Basic Information
ID: ALA3887355
Type: Binding
Description: Inhibition Assay: In the following Examples, 0.9 mL aliquots of a solution of candidate inhibitor in 100 mM potassium phosphate buffer, pH 7.2 was mixed bovine plasma amine oxidase (0.1 mL, about 8 AM) and incubated at 30° C. aerobically. Aliquots (0.1 mL) were periodically withdrawn using disposable calibrated Drummond micropipettes and diluted with 1.0 mL of benzylamine (5 mM in 50 mM sodium phosphate buffer, pH 7.2) in a 1 cm quartz cuvette (1.5 mL volume). The rate of oxidation of benzylamine to benzaldehyde was measured by recording the increase in absorbance at 250 nm for 1 minute and compared to the rate of benzylamine oxidation in a companion control solution of enzyme without inhibitor. The concentration of active BPAO was estimated from the rate of benzylamine oxidation. Inhibitory potency values (IC50 values) and partition values for inactivation of BPAO were measured at various times as in indicated in the Tables.
Tissue: Plasma
Activity Charts
Bioactivity
Activity Types for Assay ALA3887355
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 131.18 | 1.00 | 1.00 |
| 146.19 | 0.78 | 0.78 |
| 84.12 | -1.09 | -1.09 |
| 97.16 | 1.07 | 1.07 |
| 86.14 | -0.54 | -0.54 |
| 174.25 | 0.74 | 0.74 |
| 183.25 | -0.81 | -0.81 |
| 133.98 | 0.30 | 0.30 |
| 245.33 | 0.02 | 0.02 |
| 159.23 | 2.10 | 2.10 |
| 91.54 | 0.70 | 0.70 |
| 80.09 | -0.53 | -0.53 |
| 188.27 | 0.78 | 0.78 |
| 159.23 | 1.58 | 1.58 |
| 69.11 | 0.29 | 0.29 |
| 175.23 | 1.40 | 1.40 |
| 108.14 | -1.09 | -1.09 |
| 173.26 | 2.29 | 2.29 |
| 284.32 | -2.54 | -2.54 |
| 120.58 | 0.03 | 0.03 |
| 94.12 | 0.22 | 0.22 |
| 91.54 | 0.70 | 0.70 |
| 159.23 | 1.75 | 1.75 |
| 145.20 | 1.39 | 1.39 |
| 145.20 | 1.81 | 1.81 |
| 83.13 | 0.36 | 0.36 |