Figure 1.

Competitive SPR biosensor screen for SMYD3 and identified allosteric hit. A) Layout of the four surfaces on the sensor chip: Native SMYD3 alone (SMYD3) and in complex with active site‐specific tight‐binding inhibitor EPZ031686 (bSMYD3) were used as analytical surfaces, denatured protein (dSMYD3) and an empty intact surface (Mock) were used for referencing. B) Overlay of unreferenced sensorgrams for 25 μM SAH injected repeatedly over SMYD3 over the course of 10 h. C) Data for 40 compounds screened at 200 μM. Molecular weight‐adjusted responses from SMYD3 (top) and bSMYD3 (bottom) surfaces. Recurring injections of 25 μM SAH (positive control, blue bars). D) Chemical structure of the identified screening hit.