IC50 values of various ATP-competitive inhibitors conjugated to AGT(PP1). (A). Chemical structures of BG-linked, ATP-competitive kinase inhibitors 4–6. (B). In vitro activities of unconjugated inhibitors 4, 5, and 6 and bivalent conjugates AGT(PP1)-4, AGT(PP1)-5, AGT(PP1)-6 against SRC-3D. In vitro activities of unconjugated 4, 5, 6 and bivalent conjugates AGT(WT)-4, AGT(WT)-6, AGT(PP4)-4, AGT(PP4)-5, AGT(PP4)-6 against ABL-3D. All protein-small molecule conjugates were prepared in two independent labeling reactions, and values shown are the average of four assays ± SEM.