Table 2. Selectivity Profile of OUL35 (3) and Its Analogues against a Panel of ARTs (μM IC50s) and Activity in the Cell-Based Assay (μM).
OUL35 (3)a | 8b | 9b | 10c | 11c | 12d | 15d | 16d | 17d | 18e | |
---|---|---|---|---|---|---|---|---|---|---|
PARP10 | 0.330 | 0.230 | 2.4 | 3.64 | 0.480 | 0.290 | 0.140 | 0.150 | 0.160 | 0.400 |
PARP15 | >10f | 3.3 | 1.2 | 11.0 | 1.7 | 2.4 | 0.400 | 0.400 | 0.370 | n.t.g |
PARP14 | 23 | 10 | 0.630 | >100 | 41 | ≫10 | ≫10 | ≫10 | ≫10 | 5.2 |
TNKS1 | >100 | >100 | n.t. | >100 | 21 | >100 | >100 | >100 | >100 | n.t. |
TNKS2 | >100 | >100 | >100 | >100 | 6.5 | >100 | >100 | >100 | >100 | n.t. |
PARP1 | >100 | >100 | n.t. | >100 | >100 | >100 | >100 | >100 | >100 | >100 |
PARP2 | >100 | >100 | >100 | 27 | 1.7 | 38 | >100 | >100 | >100 | n.t. |
cell-based assayh | 1.35 | 2 | n.t. | 1.7 | 1.8 | 0.59 | 1.5 | 1.6 | 0.95 | n.t. |