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. 2021 Apr 12;64(9):5404–5428. doi: 10.1021/acs.jmedchem.0c01549

Table 2. Enzymatic Inhibitor Activity of Compounds 617 and Relative LogD7.4, Solubility, and Protein Bindinga.

compd hDHODH, IC50  ± SE (nM) LogD7.4  ± SDc solubility (μM) in PBS protein binding (% bond)
6 90.9 ± 13.1 0.66 ± 0.08 438 nd
7 1.35 ± 0.45 nd nd nd
8 6.23 ± 0.63 0.98 ± 0.03 47.3 99.58
9 150 ± 15 1.84 ± 0.06 20.2 nd
10 17.7 ± 3.30 insoluble <LOD nd
11 2.03 ± 0.44 2.09 ± 0.04 <LOD 99.96
12 71.8 ± 9.42 insoluble <LOD nd
13 6.34 ± 0.63 2.69 ± 0.03 <LOD 99.94
14 2.78 ± 0.32 1.82 ± 0.09 55.3 nd
15 2.30 ± 0.33 3.27 ± 0.19 8.1 100
16 2.75 ± 0.31 2.46 ± 0.04 74.3 99.95
17 4.09 ± 0.62 3.28 ± 0.12 12.9 100
a

The effect of the compounds is expressed as IC50 values. Limit of detection (LOD): 6 μM. The “nd” notation indicates that the compound was not tested in that specific assay.