Assay Detail
Binding
CHEMBL5340358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EZH2 using SAM as substrate incubated for 1 hr by microplate luminescence based HMT assay
4
Total Activities
4
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 of Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.17 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 8.57 |
| CHEMBL3287735 | GSK2816126 | 1.0 | 1 | 8.49 |
| CHEMBL5410162 | — | — | 1 | 8.36 |
| CHEMBL5406071 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 2.67 | nM | 8.57 |
| CHEMBL3287735 | GSK2816126 | IC50 | = | 3.25 | nM | 8.49 |
| CHEMBL5410162 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL5406071 | — | IC50 | = | 53.32 | nM | 7.27 |