Assay Detail
Binding
CHEMBL1810271
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Inhibition of recombinant human MAOB expressed in baculovirus infected insect cell microsomes using kynuramine as substrate assessed as formation of 4-hydroxyquinoline after 20 mins by fluorescence spectrophotometry
28
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
8-Aryl- and alkyloxycaffeine analogues as inhibitors of monoamine oxidase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.00 | 7.21 |
| Ki | 14 | 6.13 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1806760 | — | — | 2 | 7.35 |
| CHEMBL1806759 | — | — | 2 | 7.32 |
| CHEMBL1806768 | — | — | 2 | 6.92 |
| CHEMBL1806767 | — | — | 2 | 6.89 |
| CHEMBL1806763 | — | — | 2 | 6.55 |
| CHEMBL1806765 | — | — | 2 | 6.55 |
| CHEMBL1806758 | — | — | 2 | 6.35 |
| CHEMBL1806762 | — | — | 2 | 6.00 |
| CHEMBL1400294 | — | — | 2 | 5.67 |
| CHEMBL1806761 | — | — | 2 | 5.66 |
| CHEMBL1806764 | — | — | 2 | 5.56 |
| CHEMBL1529697 | — | — | 2 | 5.11 |
| CHEMBL1806766 | — | — | 2 | 4.99 |
| CHEMBL1806757 | — | — | 2 | 4.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1806760 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL1806759 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL1806760 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1806759 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1806768 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1806767 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL1806768 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL1806767 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL1806765 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL1806763 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL1806763 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL1806765 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL1806758 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL1806758 | — | IC50 | = | 615.0 | nM | 6.21 |
| CHEMBL1806762 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1806762 | — | IC50 | = | 1365.0 | nM | 5.87 |
| CHEMBL1400294 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL1806761 | — | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL1806764 | — | Ki | = | 2760.0 | nM | 5.56 |
| CHEMBL1400294 | — | IC50 | = | 2943.0 | nM | 5.53 |
| CHEMBL1806761 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL1806764 | — | IC50 | = | 3772.0 | nM | 5.42 |
| CHEMBL1529697 | — | Ki | = | 7840.0 | nM | 5.11 |
| CHEMBL1806766 | — | Ki | = | 10350.0 | nM | 4.99 |
| CHEMBL1529697 | — | IC50 | = | 10705.0 | nM | 4.97 |
| CHEMBL1806757 | — | Ki | = | 11650.0 | nM | 4.93 |
| CHEMBL1806766 | — | IC50 | = | 14130.0 | nM | 4.85 |
| CHEMBL1806757 | — | IC50 | = | 15915.0 | nM | 4.80 |