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BAY-899

2D structure
Target LHCGR 
Targeted domain Remnants of the rhodopsin binding site
Mode of action Allosteric antagonist
Control BAY-897
Recommended cellular usage concentration 1 µM
In vivo use Yes
Donated by Bayer


Probe criteria


Selectivity within target family: > 30-fold Surpasses criterion: No activity on FSHR, TSHR. (hTSH antagonism IC50 = 24 µM; hFSH antagonism IC50 > 16 µM)
Clean in commercial GPCR panel of 25 GPCRs (all < 70% inhibition / activation at 10μM compound concentration).
Off-targets in the PDSP scan are SIGMAR1 (Ki = 1431.53 nM), TMEM97 (Ki = 2051.16 nM), OPRK1 (Ki = 7634.84 nM)
Selectivity outside target family Coming soon.
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: 185 nM in cell-based assay
Control compound (100 times less potent than the probe) BAY-897 is inactive on human LHCGR (IC50 > 16 µM) and FSHR (IC50 > 16 µM).
Closest hits in the PDSP scan are TMEM97 (Ki = 675.62 nM) and HTR2C (Ki = 1082.93 nM).