BI-2540
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: Enzymatic assay (HIV1 reverse transcriptase Picogreen Fluorescence Assay), WT: IC50 = 12 nM |
| Selectivity within target family: > 30-fold | N./A. BI-2540 is non selective against mutants; tested for different HIV strains. |
| Selectivity outside target family | Eurofins SafetyScreen44: No targets < 80 % Control @ 10 µM |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: HIV 1 luciferase assay with C8166 cells, WT: EC50 = 2.6 nM; HIV viral replication assay with C8166 cells, WT: EC50 = 0.76 nM |
| Control compound (100 times less potent than the probe) | BI-2439 has 420-fold lower activity: HIV1 reverse transcriptase Picogreen Fluorescence Assay: WT IC50 = 5053 nM |