Table 2.
Compounds | ka(M−1 s−1) | kd(s−1) | KD (nM) |
---|---|---|---|
DB2457 (7a) | 2.0 ± 0.2 × 106 | 0.0081 ± 0.001 | 4.1 ± 0.4 |
DB2708 (7c) | 3.5 ± 0.3 × 106 | 0.0150 ± 0.002 | 4.3 ± 0.3 |
DB2711 (7d) | 4.1 ± 0.3 × 106 | 0.0516 ± 0.004 | 12.6 ± 0.1 |
DB2715 (7f) | 4.6 ± 0.4 × 106 | 0.0444 ± 0.004 | 9.6 ± 0.4 |
DB2728 (7g) | 2.9 ± 0.1 ×106 | 0.0217 ± 0.001 | 7.4 ± 0.2 |
DB2764 (7h) | 1.8 ± 0.2 × 106 | 0.0198 ± 0.002 | 11.0 ± 0.2 |
DB2714 (7j) | 3.4 ± 0.2 × 106 | 0.0290 ± 0.002 | 8.5 ± 0.1 |
DB2740 (7m) | 2.3 ± 0.3 × 106 | 0.0078 ± 0.001 | 3.4 ± 0.3 |
DB2753 (7q) | 7.3 ± 0.2 × 104 | 0.0076 ± 0.001 | 104 ± 2 |
DB2712 (7t) | 2.6 ± 0.3×106 | 0.0180 ± 0.002 | 7.0 ± 0.2 |
Kinetics analysis was performed by global fitting with a 1:1 binding model. ka is the association rate constant, while kd is the dissociation rate constant. KD was calculated through global fitting of the kinetic data obtained for various concentrations of the compounds; KD is given by kd / ka. The kinetics errors are based on two independent experiments and the data fitting of different concentrations of compounds. The data of DB2457, DB2711, DB2714 and DB2740 are based on three independent experiments.