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. Author manuscript; available in PMC: 2013 Apr 3.
Published in final edited form as: J Biomol Screen. 2012 May 9;17(7):885–899. doi: 10.1177/1087057112446174

Figure 5. Assessment of potency of selected hits in a panel of kinases using the luminescence ADP production kinase assay.

Figure 5

Dose response studies of gefitinib, ZM-306416 and the erbstatin analog against a kinase panel consisting of the kinases EGFR, VEGFR1, SRC and ABL. The EGFR kinase inhibitor gefitinib is selectively potent toward EGFR, with a calculated IC50 of < 0.01 μM, and low or no activity toward VEGFR1 (IC50 > 10 μM), SRC (IC50 > 10 μM) and ABL (IC50 > 10 μM). In contrast, ZM-306416 is potent toward all kinases of the panel: EGFR (IC50 < 0.01 μM), VEGFR1 (IC50 = 0.33±0.04 μM), SRC (IC50 = 0.33±0.08 μM) and ABL (IC50 =1.3±0.2 μM). Erbstatin analog is inactive (IC50 > 10 μM) toward all kinases in the panel, including EGFR kinase.