BAY-899
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). |