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. Author manuscript; available in PMC: 2014 Jul 22.
Published in final edited form as: J Med Chem. 2013 Dec 12;56(24):10103–10117. doi: 10.1021/jm401543h

Table 3.

Binding Affinity, Selectivity, and Antagonist Activity of Selected Individual Compoundsa

[3H]epibatidine binding
compd α3β4 Ki (nM) α4β2 Ki
(nM)		 selectivity
(fold)
(α3β4
Ki/α4β2 Ki)		 α4β2 antagonist
potency IC50 (nM)
207 61750 ± 36030 1587 ± 301 39 26320 ± 980
208 88895 ± 18005 3731 ± 237 24 5319 ± 346
301 56480 ± 8920 118 ± 2 478 514 ± 84
302 23765 ± 5345 323 ± 152 74 1465 ± 43
303 27550 ± 7150 433 ± 79 64 2820 ± 82
304 63320 ± 3560 307 ± 78 206 3024 ± 125
305 51893 ± 27353 2217 ± 1194 23 2953 ± 594
306 59678 ± 15253 340 ± 148 176 2830 ± 75
307 78085 ± 8355 611 ± 220 128 3405 ± 125
308 33353 ± 4373 257 ± 113 130 1686 ± 373
DHβE >10000 485 ± 33 >20 624 ± 24
a

Experiments were conducted a minimum of two times by methods described in Materials and Methods. Values shown are mean ± SEM for experiments conducted in triplicate at least twice.