Assay Detail
Binding
CHEMBL5638441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 (unknown origin)
14
Total Activities
14
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
Design, synthesis and activity evaluation of quinolinone derivatives as EZH2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.47 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5646552 | — | — | 1 | 9.03 |
| CHEMBL5646621 | — | — | 1 | 9.00 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 8.85 |
| CHEMBL5646425 | — | — | 1 | 8.78 |
| CHEMBL5647416 | — | — | 1 | 8.67 |
| CHEMBL5639947 | — | — | 1 | 8.56 |
| CHEMBL5639605 | — | — | 1 | 8.42 |
| CHEMBL5641670 | — | — | 1 | 8.38 |
| CHEMBL5639801 | — | — | 1 | 8.23 |
| CHEMBL5641753 | — | — | 1 | 8.20 |
| CHEMBL5647079 | — | — | 1 | 8.18 |
| CHEMBL5647122 | — | — | 1 | 8.13 |
| CHEMBL5641893 | — | — | 1 | 8.09 |
| CHEMBL5647466 | — | — | 1 | 8.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5646552 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5646621 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL5646425 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5647416 | — | IC50 | = | 2.12 | nM | 8.67 |
| CHEMBL5639947 | — | IC50 | = | 2.74 | nM | 8.56 |
| CHEMBL5639605 | — | IC50 | = | 3.78 | nM | 8.42 |
| CHEMBL5641670 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL5639801 | — | IC50 | = | 5.84 | nM | 8.23 |
| CHEMBL5641753 | — | IC50 | = | 6.27 | nM | 8.20 |
| CHEMBL5647079 | — | IC50 | = | 6.63 | nM | 8.18 |
| CHEMBL5647122 | — | IC50 | = | 7.42 | nM | 8.13 |
| CHEMBL5641893 | — | IC50 | = | 8.21 | nM | 8.09 |
| CHEMBL5647466 | — | IC50 | = | 8.23 | nM | 8.09 |