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BI-2540

2D structure
Target HIV NNRT 
Targeted domain Allosteric site adjacent to the polymerase active site
Mode of action Inhibitor
Control BI-2439
Recommended cellular usage concentration ≤ 100 nM
In vivo use Yes
Donated by Boehringer Ingelheim


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