Ontology highlight
ABSTRACT:
SUBMITTER: Newton AS
PROVIDER: S-EPMC5467202 | biostudies-literature | 2017 Jun
REPOSITORIES: biostudies-literature
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]