Table 1. Biochemical and Cellular Data of Compounds (±)-13 and the Separated Enantiomers.
| compound |
||||
|---|---|---|---|---|
| biochemical assay type | enzyme | (±)-13 | NMS-P515 | (R)-13 |
| FP (KD, μM) | PARP-1 | <0.03a | <0.03a | 1.32 |
| PARP-2 | >10 | >10 | ||
| PARP-3 | >10 | >10 | ||
| TNKS-1 | >10 | >10 | ||
| SPR (Kd, μM) | PARP-1 | 0.016 | 1.76 | |
| compound |
||||
|---|---|---|---|---|
| cellular assay type | cell line | (±)-13 | NMS-P515 | (R)-13 |
| PAR (IC50, μM) | HeLa | 0.050 | 0.027 | 0.162 |
Assay sensitivity limit.