Table 1. Enzymatic and Cellular Activities of B-RafV600E Amide Series Inhibitors.
IC50 (nM) |
|||
---|---|---|---|
compd | enzymea | Malme-3Mb | A375b |
3 | 3900 | 6700 | >3000 |
4 | 920 | 2400 | >3000 |
5 | 110 | 310 | 1200 |
8 | 61 | 2400 | >3000 |
9 | 38 | 94 | 290 |
10 | 3.4 | 39 | 190 |
13 | 17 | 62 | 430 |
14 | 4.0 | 44 | 260 |
15 | 12 | 86 | 830 |
16 | 8.2 | 40 | 650 |
17 | 4.8 | 19 | 150 |
18 | 6.3 | 56 | 560 |
19 | 1.7 | 20 | 240 |
1 | 31c | 61 | 190 |
Biochemical assay (B-RafV600E).
Cellular phosphorylation assay (pERK) using B-RafV600E mutant Malme-3M or A375 cell line.
Ref (23).