BAY-298

BAY-298 : Antagonist of LHCGR

Structure

Information

  • LHCGR
  • Antagonist
  • up to 1 uM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Functional, GPCR Off-Target Profiling of BAY 298 (Eurofins). Compound was tested in both, antagonistic (inhibition) and agonistic (activation) mode at a single concentration of 10 µM.
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

It is worth noting that BAY-298 shows only 24-fold selectivity to TSH (2.3 µM)

(last updated: 7 Feb 2024 )

SERP Ratings

In Cell Rating
In Model Organisms

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 )