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. 2020 Feb 12;11(4):506–513. doi: 10.1021/acsmedchemlett.9b00621

Table 4. Biological Profile of Compound 39.

cell type assay stim readout EC50 ± SD (nM)
B-cells signaling αIgM pBLNK-Y96 24
p-Btk-Y223 26
p-Akt-S473 34
pERK-T202/Y204 37
pMEK-s217/s221 51
activation CD69 112 ± 10
CD86 164 ± 16
proliferation αIgM/αCD40 EdU incorporation 108 ± 55
T-cells proliferation αCD3/αCD28 EdU incorporation 1305 ± 425
macrophages cytokine release immune complex TNFα 180
IL-1β 90
IL-6 700
basophilsa activation αIgE CD63 73 ± 20
a

Human whole blood.