TABLE 2.
EC50 and Hill constant values of mutant receptors containing unnatural amino acid at α135
| αPhe135 | ACh |
SuCh |
Efficacya | ||||
|---|---|---|---|---|---|---|---|
| EC50 | Hill constant | n | EC50 | Hill constant | n | ||
| μm | μm | ||||||
| Phe | 23 ± 0.2 | 1.5 ± 0.02 | 35 | 59 ± 1 | 1.3 ± 0.03 | 13 | 0.14 ± 0.01 |
| Pheb | 23 ± 0.4 | 1.5 ± 0.03 | 8 | NAc | NA | NA | NA |
| F-Phe | 2.6 ± 0.03 | 1.6 ± 0.02 | 7 | 32 ± 0.8 | 1.4 ± 0.04 | 9 | 0.54 ± 0.02 |
| F3-Phe | 1.0 ± 0.02 | 1.5 ± 0.05 | 15 | 8.1 ± 0.2 | 1.6 ± 0.05 | 8 | 0.86 ± 0.02 |
| Me-Phe | 1.0 ± 0.02 | 1.6 ± 0.04 | 12 | 11 ± 0.2 | 1.5 ± 0.04 | 11 | 0.82 ± 0.02 |
| Me2-Phe | 0.22 ± 0.01 | 1.6 ± 0.07 | 9 | 1.6 ± 0.06 | 1.5 ± 0.07 | 7 | 0.93 ± 0.04 |
| Cha | 16 ± 0.2 | 1.6 ± 0.02 | 15 | 60 ± 1 | 1.6 ± 0.03 | 9 | 0.10 ± 0.01 |
a Determined by the average of Imax(SuCh)/Imax(ACh).
b Data obtained by suppression mutation.
c NA, data not available.