Assay Detail
Binding
CHEMBL4627599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type EZH2 (unknown origin) by AlphaLISA assay
28
Total Activities
28
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 and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.28 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 9.47 |
| CHEMBL4637350 | — | — | 1 | 8.11 |
| CHEMBL4646490 | — | — | 1 | 8.11 |
| CHEMBL4645357 | — | — | 1 | 7.66 |
| CHEMBL4633751 | — | — | 1 | 7.64 |
| CHEMBL4646766 | — | — | 1 | 7.57 |
| CHEMBL4647553 | — | — | 1 | 7.51 |
| CHEMBL4638443 | — | — | 1 | 7.48 |
| CHEMBL4645331 | — | — | 1 | 7.46 |
| CHEMBL4639968 | — | — | 1 | 7.41 |
| CHEMBL4644018 | — | — | 1 | 7.36 |
| CHEMBL4636556 | — | — | 1 | 7.26 |
| CHEMBL4643252 | — | — | 1 | 7.25 |
| CHEMBL4645766 | — | — | 1 | 7.22 |
| CHEMBL4640284 | — | — | 1 | 6.96 |
| CHEMBL4634950 | — | — | 1 | 6.94 |
| CHEMBL4646059 | — | — | 1 | 6.86 |
| CHEMBL4643350 | — | — | 1 | 6.84 |
| CHEMBL4633092 | — | — | 1 | 6.79 |
| CHEMBL4635610 | — | — | 1 | 6.72 |
| CHEMBL4637305 | — | — | 1 | 6.72 |
| CHEMBL4635261 | — | — | 1 | 6.65 |
| CHEMBL4649585 | — | — | 1 | 6.48 |
| CHEMBL4645698 | — | — | 1 | 6.21 |
| CHEMBL4644328 | — | — | 1 | - |
| CHEMBL4646692 | — | — | 1 | - |
| CHEMBL4642615 | — | — | 1 | - |
| CHEMBL4646348 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4637350 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4646490 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4645357 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4633751 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4646766 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4647553 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4638443 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4645331 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4639968 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4644018 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4636556 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4643252 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4645766 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4640284 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4634950 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4646059 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4643350 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4633092 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4635610 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4637305 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4635261 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL4649585 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL4645698 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4644328 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL4646692 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL4642615 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL4646348 | — | IC50 | > | 1000.0 | nM | - |