Assay Detail
Binding
CHEMBL5636913
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 Y641N mutant (unknown origin) using [3H]-SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 180 mins by AlphaLISA assay
2
Total Activities
2
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
Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of dihydropyridinone derivative as a covalent EZH2 degrader.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.72 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5641699 | — | — | 1 | 8.77 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 8.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5641699 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 2.2 | nM | 8.66 |