AC220 KINOMEscan

The KINOMEscan assay platform is based on a competition binding assay that is run for a compound of interest against each of a panel of 442 kinases. The assay has three components: a kinase-tagged phage, a test compound, and an immobilized ligand that the compound competes with to displace the kinase. The amount of kinase bound to the immobilized ligand is determined using quantitative PCR of the DNA tag. Kd values (nM) reported for each compound were determined using 11 serial threefold dilutions of test compound and a DMSO control. A null result means no inhibition of kinase binding to the ligand in the presence of the compound and low Kd means strong inhibition.