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. Author manuscript; available in PMC: 2021 Jul 27.
Published in final edited form as: J Med Chem. 2018 Sep 28;61(19):8875–8894. doi: 10.1021/acs.jmedchem.8b01108

Table 6.

In-Cell Western Analysis of pERK1/2T202/Y204 Levels

Compd 47 64 42 62 56 58 55 38 60 59 63 65 29 23 10 3 61
HeLa ICW EC50 (μM) 3.2 ± 0.1 5.9 ± 0.4 6.0 ± 1.2 7.8 ± 1.9 8.8 ± 2.9 9.0 ± 2.4 10.2 ± 4.1 11.0 ± 5.0 11.4 ± 3.8 14.0 ± 1.5 14.0 ± 0.8 14.1 ± 1.3 14.5 ± 1.8 21.0 ± 7.6 21.3 ± 10.0 32.2 ± 11.0 33.2 ± 10.9
H727 ICW EC50 (μM) 7.3 ± 3.1 10.0 ± 3.2 7.3 ± 1.5 13.4 ± 2.6 13.9 ± 0.2 15.6 ± 5.5 14.5 ± 1.0 36.8 ± 4.7 15.7 ± 2.2 19.7 ± 6.4 27.5 ± 2.8 21.1 ± 6.1 21.2 ± 8.4 51.4 ± 16.8 29.1 ± 1.8 18.7 ± 5.8 42.5 ± 15.1
Kd (μM) 0.14 0.049 0.14 0.012 0.10 <0.10 0.11 0.12 0.013 0.012 0.036 0.009 0.46 14.8 2.59 55.0 0.18
HeLa biphasic + + + + + + + + + + + + + − + − −
H727 biphasic + + + + + + + − + + − + + − + + −