Abstract:
: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 Kd 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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Newton AS,Deiana L,Puleo DE,Cisneros JA,Cutrona KJ,Schlessinger J,Jorgensen WLdoi
10.1021/acsmedchemlett.7b00154subject
Has Abstractpub_date
2017-05-17 00:00:00pages
614-617issue
6issn
1948-5875journal_volume
8pub_type
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