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February 9, 2026Journal of Medicinal Chemistry6 citationsOpen Access

Cellular Context Affects Kinase Inhibitor Selectivity Assessment

Cellular Context Influences Kinase Inhibitor Selectivity

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Authors

MBM. BinderFBFrances M. BashoreKHKaitlin K. Dunn Hoffman

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Overview

Compares cell-free and cellular assays to assess kinase inhibitor selectivity, indicating significant differences in results.

Key Points

  • The aim is to assess the selectivity of kinase inhibitors using different assay systems and to identify their interactions in cellular contexts.
  • Compared selectivity profiling results from cell-free assays with cellular target engagement assays.
  • Utilized a panel of ten kinase inhibitors for systematic comparison.
  • Employed NanoBRET assays to evaluate cellular selectivity.
  • Characterized TPKI-39 based on its in-cell selectivity profile.
  • Identified divergent results between cell-free and cellular assay systems.
  • Unanticipated kinase interactions were found for type II inhibitors in cells.
  • TPKI-39 was characterized as a probe for DDR1, DDR2, and FLT1 based on cellular selectivity.
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Cite This Study

Binder et al. (2026) studied this question.

synapsesocial.com/papers/698979f5f0ec2af6756e81bahttps://doi.org/10.1021/acs.jmedchem.5c02916
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