Assay Detail
Binding
CHEMBL4134680
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant LSD1 (157 to 852 amino acids) (unknown origin) expressed in Escherichia coli BL21(DE) using H3K4me2 substrate by amplex red and horseradish peroxidase based fluorescence assay
7
Total Activities
7
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
Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.34 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173338 | — | — | 1 | 5.92 |
| CHEMBL4166084 | — | — | 1 | 5.66 |
| CHEMBL4176702 | — | — | 1 | 5.42 |
| CHEMBL4169910 | — | — | 1 | 5.39 |
| CHEMBL4162637 | — | — | 1 | 5.14 |
| CHEMBL313833 | — | — | 1 | 4.53 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173338 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4166084 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL4176702 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL4169910 | — | IC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL4162637 | — | IC50 | = | 7160.0 | nM | 5.14 |
| CHEMBL313833 | — | IC50 | = | 29310.0 | nM | 4.53 |
| CHEMBL98 | VORINOSTAT | IC50 | > | 100000.0 | nM | - |