Table 2.

Rank-order of potency for three BTK inhibitors

Classical kinase screening assays measuring phosphokinase activity were conducted using recombinant BTK protein and a fluorescent peptide pseudosubstrate in the presence of 16 µM ATP and defined concentrations of inhibitor. The concentration response curve (right panel) was fit to a normal hyperbola adjusted using a logit calculation to estimate the IC₅₀ and Hill slope for each test article. Results represent the average of two independent determinations