Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 8, Issue 6, Pages 614-617Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00154
Keywords
Janus Kinase 2; JAK2; JAK2 JH2; Pseudokinase domain; Fluorescence polarization; FP; JNJ7706621; NVP-BSK805; Filgotinib (GLPG0634); Protein crystallography
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Funding
- Yale Medical School X-ray generator and detector [1S10OD018007]
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A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe molecules with the pseudokinase JAK2 JH2 allosteric site. The syntheses of the fluorescent 5 and 6 used in the assay are reported as well as K-d results for 10 compounds, including JNJ7706621, NVP-BSK805, and filgotinib (GLPG0634). X-ray crystal structures of JAK2 JH2 in complex with NVP-BSK805, filgotinib, and diaminopyrimidine 8 elucidate the binding poses.
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