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JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.


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.

SUBMITTER: Newton AS 

PROVIDER: S-EPMC5467202 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

Newton Ana S AS   Deiana Luca L   Puleo David E DE   Cisneros José A JA   Cutrona Kara J KJ   Schlessinger Joseph J   Jorgensen William L WL  

ACS medicinal chemistry letters 20170517 6


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 <b>5</b> and <b>6</b> used in the assay are reported as well as <i>K</i><sub>d</sub> 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 <b>8</b> elucidate the binding  ...[more]

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