Assay Detail
Binding
CHEMBL3398933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminally FLAG-tagged wild type EZH2 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
17
Total Activities
17
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 | 17 | 4.84 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3397332 | — | — | 1 | 6.57 |
| CHEMBL3397325 | — | — | 1 | 5.85 |
| CHEMBL3397329 | — | — | 1 | 5.52 |
| CHEMBL3397327 | — | — | 1 | 5.10 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 4.96 |
| CHEMBL3397330 | — | — | 1 | 4.85 |
| CHEMBL3397316 | — | — | 1 | 4.72 |
| CHEMBL3397323 | — | — | 1 | 4.62 |
| CHEMBL3397315 | — | — | 1 | 4.62 |
| CHEMBL3397324 | — | — | 1 | 4.55 |
| CHEMBL3397328 | — | — | 1 | 4.40 |
| CHEMBL3397331 | — | — | 1 | 4.40 |
| CHEMBL3397319 | — | — | 1 | 4.40 |
| CHEMBL3397326 | — | — | 1 | 4.30 |
| CHEMBL3397320 | — | — | 1 | 4.30 |
| CHEMBL3397317 | — | — | 1 | 4.22 |
| CHEMBL3397318 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3397332 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3397325 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3397329 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3397327 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3397330 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3397316 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3397323 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3397315 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3397324 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3397328 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3397331 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3397319 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3397326 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3397320 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3397317 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL3397318 | — | IC50 | = | 120000.0 | nM | - |