Table 1. DARC screening hits confirmed experimentally as inhibitors of Mcl-1.
The complete set of DARC hits (including those that did not inhibit Mcl-1) are included as Table S2. Ki values were determined via a fluorescence polarization competition assay (see Supplementary Methods), and then bio-layer interferometry was used to directly confirm binding to Mcl-1 (see Supplementary Results).
| Compound | Chemical structure | Ki (µM) | L.E. (kcal/mol•heavyatom) |
|---|---|---|---|
| M0 |  |
21 | 0.27 |
| M1 |  |
1.2 | 0.24 |
| M5 |  |
12 | 0.21 |
| M7 |  |
7 | 0.27 |