Table 1. Potency and Selectivity Data for 1 and 4.
| IC50 [μM]a | 1 | 4 |
|---|---|---|
| BTKb | 0.005f | 0.014 (0.016) |
| BMXb | 0.001 (0) | 5.0 (0) |
| EGFRb | 0.016f | >10 |
| ERBB4b | 0.007f | >10f |
| Cellular FcγR/IL8c | <0.005 | 0.080 (0.0007) |
| Cellular pEGFR/A431d | 0.045 (0.015) | >8f |
| Human blood CD69e | 0.066 (0.022) | 0.934 (0.407) |
a
IC50 determined as a mean (n ≥ 2) (SD).
b
Enzyme assay.
c
FcγR-induced IL8 release in THP1 cells.
d
EGFR phosphorylation in A431 cells.
e
anti-IgM/IL-4 induced CD69 expression on B cells in human blood.
f
Single experiment.