Table 3 Summary of in vitro JNK1 PhALC assay (with 10 mM GSH) results with compounds containing the same warhead with modified ATP-competitive fragments

From: Reversible covalent c-Jun N-terminal kinase inhibitors targeting a specific cysteine by precision-guided Michael-acceptor warheads

R2

PhALC IC50/(nM)

1aR-IN-7

17 ± 5

1aR-IN-9

12 ± 1

1aR-IN-10

13 ± 2

1aR-isoPHEN

16 ± 2

  1. (Data show the mean±parameter error estimate from weighted least squares method; n = 3, independent experiments).
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