Skip to main content
. 2023 Apr 14;13:6118. doi: 10.1038/s41598-023-32854-4

Table 2.

NanoBRET and solubility data for Indolyl Pyrimidinamine Library

graphic file with name 41598_2023_32854_Fign_HTML.gif
Compound Scaffold n R TTBK1 intact cell NB IC50 (µM)[a] TTBK1 permeabilized cell NB IC50 (µM)[b] TTBK2 intact cell NB IC50 (µM)[a] TTBK2 permeabilized cell NB IC50 (µM)[b] Kinetic solubility (µM)
1 A 1 graphic file with name 41598_2023_32854_Figo_HTML.gif  > 30 2.5 16 3.6 NT[c]
AMG28 A 2 graphic file with name 41598_2023_32854_Figp_HTML.gif 20.9 ± 1.4[e] 2.88 ± 0.26[e] 12.6 ± 0.9[e] 4.10 ± 0.65[e] NT
2 A 3 graphic file with name 41598_2023_32854_Figq_HTML.gif  > 30 19  > 30 17 NT
3 B N/A[d] graphic file with name 41598_2023_32854_Figr_HTML.gif 15.8 ± 3.3[e] 2.34 ± 0.31[e] 11.7 ± 3.7[e] 2.52 ± 0.62[e] 133
4 A 2 graphic file with name 41598_2023_32854_Figs_HTML.gif  > 30 20  > 30  > 30 NT
5 A 2 graphic file with name 41598_2023_32854_Figt_HTML.gif  > 30 7.2 26 9.3 NT
6 A 2 graphic file with name 41598_2023_32854_Figu_HTML.gif  > 30 25  > 30 19 NT
7 A 2 graphic file with name 41598_2023_32854_Figv_HTML.gif  > 30  > 30  > 30  > 30 NT
8 A 2 graphic file with name 41598_2023_32854_Figw_HTML.gif  > 30  > 30  > 30  > 30 NT
9 A 2 graphic file with name 41598_2023_32854_Figx_HTML.gif 12.7 ± 0.7[e] 2.11 ± 0.43[e] 6.40 ± 1.17[e] 1.47 ± 0.36[e] 50
10 A 2 graphic file with name 41598_2023_32854_Figy_HTML.gif 11.1 ± 2.0[e] 1.97 ± 0.00[e] 6.39 ± 1.59[e] 1.39 ± 0.44[e] 131
11 A 2 graphic file with name 41598_2023_32854_Figz_HTML.gif  > 30  > 30  > 30  > 30 NT

aAssay executed in intact HEK293 cells. bAssay executed in permeabilized HEK293 cells. cNT: not tested. dN/A: not applicable. eData representative of two biological replicates ± SEM.