FAK inhibitor 5 is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.

FAK (pre-incubation 5 min ATP 1000 μM): 3.0 μM , FAK (pre-incubation 5 min ATP 0.5 μM):1.6 μM , FAK (pre-incubation 60 min ATP 0.5 μM): 1.3 μM , FAK (pre-incubation 60 min ATP 1000 μM): 1.0 μM

The binding interactions between FAK inhibitor 5 in the FAK allosteric site is mostly hydrophobic in nature.?Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2.