Extended Data Fig. 4: Additional colorimetric ACP3 inhibition assays.
(a) Experiments performed with conjugates d9, d10, d11, and d12 from SOP-DEL. (b) Experiment performed with oligonucleotides bearing building block A2723 (d13 and d14) and (c) oligonucleotides bearing building block A2855 (d15 and d16) from FMA-DEL. Colorimetric ACP3 inhibition assay of B1326 (SOP-DEL), B125 (FMA-DEL), and their regioisomer derivatives were further performed (d, e). Possible exit-vector modifications of the benchmark scaffold were explored on the phenyl side (d) with compounds s13a-c, or benzyl side (e) with compounds s14a-c. ProXBM-DOTAGA, derived from compound s13c, was selected as the most potent conjugate, and used for further in vitro and in vivo studies. IC50 values are given as mean, with error bars indicating standard deviations of the replicates (n = 3).
