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. Author manuscript; available in PMC: 2021 Jun 17.
Published in final edited form as: ChemMedChem. 2020 Apr 28;15(12):1058–1066. doi: 10.1002/cmdc.202000137

Table 2.

PLK PBD In vitro binding for FLIP compounds (Ncap-S[pT]PNGL)

graphic file with name nihms-1621665-t0006.jpg

Compound R1 PLK1 PBD FP IC50 [μM]

10 OH >600
11 OCH3 21.9 ± 4.3
12 OCH2CH3 15.9 ± 2.1
13 OCH2CH2CH3 10.4 ± 2.6
14 OCH2C6H4F 5.0 ± 0.86
15 OCH2CH2C6H5 4.5 ± 0.72
16 SCH3 3.0 ± 0.72
17 NCH3 11.2 ± 2.6
18 NCH2CH2CH3 5.4 ± 1.8
19 CH2CH2CH2CH3 2.5 ± 0.96