| 摘要 |
The invention provides methods and assay systems for both quantitative determination of a target, particularly a kinase, including a Tec family kinase, particularly BTK, and target occupancy, including the relative amount of available target associated with a target inhibitor or ligand, particularly wherein the target inhibitor or ligand is a covalent or irreversible kinase inhibitor, particularly including irreversible BTK inhibitor. The invention also relates to assays for determining target occupancy, normalized to total quantified target in a biological system or clinical sample, wherein target is quantified, normalized and occupancy determined using the same or a common assay format. In an aspect of the invention, biotinylated anti-BTK antibody and biotinylated BTK inhibitor probe are utilized in the assay format, on samples split for simultaneous or commensurate analysis. |
