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 |
Human whole blood.