Menu

BI 653048

2D structure
Target NR3C1 
Targeted domain Ligand binding domain
Mode of action Agonist
Control BI-3047
Recommended cellular usage concentration 1 µM
In vivo use Yes
Donated by Boehringer Ingelheim


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