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PLK PBD In vitro binding and cellular activity for FLIP compounds (Ncap-S[pT]PNGL)
| SCCP ID | Abbreviation | N Capping Group | PLK1 PBD FP IC50 [µM] |
PLK3 PBD FP IC50 [µM] |
Apoptosis @ 24hr, 30 µM |
Aberrant mitoses, @ 24hr, 30 µM |
|---|---|---|---|---|---|---|
| 5594 | 1G1-S[pT]PNGL |  |
350 | ND | ND | ND |
| 5598 | 1G2-S[pT]PNGL |  |
320 | ND | ND | ND |
| 5603 | 1G3-S[pT]PNGL |  |
250 | ND | ND | ND |
| 5756 | 2G1-S[pT]PNGL |  |
99 | ND | ND | ND |
| 5788 | 3G1-S[pT]PNGL |  |
16.5 | >600 | 36.2% | 47.9% |
| 5827 | 3G2-S[pT]PNGL |  |
8.6 | >600 | 55.5% | 53.8% |
| 5743 | Ac-PLHS[pT]A | - | 2 | >600 | 34.0% | 40.3% |
