Assay Detail
Binding
CHEMBL3399055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminally FLAG-tagged EZH2 Y641N mutant in EZH2/SUZ12/EED/RbAp48 complex (unknown origin) expressed in baculovirus infected in SF9 cells assessed as inhibition of methylation of nucleosomes at H3K27 by scintillation counting in presence of [3H]SAM
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SAH derived potent and selective EZH2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.02 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3397332 | — | — | 1 | 7.16 |
| CHEMBL3397325 | — | — | 1 | 6.22 |
| CHEMBL3397329 | — | — | 1 | 6.00 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 5.72 |
| CHEMBL3397327 | — | — | 1 | 5.55 |
| CHEMBL3397330 | — | — | 1 | 5.44 |
| CHEMBL3397331 | — | — | 1 | - |
| CHEMBL3397328 | — | — | 1 | - |
| CHEMBL3397326 | — | — | 1 | - |
| CHEMBL3397324 | — | — | 1 | - |
| CHEMBL3397323 | — | — | 1 | - |
| CHEMBL3397320 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3397332 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3397325 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3397329 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3397327 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3397330 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3397331 | — | IC50 | - | — | - | |
| CHEMBL3397328 | — | IC50 | - | — | - | |
| CHEMBL3397326 | — | IC50 | - | — | - | |
| CHEMBL3397324 | — | IC50 | - | — | - | |
| CHEMBL3397323 | — | IC50 | - | — | - | |
| CHEMBL3397320 | — | IC50 | - | — | - |