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Kinome binding profile of 2 and analogs using the Kinobead assay. (A) Profile of GEM 2 (2 μM) compared to (B) chlorinated analog 43 (2 μM) with improved CDK2 selectivity; (C) acetylated analog 47 (2 μM) with alternate selectivity in the CAMK group; (D) analog 38 (50 μM) with alternate specificity in the CK1 group. Kinases with engagement >50% are labeled, kinase classes that show differentiation between analogs of 2 are highlighted.
