Table 1.
Structure | EHI# | cLogP | Solubility (μM)b | Stability (%)c | |||
---|---|---|---|---|---|---|---|
Human liver mic. | Chicken liver mic. | ||||||
| |||||||
NADPH | − | + | − | + | |||
AUDA | 5.98 −1.14a |
37.5–50 | 98 ± 14 | 69 ± 5 | 106 ± 7 | 70 ± 1 | |
1138 | 4.97 | 10–12.5 | 98 ± 3 | 57 ± 21 | 69 ± 29 | 2.1 ± 0.5 | |
1471 | 4.84 0.62a |
> 100 | 97 ± 8 | 69 ± 2 | 77 ± 2 | 60 ± 4 | |
1749 | 2.90 | 75–100 | 1.2 ± 0.5 | 2.7 ± 0.8 | 105 ± 9 | 94 ± 4 | |
2119 | 3.84 | > 100 | 91 ± 6 | 53 ± 2 | 73 ± 1 | 24 ± 2 | |
2225 | 3.88 | 50–75 | 101 ± 4 | 94 ± 2 | 96 ± 5 | 96 ± 3 | |
2228 | 4.08 | 10–12.5 | 101 ± 5 | 5.4 ± 0.1 | 119 ± 15 | 89 ± 15 |
Base form.
In sodium phosphate buffer (0.1 M pH 7.4)
Percent of compound (1 μM) remaining after 30 minutes incubation with human or chicken liver microsomes (1 mg/mL) at 37°C with or without NADPH generating system. Results are average ± standard deviation (n = 3).