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. 2024 Apr 18;67(9):7245–7259. doi: 10.1021/acs.jmedchem.4c00072

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© 2024 The Authors. Published by American Chemical Society

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NUDIX selectivity, NUDT5 and NUDT14 cell target engagement and cell viability assay results. (A) NUDIX selectivity for compound 9 and ibrutinib (1) determined by SPR. NB, no binding (K_D > 100 μM) (n = 2). (B) NUDT5 NanoBRET TE assay result for the dual NUDT5/NUDT14 inhibitor 9 (EC₅₀ = 1.08 ± 0.07 μM). (C) Compounds 1 (ΔT_m = 1.6 ± 0.3) and 9 (ΔT_m = 5.5 ± 0.3) stabilize HiBiT-NUDT14 measured by CETSA in intact HEK293 cells upon 30 μM treatment for 1 h. (D) BTK NanoBRET TE assay for evaluation of 1 (EC₅₀ = 0.005 ± 0.001 μM) and 9 (EC₅₀ = 0.377 ± 0.062 μM). (E) Cell viability assay of 1 (IC₅₀ = 0.027 ± 0.011 μM) and 9 (>10 μM) in BT-474 cells after 72 h of incubation. (F) Radar chart summary of performance of 1 and 9 in different cell-based assays. Cell-based assay data are shown as mean ± SD and are based on three technical replicates or four technical replicates in the case of the HiBiT-NUDT14 CETSA. Graphs are representative of two independent biological replicates (n = 2).