Table 1 EGFR (EGFRwt, EGFRL858R and EGFRL858R/T790M) IC50 values (nM ± S.D./n ≥ 3) determined for compounds 7a-m.

From: A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives

IC50 (nM) ± S.D.

compounds

EGFRwt

EGFRL858R

EGFRL858R/T790M

gefitinib

<1

<1

185 ± 98

afatinib

<1

<1

<1

osimertinib

1 ± 0.6

<1

<1

(7a)

>10000

>10000

>10000

(7b)

>10000

>10000

>10000

(7c)

>10000

3237 ± 1257

2710 ± 412

(7d)

>10000

>10000

9867 ± 265

(7e)

>10000

>10000

6139 ± 3469

(7f)

2499 ± 735

2163 ± 1623

>10000

(7g)

179 ± 61

2099 ± 505

9829 ± 297

(7h)

25 ± 4

18 ± 3

1682 ± 1506

(7i)

>10000

5577 ± 4163

>10000

(7j)

123 ± 134

270 ± 202

823 ± 613

(7k)

3117 ± 787

445 ± 105

6293 ± 2789

(7l)

101 ± 12

32 ± 14

132 ± 49

(7m)

>10000

>10000

>10000

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