Assay for Small-Molecule Antagonists of the TSH Receptor

National Center For Advancing Translational Sciences

Investigators

Abstract

During this period, the project team continued SAR-driven optimization of the lead molecule to improve metabolic stability. A 384-well assay to test effect of compounds on TSH-induced cAMP was re-established in the lab to support dose-response testing and further optimization. Great progress in optimizing the selected chemotype, having already molecules with high potency, selectivity and good metabolic stability. A selected optimized candidate is being scaled up for pharmacokinetic studies and potentially in vivo efficacy studies.