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BI 207127

2D structure
Target HCV NS5B 
Targeted domain Pocket 1 of the thumb domain
Mode of action Inhibitor
Control BI-7656
Recommended cellular usage concentration ≤ 100 nM
In vivo use Yes
Synonyms Deleobuvir
Donated by Boehringer Ingelheim


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