Assay Detail
Binding
CHEMBL5736639
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory Activity Assay: LSD1: A test compound dissolved in DMSO was added by to a reaction solution (50 mM Tris-HCl (pH 8.0), 0.1% BSA, 1 mM DTT) containing LSD1 enzyme, and the mixture was reacted at room temperature for 60 min. Biotin-histone H3 mono methylated K4 peptide solution (NH2-ART(me-K)QTARKSTGGKAPRKQLAGGK(Biotin)-CONH2) was added to start the reaction. After reaction at room temperature for 5 min, 2-PCPA solution was added to terminate the reaction. A detection solution (800 mM potassium fluoride, 0.1% BSA) containing europium-labeled anti-histone H3 antibody (Wako Pure Chemical Industries, Ltd.) and Streptavidin-XL665 (Cisbio) was further added, and the mixture was left standing for 60 min. A time-resolved fluorescence (excitation 320 nm, emission 615 nm, 665 nm) was measured by Envision (PerkinElmer). The LSD1 inhibitory rate (%) of the test compound was calculated by the following formula.inhibitory rate (%)=(1−(test compound count−blank)÷(control−blank))×100The count of the LSD1 enzyme reaction mixture under compound non-addition conditions is indicated as control, and the count under compound non-addition and LSD1 enzyme non-addition conditions is indicated as blank.
375
Total Activities
107
Compounds Tested
3
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
Cyclopropanamine compound and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 125 | 6.38 | 7.00 |
| kon | 125 | - | - |
| k_off | 125 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5778079 | — | — | 3 | 7.00 |
| CHEMBL3775351 | — | — | 6 | 7.00 |
| CHEMBL5983110 | — | — | 3 | 7.00 |
| CHEMBL6018178 | — | — | 3 | 7.00 |
| CHEMBL5848503 | — | — | 3 | 6.96 |
| CHEMBL5898118 | — | — | 3 | 6.92 |
| CHEMBL5964717 | — | — | 6 | 6.89 |
| CHEMBL5928368 | — | — | 3 | 6.85 |
| CHEMBL5883366 | — | — | 3 | 6.85 |
| CHEMBL5974317 | — | — | 3 | 6.82 |
| CHEMBL5887105 | — | — | 3 | 6.80 |
| CHEMBL6060068 | — | — | 3 | 6.77 |
| CHEMBL6024729 | — | — | 3 | 6.75 |
| CHEMBL6007489 | — | — | 3 | 6.75 |
| CHEMBL3775312 | — | — | 3 | 6.75 |
| CHEMBL3775480 | — | — | 15 | 6.72 |
| CHEMBL5851532 | — | — | 3 | 6.70 |
| CHEMBL5824909 | — | — | 3 | 6.68 |
| CHEMBL3774654 | — | — | 3 | 6.68 |
| CHEMBL6035130 | — | — | 3 | 6.68 |
| CHEMBL5856046 | — | — | 3 | 6.66 |
| CHEMBL5982091 | — | — | 6 | 6.64 |
| CHEMBL5797523 | — | — | 3 | 6.64 |
| CHEMBL3775248 | — | — | 3 | 6.62 |
| CHEMBL5863242 | — | — | 3 | 6.58 |
| CHEMBL5912654 | — | — | 3 | 6.58 |
| CHEMBL5914875 | — | — | 3 | 6.57 |
| CHEMBL6011057 | — | — | 3 | 6.57 |
| CHEMBL5831410 | — | — | 3 | 6.55 |
| CHEMBL5870582 | — | — | 3 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5983110 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5778079 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL6018178 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3775351 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5848503 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5898118 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5964717 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5928368 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5883366 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5974317 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5887105 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL6060068 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3775312 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL6024729 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL6007489 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3775480 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5851532 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL6035130 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3774654 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5824909 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5856046 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3775480 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5982091 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5797523 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3775248 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3775480 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5982091 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5912654 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3775480 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5863242 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5914875 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL6011057 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5831410 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5870582 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3775480 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5845394 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5857601 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5795896 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5880544 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5911578 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5966366 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3775474 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL6059512 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5838807 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5965373 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5880544 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5913395 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5797219 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5781144 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL6022437 | — | IC50 | = | 680.0 | nM | 6.17 |