Table 6.
Cpd. | IC50 ±
(nM)a |
CLipE | ||
---|---|---|---|---|
DLD-1 | HT-29 | CTRPA A1309b | ||
6 | 63 ± 5.6 | 53 ± 2.3 | 122±6.5 | 6.68 |
22 | 4.8 ± 0.5 | 2±0.1 | 3.8 ± 0.7 | 6.86 |
29 | 3.2 ± 0.06 | 1.2 ± 0.07 | 6.9±0.8 | 7.02 |
30 | 3 ± 0.25 | 3 ± 0.05 | 2.8 ±0.03 | 7.04 |
32 | 4.5 ± 0.2 | 4±0.1 | 10.5 ± 0.3 | 7.94 |
33 | 2 ± 0.006 | 2 ± 0.004 | 0.7 ± 0.02 | 7.37 |
38 | 0.6 ± 0.02 | 0.5±0.1 | 0.8 ± 0.03 | 6.75 |
40 | 2.9 ± 0.34 | 2.2 ± 0.06 | 8.2±0.63 | 6.63 |
45 | 5 ± 0.07 | 4 ± 0.02 | 9.6 ± 0.3 | 5.37 |
46 | 3 ± 0.23 | 2.2±0.3 | 3.4 ± 0.7 | 6.25 |
47 | 0.03 ± 0.0001 | 0.9 ± 0.08 | 0.04 ± 0.002 | 8.32 |
48 | 2 ± 0.05 | 1.1 ± 0.04 | 3.2 ± 0.4 | 6.26 |
49 | 0.6 ± 0.01 | 0.45 ± 0.01 | 0.7 ± 0.05 | 6.79 |
51 | 0.96 ± 0.002 | 0.74 ± 0.03 | 1.2 ± 0.06 | 6.67 |
60 | 5 ± 0.06 | 6 ± 0.07 | 10.2 ± 0.8 | 5.81 |
61 | 2 ± 0.3 | 2 ± 0.07 | 1.6 ±0.3 | 6.36 |
81 | 1.6 ± 0.03 | 1.5 ± 0.03 | 3.4 ± 0.3 | 8.17 |
85 | 1.2 ± 0.03 | 0.8 ± 0.03 | 1.5 ±0.08 | 6.14 |
87 | 0.65 ± 0.002 | 0.34 ± 0.02 | 0.94 ±0.01 | 7.50 |
92 | 0.2 ± 0.03 | 0.12 ± 0.05 | 0.9±0.07 | 8.15 |
96 | 3 ± 0.04 | 2.1±0.07 | 3.4 ± 0.8 | 5.31 |
98 | 0.3 ± 0.002 | 0.2 ± 0.001 | 0.6 ± 0.003 | 6.69 |
108 | 3.5 ± 0.03 | 3 ± 0.2 | 4.3 ± 0.1 | 4.70 |
IC50 values represent the half maximal (50%) inhibitory concentration as determined in the CellTiter-Glo® (Promega) assay. Error represents SD (n = 3). All compounds were inactive when counter-screened against the HCT116 cell line with wild-type APC status (IC50 > 5 μM).
All compounds were inactive when counter-screened against the isogenic CTRPA cell line with wild-type APC status (IC50 > 5 μM).