Assay Detail
Binding
CHEMBL5709052
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 methyltransferase activity (unknown origin) in PRC2 complex using 3H-SAM as substrate by Scintillation proximity assay
9
Total Activities
9
Compounds Tested
1
Activity Types
2
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
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.11 | 8.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0010193 |
| EFO_TERM | EFO_TERM | - | — | weaver syndrome |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4593352 | — | — | 1 | 8.00 |
| CHEMBL3414629 | — | — | 1 | 7.77 |
| CHEMBL5712052 | — | — | 1 | 7.68 |
| CHEMBL4554500 | — | — | 1 | 7.20 |
| CHEMBL5712054 | — | — | 1 | 4.89 |
| CHEMBL4594174 | — | — | 1 | - |
| CHEMBL2204997 | — | — | 1 | - |
| CHEMBL4557033 | — | — | 1 | - |
| CHEMBL3414619 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4593352 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3414629 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5712052 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4554500 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5712054 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4594174 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL2204997 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4557033 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3414619 | — | IC50 | < | 10.0 | nM | - |