BI 207127
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: Enzymatic assay with HCV NS5B polymerase D21 (SPA measuring 3H-UTP incorporation): IC50 = 19 nM |
| Selectivity within target family: > 30-fold | The human DNA polymerases alpha, beta and gamma and the Polio polymerase are not inhibited. |
| Selectivity outside target family | Eurofins SafetyScreen44 off-targets: CCKAR with 88 % inhibition, OPRD1 with 53 % inhibition |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: Cell-based replicon assay using RT-PCR for RNA quantification, genotype background 1a or 1b, Huh7 cells, 72 h incubation: EC50 = 23 nM for genotype 1a and EC50 = 11 nM for genotype 1b |
| Control compound (100 times less potent than the probe) | Enzymatic assay with HCV NS5B polymerase D21 (SPA measuring 3H-UTP incorporation) for BI-7656: IC50 > 5 µM |