Assay Detail
Binding
CHEMBL3607427
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.67 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 7.70 |
| CHEMBL3605455 | — | — | 1 | 7.23 |
| CHEMBL3605456 | — | — | 1 | 7.12 |
| CHEMBL3605457 | — | — | 1 | 7.10 |
| CHEMBL3605453 | — | — | 1 | 7.01 |
| CHEMBL3605458 | — | — | 1 | 6.58 |
| CHEMBL3287735 | GSK2816126 | 1.0 | 1 | 6.55 |
| CHEMBL3605446 | — | — | 1 | 6.32 |
| CHEMBL3605454 | — | — | 1 | 6.25 |
| CHEMBL3605452 | — | — | 1 | 6.15 |
| CHEMBL3605451 | — | — | 1 | 6.03 |
| CHEMBL3605459 | — | — | 1 | 5.97 |
| CHEMBL3603857 | — | — | 1 | - |
| CHEMBL3605450 | — | — | 1 | - |
| CHEMBL3605449 | — | — | 1 | - |
| CHEMBL3605448 | — | — | 1 | - |
| CHEMBL3605445 | — | — | 1 | - |
| CHEMBL3605447 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3605455 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3605456 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3605457 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3605453 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3605458 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL3287735 | GSK2816126 | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3605446 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL3605454 | — | IC50 | = | 568.0 | nM | 6.25 |
| CHEMBL3605452 | — | IC50 | = | 703.0 | nM | 6.15 |
| CHEMBL3605451 | — | IC50 | = | 929.0 | nM | 6.03 |
| CHEMBL3605459 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3603857 | — | IC50 | - | — | - | |
| CHEMBL3605450 | — | IC50 | - | — | - | |
| CHEMBL3605449 | — | IC50 | - | — | - | |
| CHEMBL3605448 | — | IC50 | - | — | - | |
| CHEMBL3605445 | — | IC50 | - | — | - | |
| CHEMBL3605447 | — | IC50 | - | — | - |