Table 1.
IC50 Profiles of B-Raf(V600E) TR-FRET and Ba/F3 Assays. Standard deviations for data are listed in parentheses (n=4-6).
| Inhibitor | IC50 [nM] | |||
|---|---|---|---|---|
| MEK(WT) | MEK(KD) | cSTKpep-3 | Ba/F3 | |
| 384-well | 384-well | 384-well | 384-well | |
| Cmpd A | 2(1) | 1(1) | 4(2) | 4(3) |
| Cmpd B | 112(31) | 4(1) | 140(77) | 84(7) |
| Cmpd C | 89(31) | 21(8) | 51(36) | 41(3) |
| Cmpd D | 4(2) | 2(1) | 4(3) | |
| Cmpd E | 70(27) | 19(1) | 15(16) | 33(22) |
| Cmpd F | 1153(140) | 7473(1615) | 833(63) | |
| Cmpd G | 846(601) | 41(12) | 100(2) | 1160(394) |
| Cmpd H | 10(5) | 2(2) | ||
| PD0325901 | 88(43) | NI | 122(82) | 78(35) |
| Bayer 43-9006 | 4542(1050) | 376(179) | 2309(625) | 5000(800) |
| Wortmannin | NI | NI | NI | |
| LY294002 | NI | NI | NI | |
| Cot inhibitor* | NI | NI | NI | |
| Staurosporine | 117(56) | NI | 106(40) | |
*
Cot Inhibitor: cmpd 30 [33]