Table 1 Optimization of compound 1.

From: Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors

Compound

Structures

Inhibition % at 50 μM

IC50 (μM)

KD (μM)

1

48

50

Nd

2

25

nd

44  ±  6

3

28

nd

54 ± 5

4

57

45

41 ± 5

5

66

nd

43 ± 2

6

80

22

30 ± 2

  1. In vitro CK2 inhibition in the presence of compounds 1–6 at 50 μM was assayed with a CK2β-dependent peptide substrate as described in Experimental Procedures (SEM of two biological replicates derived from technical triplicates <20%). The KD values were determined by surface plasmon resonance (nd: not determined).
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