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. Author manuscript; available in PMC: 2023 Feb 19.
Published in final edited form as: J Med Chem. 2022 Jun 2;65(12):8380–8400. doi: 10.1021/acs.jmedchem.2c00283

Table 3.

Binding Affinity (Kd, μM) for Different JAK2 Domains, and Selectivity for JH2 over JH1a

WT JH1 WT JH2 V617F JH2 JH2/JH1 Selectivity
2 6.6 ± 0.90 0.346 ± 0.034 0.478 ± 0.135 19x
6 8.1 ± 1.2 0.394 ± 0.044 0.131 ± 0.020 20x
11 5.75 ± 0.23 0.03710 ± 0.0005 0.033 ± 0.001 155x
12 3.36 ± 0.54 0.075 ± 0.015 0.062 ± 0.001 45x
13 6.81 ± 0.93 0.0334 ± 0.0033 0.043 ± 0.005 200x
14 5.91 ± 0.47 0.044 ± 0.003 0.050 ± 0.002 134x
a

For each Kd measurement, 2-3 independent experiments were carried out in quadruplicate and measured with the competitive fluorescence polarization (FP) assay.