BI 653048
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: NR3C1: IC50 = 55 nM (Fluorescence polarization assay) |
| Selectivity within target family: > 30-fold | Surpasses criterion: > 100 fold selectivity against related nuclear receptors (PGR, NR3C2, ESR1, AR) |
| Selectivity outside target family | 49 Eurofins-Panlabs targets at 10 µM – no hits; Clean PDSP scan |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: IL6: IC50 = 23 nM; IL6 maximal efficacy is 88% @ 2 µM |
| Control compound (100 times less potent than the probe) | Surpasses criterion: BI-3047 (enantiomer): NR3C1: IC50 >2 µM (Fluorescence polarization assay); Clean PDSP scan |