Mps1-IN-1 dihydrochloride, a potent ATP-competitive inhibitor of Mps1 kinase, exhibits an IC50 of 367 nM. It effectively inhibits the activity of Mps1 mitotic kinase and disrupts spindle assembly checkpoint (SAC) function, thereby reducing the viability of both cancerous and 'normal' cells.

TNK1:2600 nM (Kd), Mps1:367 nM, Mps1:27 nM (Kd), Insulin receptor:470 μM (Kd), GAK:1100 nM (Kd), IGF-1R:750 nM (Kd), TYK1/LTK:29 nM (Kd), Insulin receptor related receptor:1200 nM (Kd), FAK:440 nM (Kd), TNK2:3100 nM (Kd), ALK:21 nM (Kd), CLK1:1900 nM (Kd), PYK2:280 nM (Kd), ERK2:2900 nM (Kd)