Which in vitro assay can I use to know if the tested compound acts as an allosteric inhibitor of GPCR ?

18 July 2023 1 4K Report

I want to develop negative allosteric inhibitors of CCR2 , which is one of the GPCR , what in-vitro assay is used to know if the tested compound acting as allosteric modulator?

Zhongtian Yu

The easiest assay you can consider is the measurement of Michaelis-Menten kinetics parameters of GPCR with/without the inhibitor. If it is acting as an allosteric inhibitor, it should alter vmax and would not cause much change in Km value.

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