SERP
Comments:
BAY 298 demonstrates a noteworthy half maximal inhibitory concentration (IC50) of 96 nanomolar (nM) against its specific target, the luteinizing hormone/choriogonadotropin receptor (LHCGR). However, exposure to a concentration of 10 micromolar (µM) of BAY 298 resulted in approximately 50% inhibition or activation in a range of other G protein-coupled receptors (GPCRs), indicating a degree of non-selectivity. Furthermore, the GPCR Off-Target Profiling for BAY 298 was restricted to a narrow spectrum of approximately twenty GPCR isoforms.
Despite these off-target interactions, BAY 298 exhibits promising in vivo pharmacokinetic properties, including low systemic clearance, a prolonged plasma half-life, and high oral bioavailability. These pharmacological characteristics establish BAY 298 as a potent investigational tool compound, underscoring its significant potential for further pharmacological research and development.
(last updated:
8 Feb 2024 )