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(A) Comparative inhibitory properties of selected probes: the inhibition of NRGβ1-induced ERBB2 tyrosine phosphorylation in MCF7 cells was evaluated at 0.1 and 10 μM concentrations of the indicated compounds. For comparison, lapatinib was used at its clinically used serum concentration of 3 μM. (B) Compounds 3d and 1a show comparable affinity in inhibition studies but a difference in the maximum achievable inhibition.
