Assay Detail
Binding
CHEMBL5588902
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human LSD1 using Histone H3 as fluorometric substrate incubated for 30 mins by HRP based plate reader assay
28
Total Activities
28
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, Synthesis, and Biological Evaluation of Potent EZH2/LSD1 Dual Inhibitors for Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.54 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3906257 | — | — | 1 | 7.70 |
| CHEMBL5596715 | — | — | 1 | 7.05 |
| CHEMBL5596949 | — | — | 1 | 7.00 |
| CHEMBL5591195 | — | — | 1 | 6.92 |
| CHEMBL5597478 | — | — | 1 | 6.60 |
| CHEMBL5597625 | — | — | 1 | 6.60 |
| CHEMBL5596478 | — | — | 1 | 6.55 |
| CHEMBL5596636 | — | — | 1 | 6.40 |
| CHEMBL5596419 | — | — | 1 | 6.16 |
| CHEMBL5596605 | — | — | 1 | 6.06 |
| CHEMBL5597369 | — | — | 1 | 6.04 |
| CHEMBL5597474 | — | — | 1 | 5.98 |
| CHEMBL5596576 | — | — | 1 | 5.94 |
| CHEMBL5597207 | — | — | 1 | - |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | - |
| CHEMBL5596057 | — | — | 1 | - |
| CHEMBL5596472 | — | — | 1 | - |
| CHEMBL5589934 | — | — | 1 | - |
| CHEMBL5597134 | — | — | 1 | - |
| CHEMBL5596110 | — | — | 1 | - |
| CHEMBL5597945 | — | — | 1 | - |
| CHEMBL5598229 | — | — | 1 | - |
| CHEMBL5596727 | — | — | 1 | - |
| CHEMBL5597188 | — | — | 1 | - |
| CHEMBL5596377 | — | — | 1 | - |
| CHEMBL5596971 | — | — | 1 | - |
| CHEMBL5597949 | — | — | 1 | - |
| CHEMBL5597190 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3906257 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5596715 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5596949 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5591195 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5597478 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5597625 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5596478 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5596636 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5596419 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5596605 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL5597369 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5597474 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL5596576 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL5597207 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL3989843 | TRANYLCYPROMINE | IC50 | > | 3000.0 | nM | - |
| CHEMBL5596057 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5596472 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5589934 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5597134 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5596110 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5597945 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5598229 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5596727 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5597188 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5596377 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5596971 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5597949 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5597190 | — | IC50 | > | 3000.0 | nM | - |