Assay Detail
Binding
CHEMBL3271452
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Inhibition of EZH2 Y641N mutant (unknown origin)
13
Total Activities
13
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 and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.54 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3264788 | — | — | 1 | 6.89 |
| CHEMBL3264787 | — | — | 1 | 6.72 |
| CHEMBL3264786 | — | — | 1 | 6.25 |
| CHEMBL3264783 | — | — | 1 | 5.85 |
| CHEMBL3264795 | — | — | 1 | 5.70 |
| CHEMBL3264784 | — | — | 1 | 5.66 |
| CHEMBL3264794 | — | — | 1 | 5.60 |
| CHEMBL3264785 | — | — | 1 | 5.40 |
| CHEMBL3264792 | — | — | 1 | 5.00 |
| CHEMBL3264793 | — | — | 1 | 5.00 |
| CHEMBL3264789 | — | — | 1 | 4.21 |
| CHEMBL3264791 | — | — | 1 | 4.18 |
| CHEMBL3264790 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3264788 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3264787 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3264786 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3264783 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3264795 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3264784 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3264794 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3264785 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3264792 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3264793 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3264789 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL3264791 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL3264790 | — | IC50 | > | 80000.0 | nM | - |