Selectivity index, ratio of EC50 for agonist activity at human S1P3 receptor expressed in EDG3-Ga15-bla HEK293T cell membranes to EC50 for agonist activity at human S1P1 receptor expressed in CHO cell membranes
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
Agonist activity at human S1P3 receptor expressed in EDG3-Ga15-bla HEK293T cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes assessed as remaining receptor level in cell membrane at 4.6 nM preincubated for 50 mins followed by compound washout measured at 4 hrs relative to control
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes assessed as remaining receptor level in cell membrane at 4.6 nM preincubated for 50 mins followed by compound washout measured at 16 hrs relative to control