Assay Method Information

Assay Name:  5-HT2 Receptor Assays
Description:  Compounds of the present application bind to the 5-HT2 receptor subtypes in the following assays: Compounds of the invention are tested on 5-HT2A and 5-HT2C human recombinant G protein-coupled receptors using a CHO-K1-mt aequorin Galpha16 cell line and IP-One assays (Euroscreen Laboratory, Belgium). Dose-response curves for the test compounds are generated over the concentration range of 0.01 to 20,000 nM to determine effective concentration (EC50), inhibitory concentration (IC50) as seen in Table 2, and relative degree of agonistic and antagonistic response ( relative response ). Compound binding was calculated as a % inhibition of the binding of a radioactively labeled ligand specific for each receptor. Results with inhibition >50% were considered to represent significant effects. In each experiment, the respective reference compound was tested in parallel with the test compounds, and the data were compared with previous values determined at Eurofins.
Affinity data for this assay
 

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