Assay Detail
Binding
CHEMBL1799131
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His-tagged full length LSD1 expressed in Escherichia coli BL21 (DE3) assessed as inactivation constant preincubated for 20 mins with substrate measured after 30 mins by AmplexRed based fluorescence quenching assay
11
Total Activities
11
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 |
Target
Lysine-specific histone demethylase 1A (CHEMBL6136) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 4.75 | 5.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1795974 | — | — | 1 | 5.43 |
| CHEMBL1795982 | — | — | 1 | 5.17 |
| CHEMBL1795975 | — | — | 1 | 5.05 |
| CHEMBL1795976 | — | — | 1 | 4.93 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 4.60 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | — | 1 | 4.58 |
| CHEMBL1179 | — | — | 1 | 4.55 |
| CHEMBL1795972 | — | — | 1 | 4.38 |
| CHEMBL1795973 | — | — | 1 | 4.10 |
| CHEMBL1795983 | — | — | 1 | - |
| CHEMBL1795984 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1795974 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL1795982 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL1795975 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL1795976 | — | Ki | = | 11700.0 | nM | 4.93 |
| CHEMBL3989843 | TRANYLCYPROMINE | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | Ki | = | 26600.0 | nM | 4.58 |
| CHEMBL1179 | — | Ki | = | 28100.0 | nM | 4.55 |
| CHEMBL1795972 | — | Ki | = | 41800.0 | nM | 4.38 |
| CHEMBL1795973 | — | Ki | = | 79600.0 | nM | 4.10 |
| CHEMBL1795983 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1795984 | — | Ki | > | 100000.0 | nM | - |