GSK2256098 [2-[5-Chloro-2-(2-isopropyl-5-methyl-2H-pyrazol-3-yiamino)-pyridin-4-ylamino]-N-methoxy-benzamide] as a potent, selective, reversible, and ATP competitive inhibitor of FAK (Focal adhesion kinase) activity (apparent Ki = 0.4 nM). The cocrystal structure reveals compound bound in the ATP binding pocket of FAK .
|GSK2256098: 2D and 3D Structure|
The potent enzymatic activity translates to cellular activity when IC50 values for reducing cellular phospho-FAK levels (pFAK-(Tyr 397)) were determined by ELISA. GSK2256098 inhibited cellular pFAK with IC50 values from 2-15 nM and level of pFAK remained low over time in the continues presence of the compound .
|1H NMR (Estimated) for GSK2256098|