Table 2.
Rate Constant | 4°C | 10°C | 15°C | 25°C | 30°C | 35°C |
---|---|---|---|---|---|---|
ak+ligand (µM−1·s−1) | 1.5 ± 0.1 | 2.5 ± 0.1 | 3.8 ± 0.1 | 7.6 ± 0.7 | 9.9 ± 0.6 | 12.8 ± 0.9 |
bk−ligand (s−1) | 1.7± 0.2 | 3.4 ± 0.4 | 5.6 ± 1.3 | 15.4 ± 3.2 | 22.2 ± 1.7 | 38.9 ± 2.5 |
1/Kligand (µM) | 1.1 ± 0.2 | 1.4 ± 0.2 | 1.5 ± 0.4 | 2.0 ± 0.5 | 2.2 ± 0.3 | 3.0 ± 0.6 |
bk+pocket (s−1) | 0.3 ± 0.1 | 1.3 ± 0.4 | 1.2 ± 0.3 | 1.3 ± 0.4 | 2.3 ± 1.0 | 2.0 ± 0.9 |
bk−pocket (s−1) | 0.7 ± 0.2 | 2.4 ± 0.6 | 3.3 ± 0.7 | 6.3 ± 1.1 | 9.7 ± 1.9 | 12.5 ± 2.6 |
Kpocket = kon /koff | 0.4 ± 0.2 | 0.5 ± 0.2 | 0.4 ± 0.1 | 0.2 ± 0.1 | 0.2 ± 0.1 | 0.2 ± 0.1 |
cKD overall (µM) | 0.8 ± 0.2 | 0.9 ± 0.2 | 1.1 ± 0.3 | 1.7 ± 0.4 | 1.8 ± 0.3 | 2.6 ± 0.5 |
dKD overall (µM) | 0.8 ± 0.1 | 1.0 ± 0.1 | 1.3 ± 0.1 | 1.3 ± 0.1 | 1.5 ± 0.1 | 1.7 ± 0.1 |