225240-83-5Relevant articles and documents
Installation of Pargyline, a LSD1 Inhibitor, in the HDAC Inhibitory Template Culminated in the Identification of a Tractable Antiprostate Cancer Agent
Chen, I-Chung,Chen, Mei-Chuan,Hsieh, Chien-Ming,Hsu, Kai-Cheng,Lai, Row-Wen,Lin, Tony Eight,Liou, Jing-Ping,Nepali, Kunal,Ojha, Ritu,Pan, Shiow-Lin
, p. 17824 - 17845 (2022/01/03)
Pragmatic insertion of pargyline, a LSD1 inhibitor, as a surface recognition part in the HDAC inhibitory pharmacophore was planned in pursuit of furnishing potent antiprostate cancer agents. Resultantly, compound 14 elicited magnificent cell growth inhibi
JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules
Newton, Ana S.,Deiana, Luca,Puleo, David E.,Cisneros, José A.,Cutrona, Kara J.,Schlessinger, Joseph,Jorgensen, William L.
supporting information, p. 614 - 617 (2017/06/13)
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.
CHROMEN-2-ONE DERIVATIVES
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, (2010/11/28)
A compound of formula (I), wherein R1, R2, R3, R4, R5, and ring A are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical