Table 2.

Binding properties of ARBs for various mutants of N111G‐AT₁ receptors

	Candesartan		Telmisartan		Eprosartan
Mutation	Ki (nM)	ΔKi	Ki (nM)	ΔKi	Ki (nM)	ΔKi
N111G	1.4 ± 0.5	1	38.8 ± 4.9	1	44.1 ± 6.1	1
N111G/V108I	119 ± 19.0	85	627 ± 114	16.2	353 ± 36.4	8
N111G/S109T	281 ± 57.5	201	268 ± 27.6	6.9	124 ± 17.1	2.8
N111G/A163T	15.6 ± 4.9	11.1	4.0 ± 0.1	0.1	102 ± 10.5	2.3
N111G/E173A	1.3 ± 0.2	0.9	51.4 ± 3.6	1.3	46.9 ± 8.0	1.1
N111G/F182A	1.7 ± 0.6	1.2	11.1 ± 2.1	0.3	59.1 ± 10.1	1.3
N111G/Y184A	1.2 ± 0.08	0.9	17.6 ± 2.8	0.5	87.4 ± 14.9	2.0
N111G/K199A	148 ± 3.4	106	202 ± 11.6	5.2	334 ± 45.9	7.6
N111G/K199Q	82.1 ± 11.3	58.6	205 ± 46.4	5.3	446 ± 91.1	10.1
N111G/H256A	0.8 ± 0.2	0.6	47.0 ± 14.7	1.2	1262 ± 87	28.6
N111G/Q257A	4.8 ± 0.7	3.4	66.0 ± 13.5	1.7	8061 ± 648	183
N111G/Q257E	10.9 ± 5.3	7.8	258 ± 44.1	6.6	975 ± 284	22.1
N111G/Y292A	0.005 ± 0.001	0.004	0.7 ± 0.2	0.02	44.7 ± 11.6	1
N111G/N295A	6.7 ± 0.08	4.8	193 ± 30.9	5	360 ± 20.7	8.2
N111G/S109T/A163T	310.0 ± 21.4	221	150 ± 15.5	3.9	153 ± 8.8	3.5
N111G/S109T/H256A	168 ± 5.8	120	166 ± 24.7	4.3	1737 ± 258	39.4
N111G/S109T/N295A	1274 ± 139	1231	449 ± 41.2	11.6	494 ± 95	11.2
N111G/A163T/H256A	45.6 ± 17.5	32.6	19.0 ± 6.1	0.5	1410 ± 288	32
N111G/A163T/N295A	20.2 ± 4.4	14.4	6.9 ± 1.8	0.2	541 ± 105	12.3
N111G/K199Q/H256A	240 ± 5.5	171	209 ± 4.8	5.4	31 631 ± 728	717
N111G/H256A/N295A	0.06 ± 0.02	0.04	19.5 ± 0.9	0.5	612 ± 49.2	13.9

Ligand‐binding properties of various mutants of N111G‐AT₁ receptors. Values are presented as mean ± SEM of at least three independent experiments performed in duplicate. The effect of the mutations on the binding affinity is expressed as ΔK_i = K_i (mutant)∕K_i (N111G‐AT₁ receptor).