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. 2022 Feb 18;7(8):7155–7171. doi: 10.1021/acsomega.1c06836

Table 3. Kinase Inhibitory Assay of the Newly Synthesized Derivatives 57 in Comparison with Erlotinib and AZD9291 against EGFRWT and Mutant EGFRT790Ma.

  IC50 (mean ± SEM) (μM)
compound no. EGFRWT EGFRT790M
erlotinib 0.09 ± 0.05 0.55 ± 0.10
AZD9291 0.52 ± 0.03 0.03 ± 0.01
5a 0.25 ± 0.01 0.17 ± 0.05
5b 0.22 ± 0.15 0.13 ± 0.11
5c 0.24 ± 0.30 0.14 ± 0.50
6a 0.18 ± 0.10 0.12 ± 0.18
6b 0.08 ± 0.05 0.09 ± 0.01
6c 0.15 ± 0.02 0.13 ± 0.07
7 0.22 ± 0.05 0.18 ± 0.11
a

IC50: compound concentration required to inhibit the enzymes’ activities by 50%; SEM: standard error mean; each value is the mean of three independent values.