TABLE 1. Sensitivities and efficacies of ligand action at different nAChR subtypes.

⁸⁶Rb⁺ efflux assays were conducted as described in Methods and in the legends to Fig. 2–Fig. 5 for cells expressing the indicated nAChR subtypes and for the ligands listed in column 1. Agonism: Results for agonism were fit to the logistic equation to determine log molar EC₅₀ values (± SE; upper values) and efficacies (% ± SE relative to a fully efficacious concentration of carbamylcholine; lower values). Log molar IC₅₀ values (± SE; in parentheses) also are given for drugs with agonist activity also displaying self-inhibition. Inactivation: Results for inactivation of responses mediated by a standard agonist were fit to the logistic equation to determine log molar IC₅₀ values (± SE; upper values) and degree of function remaining at high ligand concentration (% ± SE relative to a fully efficacious concentration of carbamylcholine; lower values). Where efficacy or degree of inactivation values show no SE, they were constrained for curve fitting. ND – not determined. Please see Supplementary Data Table 1 for mean EC₅₀ or IC₅₀ values and Hill coefficients.

Drug	Agonism				Inactivation
	log M EC50 values (± SE)				log M IC50 values (± SE)
	(log M IC50 values (± SE) for self inhibition)
	% efficacy				% remaining function at high ligand concentration
	α4β2	α4β4	α3β4*	α1*	α4β2	α4β4	α3β4*	α1*
7	−8.23 ± 0.03	−7.60 ± 0.07	−6.47 ± 0.06	−5.65 ± 0.05	−8.32 ± 0.05	−7.54 ± 0.01	−6.22 ± 0.15	−5.61 ± 0.04
		(−4.60 ± 0.29)
	55 ± 1%	98 ± 5%	97 ± 4%	51 ± 3%	37± 2 %	−16 ± 1%	12 ± 11%	0%
16	−8.03 ± 0.02	−7.40 ± 0.10	−6.09 ± 0.04	−5.98 ± 0.02	−8.05 ± 0.03	−7.49 ± 0.01	−5.88 ± 0.07	−6.06 ± 0.04
	(−5.05 ± 0.55)	(−4.14 ± 0.52)	(−5.15 ± 0.03)	(−4.90 ± 0.03)
	52 ± 1%	114 ± 34%	43%	50%	41 ± 1%	−8 ± 1%	−2 ± 7%	0%
18	−7.53 ± 0.04	6.62 ± 0.04	≫ −5.0	−6.31 ± 0.05	−6.74 ± 0.18	−6.93 ± 0.04	−6.21 ± 0.09	−6.43 ± 0.05
	(−5.26 ± 0.05)	(−5.46 ± 0.55)		(−5.48 ± 0.07)
	43 ± 1%	97 ± 7%		7 ± 1%	0%	−8 ± 3%	−2 ± 7%	0%
13	−7.12 ± 0.08	−6.16 ± 0.07	≫ −5.0	≫ −5.0	−6.16 ± 0.24	−5.98 ± 0.05	−5.94 ± 0.11	−5.55 ± 0.08
		(−4.83 ± 0.15)
	28 ± 1%	52 ± 6%			20%	−15 ± 5%	6 ± 9%	0%
20	−7.13 ± 0.04	−6.48 ± 0.07	≫ −5.0	≫ −5.0	−6.24 ± 0.06	−6.66 ± 0.06	−6.10 ± 0.07	−6.12 ± 0.05
	(−5.15 ± 0.06)	(−5.32 ± 0.07)
	36 ± 2%	100 ± 11%			0%	−8 ± 4%	11 ± 5%	0%
10	−7.06 ± 0.08	−6.17 ± 0.07	≫ −5.0	≫ −5.0	−6.19 ± 0.12	−6.41 ± 0.05	−6.05 ± 0.04	−5.74 ± 0.02
		(−5.15 ± 0.05)
	25 ± 1%	76 ± 8%			20%	−7 ± 4%	5 ± 4%	0%
11	−6.97 ± 0.13	−5.72 ± 0.16	≫ −5.0	≫ −5.0	−5.26 ± 0.03	−5.91 ± 0.08	−5.39 ± 0.07	−4.83 ± 0.09
	6 ± 1%	105 ± 17%			0%	−9± 7%	0%	0%
1	−6.53 ± 0.05	ND	ND	ND	−6.37 ± 0.06	ND	ND	ND
	88 ± 2%				8 ± 2%
12	−6.42 ± 0.12	−6.50 ± 0.03	≫ −5.0	≫ −5.0	−5.34 ± 0.02	−6.39 ± 0.05	−6.08 ± 0.03	−6.07 ± 0.03
		(−5.50 ± 0.03)
	4 ± 1%	45%			0%	0 ± 4%	7 ± 3%	0%
26	≫ −5.0	≫ −5.0	≫ −5.0	≫ −5.0	≫ −5.0	ND	≫ −5.0	≫ −5.0
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