GPCR functional assay

Functional activity data of GPCRs (G protein-coupled receptors) are crucial in drug discovery programs for monitoring therapeutic effects and potential off-target side effects. A reliable and efficient assay for this purpose uses the non-hydrolysable GTP derivative, GTPγS, which enables the detection of G protein activation upon ligand binding. Fluorescent GTPγS offers a significant advantage over radioactive [³⁵S]GTPγS by providing the same sensitivity and robustness while allowing assays to be conducted using conventional lab equipment.

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