TABLE 3

Side chain mutations to putative ligand-contacting residues of the binding site’s complementary face

Full data, including error estimates, are reported in Supplemental Table 2.

	Acetylcholine		Epibatidine		Varenicline
	EC₅₀	Fold Shift	EC₅₀	Fold Shift	EC₅₀	Fold Shift
	μM		μM		μM
wt	99		0.34		2.0
W55A	130	1.4	5.8	17	68	34
L109A	300	3.1	0.28	1/1.2	0.53	1/3.8
Q117A	180	1.8	0.90	2.6	4.9	2.4
L119A	210	2.1	3.2	9.4	41	21

wt, wild-type.