Assay Detail
Binding
CHEMBL5540475
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant LSD1 expressed in Escherichia coli BL21 (DE3) using H3K4me2 peptide as substrate incubated for 1 hr by fluorescence based analysis
5
Total Activities
5
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
Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.43 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4650360 | PULRODEMSTAT BESILATE | 2.0 | 1 | 9.52 |
| CHEMBL3775474 | — | — | 1 | 8.54 |
| CHEMBL4297641 | SECLIDEMSTAT | 2.0 | 1 | 7.89 |
| CHEMBL5095243 | INCB-059872 | 1.0 | 1 | 7.75 |
| CHEMBL4297289 | BOMEDEMSTAT | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4650360 | PULRODEMSTAT BESILATE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3775474 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4297641 | SECLIDEMSTAT | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5095243 | INCB-059872 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4297289 | BOMEDEMSTAT | IC50 | = | 10.0 | nM | - |