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BAY-784

2D structure
Target GNRHR  
Mode of action Antagonist
Control BAY-786
Recommended cellular usage concentration ≤ 1 µM
In vivo use yes
Synonyms BAY 1214784
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) Surpasses criterion: human GnRHR: IC50 = 27 nM (Tag Lite binding assay)
Selectivity within target family: goal is > 30-fold Surpasses criterion: Selectivity against a broad range of GPCR‘s. Clean PDSP scan except for weak activity on TMEM97 (Ki = 1107.9 nM)
Eurofins-Panlabs radioligand binding assay: The closest off-target is CNR1 with IC = 3.44 µM at 3 µM.
Selectivity outside target family Surpasses criterion: Eurofins-panlabs enzyme assay: The closest off-targets found at 10 µM are MAPK3 with IC50= 4.87 µM and MAPK14 with IC50 = 10.7 µM.
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: High potency in human cell-based IP-1 assay with IC50 of 21 nM (superagonist Buserelin stimulation at EC80). Suitable pharmacokinetic profile for in vivo studies; in vivo efficacy in LH suppression experiments in female rats and male monkeys shown.
Control compound (100 times less potent than the probe) Surpasses criterion: The control compound BAY-786 has at least 114-fold lower in vitro potency (IC50 = 2.4 μM). Clean PDSP scan except for weak activity on TMEM97 (Ki = 2001.24 nM)