Table 2:
Aromatic ring modifications of the PAP scaffold and MST-derived binding affinities between Rev1-CT and PAP analogues.
| Compound | R1 | R2 | Kd (μM)[a] |
|---|---|---|---|
| 1 | 2,3-difluorobenzene | N | 21 ± 1 μM |
| 2 | 2,3-difluorobenzene | C | 18 ± 4 μM |
| 3 | 2,3-dimethylbenzene | N | 32 ± 20 μM |
| 4 | 2,3-dimethylbenzene | C | 2.9 ± 0.4 μM |
| 5 | 3,4-dimethylbenzene | N | 17± 1 μM |
| 6 | 3,4-dimethylbenzene | C | 3.9 ± 0.2 μM |
| 7 | 3,4-naphthalene | N | 1.4 ± 0.1 μM |
| 8 | 3,4-naphthalene | C | 1.5 ± 0.2 μM |
| 9 | 2,3-naphthalene | N | 1.4 ± 0.1 μM |
[a]
Kd values and errors were calculated from three repeat experiments. Binding affinities that improved over 5-fold relative to 1 are boldened.