Assay Method Information

Assay Name:  Ligand-Induced Uptake of [35S]-GTP-gamma-S
Description:  EC50s were determined by measuring the binding of [35S]-GTP-gamma-S to S1P receptors expressed in transfected Chinese hamster ovary (CHO) cell membranes. It is found that these modified 3-arylpropionic acids appeared to be more potent when evaluated in the functional assay than in the competitive binding assay, and their EC50 values served as a better guide for interpreting in vivo activity. All 3-arylpropionic acids and their modified analogs are found to be inactive against S1P2,4 receptors (IC50 > 10 uM).
Affinity data for this assay
 

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