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. Author manuscript; available in PMC: 2023 Jan 27.
Published in final edited form as: J Med Chem. 2021 Oct 20;65(2):1370–1383. doi: 10.1021/acs.jmedchem.1c00848

Table 1.

Biochemical activities against wt and mutant EGFR.

EGFR IC50 [nM]a
Compound wt LRd LR/TMd LR/TM/CSd
1 47 ± 8 2.0 ± 0.5 1.5 ± 0.3 4.9 ± 1.0
2a 6.2 ± 1 5.5 ± 0.3 32 ± 3 8.0 ± 1
2b > 1000 280 ± 22 > 1000 > 1000
2c 5.8 ± 1.0c 1.2 ± 0.4 51 ± 3 32 ± 6
LN2057 6.5 ± 1.0 0.26 ± 0.03 0.27 ± 0.05 130 ± 40
EAI045 b > 1000 8.8 ± 0.9 2.0 ± 0.5 13 ± 0.8
Osimertinib 17 ± 2 1.5 ± 0.4 0.35 ± 0.04 > 1000
a

IC50 values were measured from a single experiment in triplicate. ATP concentration was 100 μM. Errors are reported as ± standard error.

b

Data from De Clercq and Heppner ACS Med Chem Lett.20

c

Value is EC50 due to incomplete tyrosine kinase activity inhibition at [2c] = 1000 nM.

d

L858R (LR), T790M (TM), C797S (CS).