. 2020 Apr 10;63(8):4047–4068. doi: 10.1021/acs.jmedchem.9b02076

Table 2. Structure-Activity Relationships of the Benzimidazolone-N³ Position (Labeled as R³ Group).

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Data represent the geometric mean of at least three replicates. See Supporting Information Table S2 for full statistics.

Kinetic solubility measured by NMR in HEPES buffer (containing 5% DMSO) at pH 8. Where this was <30 μM, solubility by HPLC in PBS buffer and 1% DMSO at pH 7.4 was also measured and is shown in parentheses.

Table 2. Structure-Activity Relationships of the Benzimidazolone-N3 Position (Labeled as R3 Group).

Table 2. Structure-Activity Relationships of the Benzimidazolone-N³ Position (Labeled as R³ Group).