Assay Detail
Binding
CHEMBL5318868
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 (unknown origin) using SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 4 hrs by HTRF analysis
3
Total Activities
3
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
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.75 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 7.66 |
| CHEMBL5422549 | — | — | 1 | 6.60 |
| CHEMBL5415704 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5422549 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5415704 | — | IC50 | = | 1040.0 | nM | 5.98 |