Table 1.

Activity of NVP-BSK805 assessed in JAK radiometric filter binding kinase assays and compared with JAK inhibitor 1

NVP-BSK805, IC50 (nmol/L) ± SEJAK inhibitor 1, IC50 (nmol/L) ± SE
JAK1 JH131.63 ± 1.363.21 ± 0.27
JAK2 JH10.48 ± 0.021.04 ± 0.04
JAK3 JH118.68 ± 0.942.08 ± 0.09
TYK2 JH110.76 ± 0.891.56 ± 0.08
FL JAK2 V617F0.56 ± 0.041.73 ± 0.05
FL JAK2 wt0.58 ± 0.031.59 ± 0.09

NOTE: Half-maximal inhibitory concentrations ± SE were obtained by global fitting of the data of two independent experiments to the logistic equation (nonlinear regression).

Abbreviations: JH1, JAK homology 1; FL, full-length; wt, wild-type.