Assay Detail
Binding
CHEMBL5339133
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Inhibition of recombinant human LSD1 (172 to 852 residues)/His-tagged human CoREST (286 to 482 residues) expressed in Escherichia coli BL21 (DE3) cells using ART(mK)QTARKSTGGKAPRKQLAGGK-Biotin as substrate assessed as increase in H3K4 methylation incubated for 40 mins
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.90 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775474 | — | — | 1 | 8.48 |
| CHEMBL5399284 | — | — | 1 | 8.14 |
| CHEMBL5421067 | — | — | 2 | 7.85 |
| CHEMBL5417375 | — | — | 1 | 7.34 |
| CHEMBL5403890 | — | — | 1 | 7.09 |
| CHEMBL5433869 | — | — | 1 | 6.80 |
| CHEMBL5418529 | — | — | 1 | 6.64 |
| CHEMBL5436851 | — | — | 1 | 6.57 |
| CHEMBL3775248 | — | — | 1 | 6.57 |
| CHEMBL5406255 | — | — | 1 | 6.07 |
| CHEMBL5399880 | — | — | 1 | 5.75 |
| CHEMBL5397545 | — | — | 1 | 5.43 |
| CHEMBL5421844 | — | — | 1 | - |
| CHEMBL5440326 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775474 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5399284 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5421067 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5417375 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5403890 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5421067 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5433869 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5418529 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5436851 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3775248 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5406255 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5399880 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5397545 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5421844 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5440326 | — | IC50 | > | 10000.0 | nM | - |