TABLE 1.
Inhibitors identified in the HTS
Small Molecule | Mol. Wt. | cLog P | No. Relative Compounds | First HTS Assay | Second HTS Assay | IC50 | ΔFID, DNA binding |
---|---|---|---|---|---|---|---|
μM | % | ||||||
AR01 | 245.274 | 3.7 | 1 | 74 | 70 | 1.7 ± 0.3 | 8 |
AR02 | 278.348 | 5.3 | 10 | 54 | 40 | 6.4 ± 1.1 | 9.60 |
AR03 | 237.3 | 3.7 | 60 | 58 | 2.1 ± 0.1 | 12.80 | |
AR04 | 350.414 | 4.8 | 1 | 58 | 45 | 14.9 ± 8.4 | <15 |
AR05 | 351.379 | 2.4 | 75 | 85 | 6.6 ± 0.9 | <15 | |
AR06 | 262.692 | 2.7 | 1 | 52 | 44 | 1.6 ± 0.1 | 3.10 |
AR07 | 400.534 | 5.3 | 12 | 80 | 41 | ∼100 | <15 |