Assay Detail
Binding
CHEMBL2382555
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Inhibition of recombinant human MAO-B expressed in baculovirus-infected insect cells using p-tyramine as substrate incubated for 30 mins prior to substrate addition measured for 45 mins by amplex red reagent-based microplate fluorescence reader analysis
33
Total Activities
33
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
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.35 | 8.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2382430 | — | — | 1 | 8.79 |
| CHEMBL2382429 | — | — | 1 | 8.68 |
| CHEMBL972 | SELEGILINE | 4.0 | 1 | 8.21 |
| CHEMBL396778 | SAFINAMIDE | 4.0 | 1 | 8.12 |
| CHEMBL2382426 | — | — | 1 | 8.01 |
| CHEMBL2382428 | — | — | 1 | 7.95 |
| CHEMBL2380385 | — | — | 1 | 7.75 |
| CHEMBL26138 | — | — | 1 | 7.74 |
| CHEMBL2382434 | — | — | 1 | 7.46 |
| CHEMBL2382438 | — | — | 1 | 7.40 |
| CHEMBL2382433 | — | — | 1 | 7.36 |
| CHEMBL2380384 | — | — | 1 | 7.28 |
| CHEMBL2382425 | — | — | 1 | 7.16 |
| CHEMBL2382423 | — | — | 1 | 7.12 |
| CHEMBL2382420 | — | — | 1 | 7.03 |
| CHEMBL2382432 | — | — | 1 | 7.03 |
| CHEMBL2380386 | — | — | 1 | 7.02 |
| CHEMBL2382424 | — | — | 1 | 6.69 |
| CHEMBL2382439 | — | — | 1 | 6.62 |
| CHEMBL2382435 | — | — | 1 | 6.41 |
| CHEMBL2382431 | — | — | 1 | 6.33 |
| CHEMBL2382437 | — | — | 1 | 5.46 |
| CHEMBL2382427 | — | — | 1 | - |
| CHEMBL2382419 | — | — | 1 | - |
| CHEMBL2382418 | — | — | 1 | - |
| CHEMBL2382436 | — | — | 1 | - |
| CHEMBL2382422 | — | — | 1 | - |
| CHEMBL2382440 | — | — | 1 | - |
| CHEMBL2382441 | — | — | 1 | - |
| CHEMBL2380381 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2382430 | — | IC50 | = | 1.63 | nM | 8.79 |
| CHEMBL2382429 | — | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL972 | SELEGILINE | IC50 | = | 6.13 | nM | 8.21 |
| CHEMBL396778 | SAFINAMIDE | IC50 | = | 7.67 | nM | 8.12 |
| CHEMBL2382426 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2382428 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL2380385 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL26138 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL2382434 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL2382438 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL2382433 | — | IC50 | = | 43.7 | nM | 7.36 |
| CHEMBL2380384 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL2382425 | — | IC50 | = | 69.7 | nM | 7.16 |
| CHEMBL2382423 | — | IC50 | = | 76.4 | nM | 7.12 |
| CHEMBL2382432 | — | IC50 | = | 93.3 | nM | 7.03 |
| CHEMBL2382420 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2380386 | — | IC50 | = | 95.3 | nM | 7.02 |
| CHEMBL2382424 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL2382439 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL2382435 | — | IC50 | = | 389.0 | nM | 6.41 |
| CHEMBL2382431 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2382437 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL2382427 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382419 | — | IC50 | - | — | - | |
| CHEMBL2382418 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382436 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2382422 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382440 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2382441 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2380381 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2380382 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2380383 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382421 | — | IC50 | > | 10000.0 | nM | - |