Table 5. Selectivity, Stability, CYP Inhibition, hERG, Solubility, and Acute Toxicity of 18e.
entry | hHSD2 inhibition | plasma stability | CYP inhibition | hERG | aqueous solubility | acute toxicity |
---|---|---|---|---|---|---|
18e | 20% at 10 μM | 100% after 30 min incubation | 1A2 > 100 μM | 36.9 μM | 361 μM | LD50 > 1000 mpk |
2C9 > 100 μM | ||||||
2C19 > 100 μM | ||||||
2D6 > 100 μM | ||||||
3A4 > 100 μM |