Table 1. Cellular Activities of Imidazopyridazines.
Cellular
Ba/F3 assaysa |
||||
---|---|---|---|---|
compd | TRKA | TRKB | TRKC | WTb |
1 | 0.85 | 0.27 | 0.10 | 7.13 |
2 | 0.74 | 0.20 | 0.23 | >10 |
3 | 0.050 | 0.021 | 0.006 | 3.92 |
4 | 0.17 | 0.12 | 0.075 | 1.01 |
5 | 0.076 | 0.027 | 0.040 | 1.92 |
6 | 0.006 | 0.007 | 0.003 | 3.00 |
7 | 0.027 | 0.013 | 0.004 | 2.53 |
8 | 0.52 | 0.13 | 0.020 | 5.89 |
9 | 0.17 | 0.050 | 0.011 | >10 |
10 | 0.075 | 0.047 | 0.019 | >10 |
11 | 0.068 | 0.029 | 0.008 | >10 |
12 | 3.13 | 1.97 | 0.98 | 9.23 |
13 | 0.021 | 0.011 | 0.003 | >10 |
14 | 0.003 | 0.001 | 0.001 | >10 |
15 | 0.005 | 0.004 | 0.002 | >10 |
16 | 0.001 | 0.001 | <0.001 | 4.79 |
17 | 0.004 | 0.004 | 0.002 | 5.91 |
Proliferation assays with Tel-TRK fusions; IC50, μM.
Proliferation assay using parental Ba/F3 cells.