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