Table 1.
Construct | Kd, nM | Ratio of Kd | pKi (L760735) | Ratio of Ki |
WT | 2.15 0.22 | 1.0 | 8.08 0.06 | 1.0 |
E193A | 3.64 0.37 | 1.7* | 7.66 0.05 | 2.6 |
Y196A | >10,000 | ND | ND | ND |
H197A | 2.94 0.38 | 1.4* | 7.76 0.05 | 2.1 |
H265A | 5.35 0.47 | 2.5 | 6.59 0.05 | 31 |
Y272A | 4.51 0.55 | 2.1 | 7.60 0.08 | 3.1 |
ND, not determined. Ratios of Kd and Ki are for mutants over WT values
These differences did not rise to statistical significance judged by one-way ANOVA with Dunnett’s posttest (compared with WT, P < 0.05).