Synergy and Antagonism between Allosteric and Active‐Site Inhibitors of Abl Tyrosine Kinase

Allosteric inhibitors of Abl kinase are being explored in the clinic, often combination with ATP-site kinase. However, there conflicting data on whether both ATP-competitive and myristoyl-site allosteric can simultaneously bind Here, we determine is synergy or antagonism between Abl. We observe that clinical not synergistic ABL inhibitors, however, conformation-selective modulate global conformation afford synergy. demonstrate key driver to two compounds Finally, explore interaction selective a series biochemical cellular assays.