Table 2. Enzymatic Inhibitor Activity of Compounds 6–17 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 |
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.