Assay Detail
Binding
CHEMBL5164095
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Inhibition of human recombinant MAO-B using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorometric analysis
30
Total Activities
30
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
Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.71 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5174789 | — | — | 1 | 9.15 |
| CHEMBL5209131 | — | — | 1 | 9.10 |
| CHEMBL5178803 | — | — | 1 | 8.74 |
| CHEMBL5191709 | — | — | 1 | 8.60 |
| CHEMBL5177167 | — | — | 1 | 8.60 |
| CHEMBL5206513 | — | — | 1 | 8.47 |
| CHEMBL5187034 | — | — | 1 | 8.34 |
| CHEMBL5199814 | — | — | 1 | 8.30 |
| CHEMBL5187539 | — | — | 1 | 8.28 |
| CHEMBL396778 | SAFINAMIDE | 4.0 | 1 | 8.15 |
| CHEMBL5200705 | — | — | 1 | 8.05 |
| CHEMBL5181534 | — | — | 1 | 8.05 |
| CHEMBL5189255 | — | — | 1 | 7.96 |
| CHEMBL5201892 | — | — | 1 | 7.96 |
| CHEMBL5192912 | — | — | 1 | 7.89 |
| CHEMBL887 | RASAGILINE | 4.0 | 1 | 7.81 |
| CHEMBL5188859 | — | — | 1 | 7.80 |
| CHEMBL5173511 | — | — | 1 | 7.80 |
| CHEMBL5191838 | — | — | 1 | 7.43 |
| CHEMBL5175763 | — | — | 1 | 7.38 |
| CHEMBL5193874 | — | — | 1 | 7.35 |
| CHEMBL5193046 | — | — | 1 | 7.26 |
| CHEMBL5190792 | — | — | 1 | 7.05 |
| CHEMBL5197407 | — | — | 1 | 7.02 |
| CHEMBL5195779 | — | — | 1 | 6.94 |
| CHEMBL5182953 | — | — | 1 | 6.90 |
| CHEMBL5177787 | — | — | 1 | 6.70 |
| CHEMBL5171313 | — | — | 1 | 6.54 |
| CHEMBL5183690 | — | — | 1 | 5.94 |
| CHEMBL4125735 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5174789 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5209131 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5178803 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5191709 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5177167 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5206513 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5187034 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5199814 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5187539 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL396778 | SAFINAMIDE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5200705 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5181534 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5189255 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5201892 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5192912 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL887 | RASAGILINE | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL5188859 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5173511 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5191838 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5175763 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5193874 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5193046 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5190792 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5197407 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5195779 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5182953 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5177787 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL5171313 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL5183690 | — | IC50 | = | 1142.0 | nM | 5.94 |
| CHEMBL4125735 | — | IC50 | = | 1601.0 | nM | 5.80 |