Table 1.
Compound | Sequence | PLK1 PBD FP IC 50 [μM] | PLK3 PBD FP IC 50[μM] | Selectivity Index |
---|---|---|---|---|
1 | LLCS[pT]PNGL | 0.17 ± 0.03 | >600 | >17,000 |
2 | LLCSTPNGL | >600 | ND | ND |
3 | Ac-PLHS[pT]PNGL | 0.06 ± 0.04 | 163.6 | 13,633 |
4 | Ac-PLHS[pT]AI | 0.064 ± 0.01 | 270.5 | 21,133 |
5 | Ac-LHS[pT]AI | 1.57 ± 0.47 | >600 | >1900 |
6 | Ac-PLHS[pT]A | 0.46 ± 0.12 | >600 | >6500 |
7 | GPLATS[pT]PKNG | 0.0057 ± 0.002 | 2.2 | 1928 |
8 | GPLATS[pT]PNGL | 0.011 ± 0.003 | 6.3 | 2864 |
9 | Ac-PLHS[pT]PKNG | 0.032 ± 0.012 | 133.8 | 20,906 |