Table 1.
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 2 and Fig. 3); improvements in the activity of bivalent ligands relative to a monovalent control are shown
| Compound | EC50 (nM) | Fold-improvement over monovalent control (11 or 12) |
|---|---|---|
| SAM, 1 | 17.3 ± 0.3 | — |
| 11 | 120 ± 10 | — |
| 9a | 61 ± 3 | 2.0-fold |
| 9b | 37 ± 2 | 3.2-fold |
| 9c | 39 ± 1 | 3.1-fold |
| 9d | 75 ± 4 | 1.6-fold |
| 9e | 111 ± 5 | 1.1-fold |
| 12 | 36 ± 6 | — |
| 10a | 15 ± 5 | 2.4-fold |
| 10b | 10 ± 1 | 3.6-fold |
The concentration of the monovalent ligands 11 and 12 was 2 mM, and the concentration of the bivalent ligands 9 and 10 was 1 mM. The concentration of F-metC was 10 nM, and the final concentration of DMSO was 2%. EC50 values were determined based on an average of three titrations, fitted to a sigmoidal growth logistic model (see Supplementary data).