic file with name nihms426569u2.jpg
Compd hM1 EC50 (μM)a AChmax (%)a,b pEC50a
24a graphic file with name nihms426569t1.jpg 5.6 44 ± 3 5.25 ± 0.07
24b graphic file with name nihms426569t2.jpg -
24c graphic file with name nihms426569t3.jpg >10 51 ± 3
24d graphic file with name nihms426569t4.jpg -
24e graphic file with name nihms426569t5.jpg 5.2 52 ± 3 5.29 ± 0.09
24f graphic file with name nihms426569t6.jpg >10 62 ± 2
24g graphic file with name nihms426569t7.jpg >10 53 ± 2
24h graphic file with name nihms426569t8.jpg 3.2 30 ± 2 5.49 ± 0.12
24i graphic file with name nihms426569t9.jpg >10 46 ±3
24j graphic file with name nihms426569t10.jpg >10 36± 2
24k graphic file with name nihms426569t11.jpg -
a

Values represent the mean ± standard error of the means of at least three independent determinations performed in triplicate.

“-” indicates an inactive compound showing no PAM activity up to the highest concentration tested (30 μM).

b

When hM1 EC50 is reported as >10, this value represents the percent maximal ACh response when the test compound was present at its highest concentration (30 μM).