Ceritinib 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 317 to 456 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. Results for each kinase are reported as "Percent of control", where the control is DMSO and where a 100% result means no inhibition of kinase binding to the ligand in the presence of the compound, and where low percent results mean strong inhibition.

KINOMEscan检测平台（KINOMEscan assay platform）基于竞争性结合检测技术，针对目标化合物与由317至456种激酶组成的激酶组逐一开展检测。该检测包含三个组分：带有激酶标签的噬菌体（kinase-tagged phage）、受试化合物，以及可与该化合物竞争置换结合激酶的固定化配体。通过对DNA标签进行定量PCR（quantitative PCR），可测定与固定化配体结合的激酶含量。每种激酶的检测结果以"Percent of control"报告，其中对照组为二甲基亚砜（DMSO）；当结果为100%时，代表该化合物存在时未抑制激酶与配体的结合，而较低的百分比则代表较强的抑制作用。