Table 3. Selectivity over JAK Family Members.
Cmpd | TMLR Ki (μM)a | wtEGFR Select.b | JAK1 Select.c | JAK2 Select.d |
---|---|---|---|---|
13 | 0.019 | 57 | 9 | 0.5 |
19 | 0.004 | 213 | 3 | 2 |
35 | 0.026 | 16 | 42 | 0.9 |
36 | 0.031 | > 80 | 104 | 4 |
27 | 0.058 | 42 | 2 | 0.2 |
37 | 0.088 | 27 | 6 | 0.3 |
Ki data are an average of at least two independent experiments.
Ratio of wtEGFR Kiapp over EGFR(TMLR) Kiapp.
Ratio of JAK1 Kiapp over EGFR(TMLR) Kiapp.
Ratio of JAK2 Kiapp over EGFR(TMLR) Kiapp.