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IC50 values of Asinex hit compounds against MtbTopI and human topoisomerase I (hTOPI).
| Compound Number | Asinex ID | MtbTopI Relaxation Inhibition (IC 50 , µM) | hTOPI Relaxation Inhibition (IC 50 , µM) | Selectivity Score |
|---|---|---|---|---|
| 1 | SYN 12502158 | 15.6 | 93.75 | 6 |
| 2 | AOP 19767246 | 62.5 | >250 | >4 |
| 3 | ADD 15417014 | 62.5 | >250 | >4 |
| 4 | ADM 12439418 | 125 | >250 | >2 |
| 5 | LEG 11118762 | 250 | n.d. | n.d. |
| 6 | AEM 11113320 | 500 | n.d. | n.d. |
n.d. – not determined.
Selectivity Score = hTOPI IC50/MtbTopI IC50.
