Assay Detail
Binding
CHEMBL3707812
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorescent-Based (Inhibitor) Screening Assay: Human recombinant monoamine oxidase proteins MAO-A and MAO-B were purchased from Sigma Aldrich. MAOs catalyze the oxidative deamination of 1, 2 and 3 amines. In order to monitor MAO enzymatic activities and/or their inhibition rate by inhibitor(s) of interest, a fluorescent-based (inhibitor)-screening assay was set up. 3-(2-Aminophenyl)-3-oxopropamamine (kynuramine dihydrobromide, Sigma Aldrich), a non fluorescent compound was chosen as a substrate. Kynuramine is a non-specific substrate for both MAOs activities. While undergoing oxidative deamination by MAO activities, kynuramine is converted into 4-hydroxyquinoline (4-HQ), a resulting fluorescent product.The monoamine oxidase activity was estimated by measuring the conversion of kynuramine into 4-hydroxyquinoline. Assays were conducted in 96-well black plates with clear bottom (Corning) in a final volume of 100 uL. The assay buffer was 100 mM HEPES, pH 7.5. Each experiment was performed in triplicate within the same experiment.
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Phenylcyclopropylamine derivatives and their medical use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 5.14 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 6.22 |
| CHEMBL3651093 | — | — | 1 | 6.00 |
| CHEMBL3651140 | — | — | 1 | 5.82 |
| CHEMBL3651113 | — | — | 1 | 5.72 |
| CHEMBL3651102 | — | — | 1 | 5.70 |
| CHEMBL3651147 | — | — | 1 | 5.68 |
| CHEMBL3651124 | — | — | 1 | 5.66 |
| CHEMBL3651105 | — | — | 1 | 5.64 |
| CHEMBL3651148 | — | — | 1 | 5.64 |
| CHEMBL3651123 | — | — | 1 | 5.62 |
| CHEMBL3651139 | — | — | 1 | 5.60 |
| CHEMBL3651108 | — | — | 1 | 5.52 |
| CHEMBL3651110 | — | — | 1 | 5.52 |
| CHEMBL3651114 | — | — | 1 | 5.48 |
| CHEMBL3651125 | — | — | 1 | 5.46 |
| CHEMBL3651101 | — | — | 1 | 5.40 |
| CHEMBL3651118 | — | — | 1 | 5.27 |
| CHEMBL3651107 | — | — | 1 | 5.27 |
| CHEMBL3651103 | — | — | 1 | 5.22 |
| CHEMBL3651109 | — | — | 1 | 5.22 |
| CHEMBL3651111 | — | — | 1 | 5.21 |
| CHEMBL3651092 | — | — | 1 | 5.16 |
| CHEMBL3651151 | — | — | 1 | 5.13 |
| CHEMBL3651112 | — | — | 1 | 5.10 |
| CHEMBL3651104 | — | — | 1 | 5.10 |
| CHEMBL3651145 | — | — | 1 | 5.10 |
| CHEMBL3651120 | — | — | 1 | 5.09 |
| CHEMBL3651136 | — | — | 1 | 5.07 |
| CHEMBL3651128 | — | — | 1 | 5.02 |
| CHEMBL3651138 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989843 | TRANYLCYPROMINE | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3651093 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3651140 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3651113 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3651102 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3651147 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3651124 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3651105 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3651148 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3651123 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3651139 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3651108 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3651110 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3651114 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3651125 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3651101 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3651118 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3651107 | — | IC50 | = | 5330.0 | nM | 5.27 |
| CHEMBL3651103 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3651109 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3651111 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3651092 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3651151 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3651145 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3651112 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3651104 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3651120 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL3651136 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3651128 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3651138 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL3651146 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3651135 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3651091 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3651100 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3651129 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL3651094 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3639499 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3651137 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL3651096 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3651126 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3651119 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL3651099 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3651095 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3651117 | — | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL3651134 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL3651122 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3651142 | — | IC50 | = | 23800.0 | nM | 4.62 |
| CHEMBL3651141 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL3651097 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3651121 | — | IC50 | = | 34300.0 | nM | 4.46 |