Assay Detail
Binding
CHEMBL5729883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
MAO-A and MAO-B Assays: MAO assays included luminogenic MAO substrate, reaction buffers, Luciferin Detection and the reconstitution buffer with esterase. Standard MAO reaction mixtures included microsome contained MAO-A (2 ug) or MAO-B (10 ug), 160 uM substrate for MAO-A or 16 uM substrate for MAO-B, MAO-A buffer (100 mM Hepes buffer, pH 7.5, 5% glycerol) or MAO-B buffer (100 mM Hepes, pH 7.5, 5% glycerol, 10% dimethyl sulfoxide) in a final volume of 30 ul. After 20 minutes of pre-incubation of the enzyme with compounds, the reaction was initiated by adding enzyme substrate and the reaction was allowed to proceed for 60 minutes. Reconstituted Luciferin Detection Reagent (30 ul) was then added is added to simultaneously stop the MAO reaction and convert the methyl ester derivative to luciferin and produce light. The amount of light produced is directly proportional to the activity of MAO.
123
Total Activities
41
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
ALDH-2 inhibitors in the treatment of addiction
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 4.33 | 4.33 |
| kon | 41 | - | - |
| k_off | 41 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3660740 | — | — | 3 | 4.33 |
| CHEMBL3660747 | — | — | 3 | - |
| CHEMBL3918259 | — | — | 3 | - |
| CHEMBL3660719 | — | — | 3 | - |
| CHEMBL3660718 | — | — | 3 | - |
| CHEMBL3660717 | — | — | 3 | - |
| CHEMBL3660716 | — | — | 3 | - |
| CHEMBL3935026 | — | — | 3 | - |
| CHEMBL3660714 | — | — | 3 | - |
| CHEMBL3660713 | — | — | 3 | - |
| CHEMBL3660722 | — | — | 3 | - |
| CHEMBL3660752 | — | — | 3 | - |
| CHEMBL3660751 | — | — | 3 | - |
| CHEMBL5856466 | — | — | 3 | - |
| CHEMBL3660749 | — | — | 3 | - |
| CHEMBL3660748 | — | — | 3 | - |
| CHEMBL3660746 | — | — | 3 | - |
| CHEMBL3660745 | — | — | 3 | - |
| CHEMBL3660744 | — | — | 3 | - |
| CHEMBL3660732 | — | — | 3 | - |
| CHEMBL3660742 | — | — | 3 | - |
| CHEMBL3660741 | — | — | 3 | - |
| CHEMBL3660739 | — | — | 3 | - |
| CHEMBL3660738 | — | — | 3 | - |
| CHEMBL3915386 | — | — | 3 | - |
| CHEMBL3660736 | — | — | 3 | - |
| CHEMBL3660735 | — | — | 3 | - |
| CHEMBL3660734 | — | — | 3 | - |
| CHEMBL3660733 | — | — | 3 | - |
| CHEMBL3660743 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3660740 | — | IC50 | = | 46947.0 | nM | 4.33 |
| CHEMBL3660751 | — | IC50 | = | 110381.0 | nM | - |
| CHEMBL3660741 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660741 | — | kon | = | - | — | - |
| CHEMBL3660741 | — | k_off | = | - | s-1 | - |
| CHEMBL3660742 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660742 | — | kon | = | - | — | - |
| CHEMBL3660747 | — | k_off | = | - | s-1 | - |
| CHEMBL3660752 | — | k_off | = | - | s-1 | - |
| CHEMBL3660752 | — | kon | = | - | — | - |
| CHEMBL3660752 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660751 | — | k_off | = | - | s-1 | - |
| CHEMBL3660751 | — | kon | = | - | — | - |
| CHEMBL3660740 | — | k_off | = | - | s-1 | - |
| CHEMBL5856466 | — | k_off | = | - | s-1 | - |
| CHEMBL5856466 | — | kon | = | - | — | - |
| CHEMBL5856466 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660749 | — | k_off | = | - | s-1 | - |
| CHEMBL3660749 | — | kon | = | - | — | - |
| CHEMBL3660749 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660748 | — | k_off | = | - | s-1 | - |
| CHEMBL3660748 | — | kon | = | - | — | - |
| CHEMBL3660748 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660744 | — | k_off | = | - | s-1 | - |
| CHEMBL3660744 | — | kon | = | - | — | - |
| CHEMBL3660744 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660736 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660742 | — | k_off | = | - | s-1 | - |
| CHEMBL3660732 | — | k_off | = | - | s-1 | - |
| CHEMBL3660733 | — | IC50 | > | 86479.0 | nM | - |
| CHEMBL3660733 | — | kon | = | - | — | - |
| CHEMBL3660733 | — | k_off | = | - | s-1 | - |
| CHEMBL3660734 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660734 | — | kon | = | - | — | - |
| CHEMBL3660734 | — | k_off | = | - | s-1 | - |
| CHEMBL3660735 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660735 | — | kon | = | - | — | - |
| CHEMBL3660735 | — | k_off | = | - | s-1 | - |
| CHEMBL3660740 | — | kon | = | - | — | - |
| CHEMBL3660736 | — | kon | = | - | — | - |
| CHEMBL3660736 | — | k_off | = | - | s-1 | - |
| CHEMBL3915386 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3915386 | — | kon | = | - | — | - |
| CHEMBL3915386 | — | k_off | = | - | s-1 | - |
| CHEMBL3660738 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660738 | — | kon | = | - | — | - |
| CHEMBL3660738 | — | k_off | = | - | s-1 | - |
| CHEMBL3660739 | — | IC50 | > | 130000.0 | nM | - |
| CHEMBL3660739 | — | kon | = | - | — | - |
| CHEMBL3660739 | — | k_off | = | - | s-1 | - |