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]