Assay Detail
Binding
CHEMBL3607426
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method
22
Total Activities
22
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 | 22 | 7.29 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 9.00 |
| CHEMBL3287735 | GSK2816126 | 1.0 | 1 | 8.70 |
| CHEMBL3605457 | — | — | 1 | 8.52 |
| CHEMBL3605455 | — | — | 1 | 8.52 |
| CHEMBL3605456 | — | — | 1 | 8.40 |
| CHEMBL3605453 | — | — | 1 | 8.40 |
| CHEMBL3605454 | — | — | 1 | 8.15 |
| CHEMBL3605446 | — | — | 1 | 7.47 |
| CHEMBL3605458 | — | — | 1 | 7.40 |
| CHEMBL3605452 | — | — | 1 | 7.37 |
| CHEMBL3605445 | — | — | 1 | 7.21 |
| CHEMBL3605447 | — | — | 1 | 7.01 |
| CHEMBL3605451 | — | — | 1 | 6.93 |
| CHEMBL3605449 | — | — | 1 | 6.45 |
| CHEMBL3605448 | — | — | 1 | 6.41 |
| CHEMBL3605459 | — | — | 1 | 6.31 |
| CHEMBL3605450 | — | — | 1 | 6.29 |
| CHEMBL3605441 | — | — | 1 | 6.10 |
| CHEMBL3605442 | — | — | 1 | 5.87 |
| CHEMBL3605443 | — | — | 1 | 5.26 |
| CHEMBL3603857 | — | — | 1 | - |
| CHEMBL3605444 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3287735 | GSK2816126 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3605457 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3605455 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3605456 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3605453 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3605454 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3605446 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3605458 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3605452 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3605445 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3605447 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3605451 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3605449 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL3605448 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL3605459 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL3605450 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL3605441 | — | IC50 | = | 795.0 | nM | 6.10 |
| CHEMBL3605442 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL3605443 | — | IC50 | = | 5550.0 | nM | 5.26 |
| CHEMBL3603857 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3605444 | — | IC50 | > | 10000.0 | nM | - |