Assay Detail
Binding
CHEMBL5551160
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 Y641N mutant (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 45 mins by AlphaLISA assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of novel pyridone-benzamide derivatives possessing a 1-methyl-2-benzimidazolinone moiety as potent EZH2 inhibitors for the treatment of B-cell lymphomas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 9.65 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5568736 | — | — | 1 | 10.10 |
| CHEMBL5575119 | — | — | 1 | 9.77 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 9.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5568736 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5575119 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 0.85 | nM | 9.07 |