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. 2011 Mar 8;2(5):342–347. doi: 10.1021/ml200025q

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
a

Biochemical assay (B-RafV600E).

b

Cellular phosphorylation assay (pERK) using B-RafV600E mutant Malme-3M or A375 cell line.

c

Ref (23).