Table 2. IC50 / EC50 in μM for selected compounds across phenotypic assay modules.
| Module a | Compound | Anti-Angio | G2/M | GLP1sec. | Ins.sec. | Wntpot. | Colo320 viab. | DLD-1 viab. | HCT-116viab. | HT-29 viab. | RKO viab. | SNU-C1 viab. | SW480 viab. | HCT-116 (GSK3β) viab. |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Wnt | methotrexate | 20 b | 20 | 20.1 | 20.1 | 0.012 | 0.001 | 0.70 | 0.001 | 0.001 | 0.001 | 20 | 0.001 | 0.001 |
| pyrimethamine | 20.1 c | 20 | 20.1 | 20.1 | 0.068 | NA | 20 | 18.2 | NA | NA | NA | 12.5 | 20 | |
| nolatrexed | 7.4 | 20 | 20.1 | 20.1 | 0.24 | 20 | 20 | 3.5 | 4.7 | 0.34 | 20 | 2.2 | 0.83 | |
| trimetrexate | 4.4 | 20 | 20.1 | 20.1 | 0.003 | 0.39 | 0.20 | 0.023 | 0.021 | 0.003 | 5.1 | 0.059 | 0.004 | |
| raltitrexed | 0.35 | 20 | 20.1 | 20.1 | 0.004 | 20 | 20 | 0.004 | 20 | 0.003 | 20 | 0.001 | 0.002 | |
| metoprine | 20.1 | 20 | 20.1 | 20.1 | 0.030 | 2.0 | 0.63 | 0.41 | 0.93 | 0.12 | 2.2 | 0.51 | 0.059 | |
| dasatinib | 20 | 20 | 20.1 | 20.1 | 0.007 | NA | 3.5 | 11.9 | NA | NA | NA | 7.0 | 20 | |
| rotenone | 0.026 | 0.31 | 20.1 | 20.1 | 0.25 | NA | 0.35 | 1.2 | NA | NA | NA | 0.16 | 0.067 | |
| Insulin | glibenclamide | 20.1 | NA | 20.1 | 0.002 | 20.1 | NA | 20 | 20 | NA | NA | NA | 2.9 | 20 |
| glimepiride | 20.1 | NA | 20.1 | 0.004 | 20.1 | NA | 20 | 20 | NA | NA | NA | 20 | 20 | |
| gliquidone | NA | NA | NA | 0.23 | 20.1 | NA | 5.1 | 10.1 | NA | NA | NA | 5.5 | 7.0 | |
| gliclazide | 20.1 | 20 | 20.1 | 1.8 | 20.1 | NA | 20 | 20 | NA | NA | NA | 20 | 20 | |
| repaglinide | 20.1 | 20.1 | 20.1 | 0.030 | 20.1 | NA | 20 | 20 | NA | NA | NA | 20 | 20 | |
| amitriptyline | 20.1 | 20 | 20.1 | 3.0 | 20.1 | NA | 20 | 20 | NA | NA | NA | 10.1 | 20 | |
| butriptyline | 20.1 | 20 | 20.1 | 3.6 | 20.1 | NA | 8.1 | 6.2 | NA | NA | NA | 7.8 | 20 | |
| metitepine | 20 | 20 | 20.1 | 2.9 | 20 | NA | 4.4 | 3.8 | NA | NA | NA | 1.9 | 4.6 | |
| propafenone | 20.1 | 20 | 20.1 | 4.9 | 20.1 | NA | 20 | 20 | NA | NA | NA | 20 | 20 | |
| etafenone | 20.1 | 20 | NA | 3.9 | 20.1 | NA | 20 | 11.2 | NA | NA | NA | 16.9 | 20 | |
| mebeverine | 20.1 | 20 | 20.1 | 2.0 | 20.1 | NA | 20 | 20 | NA | NA | NA | 20 | 20 | |
| Angio | semaxanib | 1.6 | 9.1 | 20.1 | 20.1 | 20.1 | NA | 20 | 20 | NA | NA | NA | 19.7 | 20 |
| vatalanib | 0.11 | 20 | 20.1 | 20.1 | 20.1 | NA | 20 | 20 | NA | NA | NA | 19.5 | 10.5 | |
| axitinib | 0.001 | 20 | 20.1 | 20.1 | 20.1 | NA | 4.5 | 16.8 | NA | NA | NA | 5.1 | 20 | |
| pazopanib | 0.047 | 20 | 20.1 | 20.1 | 20.1 | NA | 20 | 20 | NA | NA | NA | 5.7 | 20 | |
| sunitinib | 0.025 | 20 | 20.1 | 20 | 20.1 | NA | 1.6 | 2.3 | NA | NA | NA | 2.8 | 0.36 | |
| cetaben sodium | 0.37 | 20 | 20.1 | 20.1 | 20.1 | NA | 10.6 | 20 | NA | NA | NA | 4.4 | 7.4 | |
| KRAS | PD-184352 | 0.37 | 20 | 20.1 | 20.1 | 20.1 | 0.85 | 2.2 | 0.002 | 0.026 | 0.003 | 0.017 | 0.005 | 0.97 |
| bortezomib | 0.004 | 20 | 20.1 | 20.1 | 0.001 | 2.8 | 0.006 | 0.004 | 0.003 | 0.008 | 0.003 | 0.005 | 0.002 | |
| carfilzomib | 0.020 | 20 | 20.1 | 20.1 | 0.015 | 0.14 | 0.007 | 0.006 | 0.003 | 0.004 | 0.001 | 0.008 | 0.002 | |
| simvastatin | 1.5 | 20 | 3.3 | 20.1 | 20.1 | 4.9 | 20 | 20 | 20 | 20 | 20 | 5.9 | 4.7 | |
| cerivastatin | 0.089 | 20 | 20.1 | 20.1 | 19.9 | 1.9 | 2.5 | 0.24 | 1.2 | 1 | 1.9 | 0.14 | 0.053 | |
| fluvastatin | 0.98 | 20 | 20.1 | 20.1 | 20.1 | 13.0 | 20 | 0.97 | 20 | 19.2 | 20 | 1.7 | 0.040 |
a the module in which compound exhibits activity; only the IC50 value in the primary assay (or most potent of multiple primary assays) is shown; all compounds meet the selectivity criteria described in the methods.
b values shown as 20 indicate that the compound was tested in concentration-response and showed no response at the highest concentration tested (e.g. IC50 > 20 μM).
c values shown as 20.1 indicate that compound was inactive in single concentration testing and not advanced to concentration-response profiling. Refer to S2 Table for the full list of 173 actives and S4 Table and S5 Table for the complete results from concentration-response and single-concentration testing, respectively.