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. 2017 Mar 28;7:466. doi: 10.1038/s41598-017-00482-4

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© The Author(s) 2017

This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/

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Characterization of CHMFL-BTK-11 as an selective irreversible Bruton’s tyrosine kinase (BTK) inhibitor. (a) Chemical structure of CHMFL-BTK-11 and CHMFL-BTK-12; (b) ADP-Glo biochemical characterization of CHMFL-BTK-11 and CHMFL-BTK-12 against BTK kinase. (c) In vitro kinase assay using Flag-tagged BTK of wild-type or C481S immunopurified from HEK293 cells showed that CHMFL-BTK-11 inhibits only wild-type BTK, whereas CHMFL-BTK-12 fails to inhibit both wild-type and C481S BTK. Blots were cropped for improved clarity and conciseness. (d) Predicted mode of binding of CHMFL-BTK-11 to BTK based upon molecular modeling (PDB: 3OCS); (e) TreeSpot view of the kinase selectivity profile of CHMFL-BTK-11 using data generated from the KinomeScan approach. Data were representative of at least 2 independent experiments.