Assay Detail
Binding
CHEMBL4253675
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MAO-A (unknown origin) using beetle luciferin derived luminogenic substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by MAO-Glo assay
18
Total Activities
16
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
Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.55 | 6.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4292597 | — | — | 1 | 6.79 |
| CHEMBL4289408 | — | — | 2 | 6.69 |
| CHEMBL4294686 | — | — | 1 | 6.62 |
| CHEMBL4292257 | — | — | 1 | 6.51 |
| CHEMBL4281778 | — | — | 2 | 6.31 |
| CHEMBL4278271 | — | — | 1 | 6.11 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | — | 1 | 5.47 |
| CHEMBL492697 | — | — | 1 | 5.24 |
| CHEMBL4285166 | — | — | 1 | 5.01 |
| CHEMBL4288999 | — | — | 1 | 4.77 |
| CHEMBL4280740 | — | — | 1 | 4.67 |
| CHEMBL4294740 | — | — | 1 | 4.61 |
| CHEMBL4287563 | — | — | 1 | 4.55 |
| CHEMBL4283975 | — | — | 1 | 4.38 |
| CHEMBL4285989 | — | — | 1 | - |
| CHEMBL4289655 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4292597 | — | IC50 | = | 160.5 | nM | 6.79 |
| CHEMBL4289408 | — | IC50 | = | 205.5 | nM | 6.69 |
| CHEMBL4294686 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL4292257 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4281778 | — | IC50 | = | 488.5 | nM | 6.31 |
| CHEMBL4278271 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL492697 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4285166 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4288999 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL4280740 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL4294740 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL4287563 | — | IC50 | = | 27900.0 | nM | 4.55 |
| CHEMBL4283975 | — | IC50 | = | 41400.0 | nM | 4.38 |
| CHEMBL4289655 | — | IC50 | - | — | - | |
| CHEMBL4281778 | — | IC50 | - | — | - | |
| CHEMBL4285989 | — | IC50 | - | — | - | |
| CHEMBL4289408 | — | IC50 | - | — | - |