Table 1.
Dissociation Constants (Kd) Measured by SPR and G-Quadruplex Stabilization (ΔTm) Potential by FRET-Melting
| DNA | 1a | 1b | 1c | 1d | 1e | 1f |
|---|---|---|---|---|---|---|
| Kd [μM] | ||||||
| c-kit2 | 3 ± 0.5 | 5.8 ± 2.3 | 9.2 ± 1.5 | 9.7 ± 0.8 | 2.8 ± 0.5 | 7.7 ± 0.2 |
| c-kit1 | 6.4 ± 0.1 | 9.1 ± 2.3 | 21 ± 2 | 31 ± 1 | 4.9 ± 0.3 | 13.7 ± 1 |
| htelo | 43 ± 3 | 8.6 ± 2 | 69 ± 7 | b | 21 ± 1 | 63 ± 2 |
| ds | nd17 | nd17 | nd17 | nd17 | nd17 | nd17 |
| ΔTm at 1 μM (°C) | ||||||
| c-kit2 | 18 | 17.5 | 5.4 | nda | 17.2 | 14 |
| c-kit1 | 25.3 | 24.6 | 11 | nda | 27.1 | 13.7 |
| htelo | 19.1 | 19.3 | 7 | nda | 15.5 | 15.4 |
| ds | 0 | 0 | 0 | nda | 0 | 0 |
| G-Quadruplex Binding Discrimination (Fold) | ||||||
| c-kit2/ c-kit1/htelo |
1/2/14 | 1/2/2 | 1/2/8 | 1/3 | 1/2/7 | 1/2/9 |
a
Not determined (nd) due to intrinsic fluorescence of ligand.
b
No detectable binding was observed; SPR standard deviations are given for two independent experiments; ΔTm ± 1 °C.