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. Author manuscript; available in PMC: 2015 Jan 15.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Nov 28;24(2):674–678. doi: 10.1016/j.bmcl.2013.11.049

Table 1.

SAR of the 3-pyridinyl group of NS9283

Analogue Structure PAM(Y or N)a EC50 (uM) Emaxb
1a graphic file with name nihms551756t1.jpg Y 0.79±0.2 1
1b graphic file with name nihms551756t2.jpg N — —
1c graphic file with name nihms551756t3.jpg N — —
1d graphic file with name nihms551756t4.jpg N — —
1e graphic file with name nihms551756t5.jpg N — —
a

PAM: Positive Allosteric Modulator for α4β2α5.

Y (for yes): 1 µM compound potentiates EC20–30 nicotine >50%;

N (for no): 1 µM compound potentiates EC20–30 nicotine <50%. Average of n = 2;

b

Maximum efficacy relative to NS9283.