Assay Detail
Binding
CHEMBL3607425
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method
26
Total Activities
26
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, design, and synthesis of indole-based EZH2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.41 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3287735 | GSK2816126 | 1.0 | 1 | 9.00 |
| CHEMBL3605455 | — | — | 1 | 9.00 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 9.00 |
| CHEMBL3605457 | — | — | 1 | 8.70 |
| CHEMBL3605456 | — | — | 1 | 8.70 |
| CHEMBL3605454 | — | — | 1 | 8.70 |
| CHEMBL3605458 | — | — | 1 | 8.30 |
| CHEMBL3605452 | — | — | 1 | 8.30 |
| CHEMBL3605446 | — | — | 1 | 8.15 |
| CHEMBL3605445 | — | — | 1 | 7.89 |
| CHEMBL3605451 | — | — | 1 | 7.85 |
| CHEMBL3605447 | — | — | 1 | 7.66 |
| CHEMBL3264787 | — | — | 1 | 7.50 |
| CHEMBL3605459 | — | — | 1 | 7.40 |
| CHEMBL3605448 | — | — | 1 | 7.14 |
| CHEMBL3605449 | — | — | 1 | 7.12 |
| CHEMBL3605442 | — | — | 1 | 7.03 |
| CHEMBL3605441 | — | — | 1 | 6.82 |
| CHEMBL3605450 | — | — | 1 | 6.80 |
| CHEMBL3605440 | — | — | 1 | 6.37 |
| CHEMBL3605443 | — | — | 1 | 6.22 |
| CHEMBL3605444 | — | — | 1 | 5.79 |
| CHEMBL3603857 | — | — | 1 | 5.75 |
| CHEMBL3605439 | — | — | 1 | 5.75 |
| CHEMBL3605438 | — | — | 1 | 4.41 |
| CHEMBL3605453 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3287735 | GSK2816126 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3605455 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3605457 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3605456 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3605454 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3605458 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3605452 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3605446 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3605445 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3605451 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3605447 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3264787 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3605459 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3605448 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3605449 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3605442 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3605441 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3605450 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL3605440 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3605443 | — | IC50 | = | 604.0 | nM | 6.22 |
| CHEMBL3605444 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL3603857 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL3605439 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3605438 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3605453 | — | IC50 | < | 1.0 | nM | - |