Melting temperature (Tm) shift calculated with a DSF assay and kinetic constants calculated from SPR.
| Compound | Aveg. Tm (°C) | apo-BMX Tm (°C) | ΔTm (°C) | k on/M−1 s−1 | k off/s−1 | K D/M |
|---|---|---|---|---|---|---|
| BMX-IN-1 | 60.17 ± 0.32 | 52.13 ± 0.11 | 8.04 ± 0.32 | 7.4 × 103 | 5.10 × 10−4 | 6.9 × 10−8 |
| JS24 | 63.57 ± 0.01 | 52.23 ± 0.06 | 11.34 ± 0.01 | 1.4 × 105 | <1 × 10−4 | Nda |
| JS25 | 61.43 ± 0.48 | 52.13 ± 0.11 | 9.30 ± 0.48 | 5.4 × 104 | <1 × 10−4 | Nda |
| JS26 | 61.47 ± 0.21 | 52.13 ± 0.11 | 9.34 ± 0.21 | 7.2 × 104 | <1 × 10−4 | Nda |
| JS27 | 62.94 ± 0.06 | 52.13 ± 0.11 | 10.81 ± 0.06 | 9.9 × 104 | <1 × 10−4 | Nda |
a
K D not measured due to very prolonged off-rates (outside instrument specifications).