Assay Detail
Binding
CHEMBL5730349
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Inhibitory Activity Assay: The MAO-A inhibitory activity evaluation described below followed the protocol of MAO-Glo (registered trademark) Assay of Promega KK.A test compound dissolved in DMSO was added to a reaction solution (100 mM HEPES (pH 7.5), 5% glycerol) containing MAO-A enzyme (Sigma-Aldrich Co. LLC.), and the mixture was reacted at room temperature for 15 min. MAO substrate (Promega KK) was added to start the reaction. After reaction at room temperature for 60 min, Luciferine detection reagent (Promega KK) was added to terminate the reaction. After reaction at room temperature for 20 min with stirring, the luminescence was measured by Envision (PerkinElmer). The MAO-A inhibitory rate (%) of the test compound was calculated by the following formula.inhibitory rate (%)=(1-(test compound count-blank)/(control-blank))x100The count of the MAO-A enzyme reaction mixture under compound non-addition conditions is indicated as control, and the count under compound non-addition and MAO-A enzyme non-addition conditions is indicated as blank. A concentration necessary for achieving 50% inhibitory rate was taken as IC50 value.
375
Total Activities
113
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Cyclopropanamine compound and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 125 | 4.33 | 5.00 |
| kon | 125 | - | - |
| k_off | 125 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5934359 | — | — | 3 | 5.00 |
| CHEMBL6038994 | — | — | 3 | 4.66 |
| CHEMBL5842495 | — | — | 3 | 4.64 |
| CHEMBL5957170 | — | — | 3 | 4.60 |
| CHEMBL5992118 | — | — | 3 | 4.51 |
| CHEMBL5960687 | — | — | 3 | 4.48 |
| CHEMBL5811556 | — | — | 3 | 4.44 |
| CHEMBL5946126 | — | — | 3 | 4.31 |
| CHEMBL6056605 | — | — | 3 | 4.21 |
| CHEMBL5983110 | — | — | 3 | 4.21 |
| CHEMBL6013083 | — | — | 6 | 4.17 |
| CHEMBL6018178 | — | — | 3 | 4.12 |
| CHEMBL5863242 | — | — | 3 | 4.09 |
| CHEMBL6016392 | — | — | 3 | 4.07 |
| CHEMBL5745337 | — | — | 3 | 4.06 |
| CHEMBL6012828 | — | — | 3 | 4.05 |
| CHEMBL5910071 | — | — | 3 | 4.01 |
| CHEMBL5955351 | — | — | 3 | - |
| CHEMBL5880544 | — | — | 6 | - |
| CHEMBL5870582 | — | — | 3 | - |
| CHEMBL5773232 | — | — | 3 | - |
| CHEMBL5957352 | — | — | 3 | - |
| CHEMBL5848503 | — | — | 3 | - |
| CHEMBL5747328 | — | — | 3 | - |
| CHEMBL5919816 | — | — | 3 | - |
| CHEMBL5797523 | — | — | 3 | - |
| CHEMBL6024729 | — | — | 3 | - |
| CHEMBL5830307 | — | — | 3 | - |
| CHEMBL6026011 | — | — | 3 | - |
| CHEMBL6044125 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5934359 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL6038994 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5842495 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5957170 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5992118 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL5960687 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL5811556 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL5946126 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL5983110 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL6056605 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL6013083 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL6018178 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL5863242 | — | IC50 | = | 82000.0 | nM | 4.09 |
| CHEMBL6016392 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL5745337 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL6012828 | — | IC50 | = | 89000.0 | nM | 4.05 |
| CHEMBL5910071 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL5745337 | — | k_off | = | - | s-1 | - |
| CHEMBL5807170 | — | kon | = | - | — | - |
| CHEMBL6007489 | — | k_off | = | - | s-1 | - |
| CHEMBL5807170 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL6007489 | — | kon | = | - | — | - |
| CHEMBL5903914 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5903914 | — | kon | = | - | — | - |
| CHEMBL5903914 | — | k_off | = | - | s-1 | - |
| CHEMBL6056929 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5887105 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL6056929 | — | kon | = | - | — | - |
| CHEMBL6056929 | — | k_off | = | - | s-1 | - |
| CHEMBL5861157 | — | k_off | = | - | s-1 | - |
| CHEMBL5861157 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5861157 | — | kon | = | - | — | - |
| CHEMBL5943902 | — | k_off | = | - | s-1 | - |
| CHEMBL5831410 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL6007489 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5887105 | — | k_off | = | - | s-1 | - |
| CHEMBL5824909 | — | k_off | = | - | s-1 | - |
| CHEMBL5811556 | — | kon | = | - | — | - |
| CHEMBL5811556 | — | k_off | = | - | s-1 | - |
| CHEMBL3775248 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3775248 | — | kon | = | - | — | - |
| CHEMBL3775248 | — | k_off | = | - | s-1 | - |
| CHEMBL5997734 | — | k_off | = | - | s-1 | - |
| CHEMBL5831410 | — | kon | = | - | — | - |
| CHEMBL5831410 | — | k_off | = | - | s-1 | - |
| CHEMBL3775480 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3775480 | — | kon | = | - | — | - |
| CHEMBL3775480 | — | k_off | = | - | s-1 | - |
| CHEMBL5997734 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5997734 | — | kon | = | - | — | - |