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. Author manuscript; available in PMC: 2023 Jul 15.
Published in final edited form as: Bioorg Med Chem Lett. 2022 Apr 1;68:128718. doi: 10.1016/j.bmcl.2022.128718

Table 3.

EGFRL858R/T790M enzyme and Ba/F3 cell activity of isoquinolinones (C), quinazolinones (D) and phthalazinones (E) 16-27

graphic file with name nihms-1852250-t0009.jpg graphic file with name nihms-1852250-t0010.jpg graphic file with name nihms-1852250-t0011.jpg
Cpd Core R Enzyme
IC50 (nM)		 L858R/T790M
Cell IC50 (μM)		 L858R/T790M
Cetux co-dosing
Cell IC50 (μM)		 L858R/T790M
/C797S
Cell IC50 (μM)
7 0.9 1.00 0.020 0.18
16 C 6, N-Me piperazine 3.4 1.27 0.062 -
17 C 6, N-Me piperidine 1.2 1.28 0.024 0.50
18 C 7, N-Me piperazine 5.0 1.85 0.044 -
19 C 7, N-Me piperidine 1.8 1.50 0.070 0.38
20 D 7, N-Me piperidine 3.1 2.00 0.375 -
21 D 7, N-Me piperidine 5.8 2.43 0.225 0.90
22 D 6, N-Me piperidine 0.9 2.32 0.021 -
23 D 6, N-Me piperidine 0.2 0.78 0.007 0.05
24 E 6, N-Me piperidine 17.8 3.46 1.67 -
25 E 6, N-Me piperidine 9.7 1.24 0.538 0.99
26 E 7, N-Me piperidine 10.3 2.16 0.380 -
27 E 7, N-Me piperidine 4.0 1.54 0.207 0.44