Assay Detail
Binding
CHEMBL2382556
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MAO-B in mitochondria-enriched Sprague-Dawley rat liver fractions 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 | Rattus norvegicus |
| Subcellular | Mitochondria |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Amine oxidase [flavin-containing] B (CHEMBL2993) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6.50 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL972 | SELEGILINE | 4.0 | 1 | 8.17 |
| CHEMBL396778 | SAFINAMIDE | 4.0 | 1 | 7.59 |
| CHEMBL2382426 | — | — | 1 | 7.58 |
| CHEMBL26138 | — | — | 1 | 7.42 |
| CHEMBL2380385 | — | — | 1 | 7.37 |
| CHEMBL2382429 | — | — | 1 | 7.19 |
| CHEMBL2382433 | — | — | 1 | 7.13 |
| CHEMBL2382434 | — | — | 1 | 6.73 |
| CHEMBL2382431 | — | — | 1 | 6.55 |
| CHEMBL2382425 | — | — | 1 | 6.54 |
| CHEMBL2382424 | — | — | 1 | 6.53 |
| CHEMBL2382420 | — | — | 1 | 6.49 |
| CHEMBL2382438 | — | — | 1 | 6.44 |
| CHEMBL2380386 | — | — | 1 | 6.21 |
| CHEMBL2382430 | — | — | 1 | 6.18 |
| CHEMBL2382428 | — | — | 1 | 6.14 |
| CHEMBL2382432 | — | — | 1 | 6.09 |
| CHEMBL2382440 | — | — | 1 | 6.08 |
| CHEMBL2382423 | — | — | 1 | 5.91 |
| CHEMBL2382435 | — | — | 1 | 5.89 |
| CHEMBL2382439 | — | — | 1 | 5.70 |
| CHEMBL2382437 | — | — | 1 | 5.48 |
| CHEMBL2382441 | — | — | 1 | 5.33 |
| CHEMBL2382436 | — | — | 1 | 5.16 |
| CHEMBL2380381 | — | — | 1 | - |
| CHEMBL2380382 | — | — | 1 | - |
| CHEMBL2380383 | — | — | 1 | - |
| CHEMBL2380384 | — | — | 1 | - |
| CHEMBL2382427 | — | — | 1 | - |
| CHEMBL2382421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL972 | SELEGILINE | IC50 | = | 6.74 | nM | 8.17 |
| CHEMBL396778 | SAFINAMIDE | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL2382426 | — | IC50 | = | 26.6 | nM | 7.58 |
| CHEMBL26138 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL2380385 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL2382429 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2382433 | — | IC50 | = | 73.9 | nM | 7.13 |
| CHEMBL2382434 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL2382431 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL2382425 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL2382424 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL2382420 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL2382438 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL2380386 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL2382430 | — | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL2382428 | — | IC50 | = | 725.0 | nM | 6.14 |
| CHEMBL2382432 | — | IC50 | = | 815.0 | nM | 6.09 |
| CHEMBL2382440 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL2382423 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL2382435 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2382439 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL2382437 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2382441 | — | IC50 | = | 4640.0 | nM | 5.33 |
| CHEMBL2382436 | — | IC50 | = | 6880.0 | nM | 5.16 |
| CHEMBL2380381 | — | IC50 | - | — | - | |
| CHEMBL2380382 | — | IC50 | - | — | - | |
| CHEMBL2380383 | — | IC50 | - | — | - | |
| CHEMBL2380384 | — | IC50 | - | — | - | |
| CHEMBL2382427 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382421 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382422 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382419 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2382418 | — | IC50 | - | — | - |