Table 2.
EC50 values, that is the concentration of MetJ monomer required to promote half-maximal formation of its complex with the F-metC DNA, in the presence of ligands (see Scheme 3 and Fig. 2); improvements in the activity of bivalent ligands relative to a monovalent control are shown
| Compound | EC50 (nM) | Fold-improvement over monovalent control 4 |
|---|---|---|
| 4 | 1000 ± 100 | — |
| 15a (n = 2) | 110 ± 6 | 9.1-fold |
| 15b (n = 4) | 76 ± 2 | 13-fold |
| 18a (n = 2) | 700 ± 50 | 1.4-fold |
| 18b (n = 3) | 320 ± 40 | 3.1-fold |
| 18c (n = 4) | 220 ± 20 | 4.5-fold |
| 18d (n = 6) | 47 ± 1 | 21-fold |
The concentration of the ligands was 2 mM and the concentration of F-metC was 10 nM. EC50 values were determined based on an average of three titrations, fitted to a sigmoidal growth logistic model (see Supplementary data).