Assay Detail
Binding
CHEMBL5159712
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His/GST-tagged human LSD1 (172 to 852 residues) expressed in expressed in baculovirus infected insect cells using biotinylated H3K4Me2 peptide as substrate by TR-FRET assay
29
Total Activities
29
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
Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 4.48 | 5.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5208082 | — | — | 1 | 5.06 |
| CHEMBL5201504 | — | — | 1 | 4.82 |
| CHEMBL5174650 | — | — | 1 | 4.81 |
| CHEMBL5206450 | — | — | 1 | 4.77 |
| CHEMBL5170011 | — | — | 1 | 4.61 |
| CHEMBL5170567 | — | — | 1 | 4.60 |
| CHEMBL5205837 | — | — | 1 | 4.55 |
| CHEMBL5181753 | — | — | 1 | 4.54 |
| CHEMBL5196436 | — | — | 1 | 4.52 |
| CHEMBL5191047 | — | — | 1 | 4.47 |
| CHEMBL5183291 | — | — | 1 | 4.47 |
| CHEMBL5172252 | — | — | 1 | 4.42 |
| CHEMBL5191605 | — | — | 1 | 4.41 |
| CHEMBL5196564 | — | — | 1 | 4.40 |
| CHEMBL5191876 | — | — | 1 | 4.38 |
| CHEMBL5174599 | — | — | 1 | 4.37 |
| CHEMBL5204790 | — | — | 1 | 4.36 |
| CHEMBL5194745 | — | — | 1 | 4.32 |
| CHEMBL5175125 | — | — | 1 | 4.31 |
| CHEMBL5184995 | — | — | 1 | 4.30 |
| CHEMBL5197243 | — | — | 1 | 4.21 |
| CHEMBL5171190 | — | — | 1 | 4.20 |
| CHEMBL5177857 | — | — | 1 | 4.17 |
| CHEMBL5176847 | — | — | 1 | - |
| CHEMBL5188749 | — | — | 1 | - |
| CHEMBL5177765 | — | — | 1 | - |
| CHEMBL5200994 | — | — | 1 | - |
| CHEMBL5196822 | — | — | 1 | - |
| CHEMBL3786182 | GSK2879552 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5208082 | — | IC50 | = | 8720.0 | nM | 5.06 |
| CHEMBL5201504 | — | IC50 | = | 15250.0 | nM | 4.82 |
| CHEMBL5174650 | — | IC50 | = | 15640.0 | nM | 4.81 |
| CHEMBL5206450 | — | IC50 | = | 17101.0 | nM | 4.77 |
| CHEMBL5170011 | — | IC50 | = | 24430.0 | nM | 4.61 |
| CHEMBL5170567 | — | IC50 | = | 25010.0 | nM | 4.60 |
| CHEMBL5205837 | — | IC50 | = | 28170.0 | nM | 4.55 |
| CHEMBL5181753 | — | IC50 | = | 28810.0 | nM | 4.54 |
| CHEMBL5196436 | — | IC50 | = | 29900.0 | nM | 4.52 |
| CHEMBL5191047 | — | IC50 | = | 33610.0 | nM | 4.47 |
| CHEMBL5183291 | — | IC50 | = | 33630.0 | nM | 4.47 |
| CHEMBL5172252 | — | IC50 | = | 38241.0 | nM | 4.42 |
| CHEMBL5191605 | — | IC50 | = | 38850.0 | nM | 4.41 |
| CHEMBL5196564 | — | IC50 | = | 39490.0 | nM | 4.40 |
| CHEMBL5191876 | — | IC50 | = | 41570.0 | nM | 4.38 |
| CHEMBL5174599 | — | IC50 | = | 42530.0 | nM | 4.37 |
| CHEMBL5204790 | — | IC50 | = | 43600.0 | nM | 4.36 |
| CHEMBL5194745 | — | IC50 | = | 47540.0 | nM | 4.32 |
| CHEMBL5175125 | — | IC50 | = | 48640.0 | nM | 4.31 |
| CHEMBL5184995 | — | IC50 | = | 50280.0 | nM | 4.30 |
| CHEMBL5197243 | — | IC50 | = | 62210.0 | nM | 4.21 |
| CHEMBL5171190 | — | IC50 | = | 62920.0 | nM | 4.20 |
| CHEMBL5177857 | — | IC50 | = | 68150.0 | nM | 4.17 |
| CHEMBL5176847 | — | IC50 | = | 261050.0 | nM | - |
| CHEMBL5188749 | — | IC50 | = | 164000.0 | nM | - |
| CHEMBL5177765 | — | IC50 | = | 222900.0 | nM | - |
| CHEMBL5200994 | — | IC50 | = | 334500.0 | nM | - |
| CHEMBL5196822 | — | IC50 | = | 353800.0 | nM | - |
| CHEMBL3786182 | GSK2879552 | IC50 | = | 403900.0 | nM | - |