Fig. 1.

In-cell inhibitor–binding affinities of mutant panel. (A) Structure of the Abl KD (PDB entry 2HYY). The locations of 94 patient-derived Abl mutants associated with resistance are indicated as spheres. The color of the spheres indicates the level of imatinib resistance conferred by the mutation: blue, affinity of mutant is less than twofold weaker than wt; green, affinity is between two- and fourfold weaker than wt; red, affinity is more than eightfold weaker than wt. (B) Fraction of mutations in different resistance classes. The colors correspond to A. (C) Imatinib and dasatinib resistance distribution of Abl mutants determined by in-cell NanoBRET target engagement assay. Colors correspond to A. Confidence of values is ± 23% based off of wt SD, n = 2.