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. Author manuscript; available in PMC: 2013 Jan 26.
Published in final edited form as: J Med Chem. 2012 Jan 4;55(2):812–823. doi: 10.1021/jm201301h

Table 4.

Potencies and efficacies of ligand agonism and inactivation of α3β4*-nAChRsa

Compound Agonism Inactivation Ki (nM)

EC50 (nM) Efficacy (%) IC50 (nM) Efficacy (%) α3β4
39 3400 120 > 3000 > 70 1270
43 1200 120 > 3000 > 70 692
44 > 3000 > 80 > 3000 > 30 8780
3 30000 90 ND ND 260
1 2200 110 ND ND ND
a

See Experimental Section and the legend to Table 3 for details.