Assay Detail
Binding
CHEMBL5730132
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Monoamine Oxidase (MAO) Assay: Inhibition of monoamine oxidase activity was carried used using the MAO-GIo Assay Kit according to the manufacturer's suggested protocol. Briefly, 6.25 μL of test compound was added to each well of a 384-well plate. Enzyme (either MAO A or B) was added (12.5 μL in 2× buffer containing 1 μg protein) and allowed to incubate for 5 minutes. Finally, 6.25 μL of 4×MAO substrate was added to each well. Following a one hour incubation, 25 μL of Luciferin detection reagent was added to each well, and incubated for 20 minutes. Luminescence was then measured on an Envision microplate reader. Representative data used to determine IC50 for inhibition of each MAO isoform is provided in Figure 4, and representative data for several compounds is summarized in Table 8 below.
15
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.87 | 5.68 |
| kon | 5 | - | - |
| k_off | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3682538 | — | — | 3 | 5.68 |
| CHEMBL199600 | — | — | 3 | 4.05 |
| CHEMBL3104250 | — | — | 3 | - |
| CHEMBL3682530 | — | — | 3 | - |
| CHEMBL3682536 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3682538 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL199600 | — | IC50 | = | 88500.0 | nM | 4.05 |
| CHEMBL3682538 | — | kon | = | - | — | - |
| CHEMBL3682538 | — | k_off | = | - | s-1 | - |
| CHEMBL199600 | — | kon | = | - | — | - |
| CHEMBL199600 | — | k_off | = | - | s-1 | - |
| CHEMBL3104250 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3104250 | — | kon | = | - | — | - |
| CHEMBL3104250 | — | k_off | = | - | s-1 | - |
| CHEMBL3682530 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3682530 | — | kon | = | - | — | - |
| CHEMBL3682530 | — | k_off | = | - | s-1 | - |
| CHEMBL3682536 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3682536 | — | kon | = | - | — | - |
| CHEMBL3682536 | — | k_off | = | - | s-1 | - |