Ana S Newton, Luca Deiana, David E Puleo, José A Cisneros, Kara J Cutrona, Joseph Schlessinger, William L Jorgensen
ACS medicinal chemistry letters 2017 Jun 08A 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.
Ana S Newton, Luca Deiana, David E Puleo, José A Cisneros, Kara J Cutrona, Joseph Schlessinger, William L Jorgensen. JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules. ACS medicinal chemistry letters. 2017 Jun 08;8(6):614-617
PMID: 28626520
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