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. 2015 Dec 17;7(1):100–104. doi: 10.1021/acsmedchemlett.5b00428

Table 3. Selectivity over JAK Family Members.

graphic file with name ml-2015-00428k_0007.jpg

Cmpd TMLR Ki (μM)a wtEGFR Select.b JAK1 Select.c JAK2 Select.d
13 0.019 57 9 0.5
19 0.004 213 3 2
35 0.026 16 42 0.9
36 0.031 > 80 104 4
27 0.058 42 2 0.2
37 0.088 27 6 0.3
a

Ki data are an average of at least two independent experiments.

b

Ratio of wtEGFR Kiapp over EGFR(TMLR) Kiapp.

c

Ratio of JAK1 Kiapp over EGFR(TMLR) Kiapp.

d

Ratio of JAK2 Kiapp over EGFR(TMLR) Kiapp.