Assay Detail
Binding
CHEMBL5584489
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Inhibition of EZH2 (unknown origin)
19
Total Activities
19
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
Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.01 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5596528 | — | — | 1 | 9.28 |
| CHEMBL5597893 | — | — | 1 | 9.22 |
| CHEMBL5596732 | — | — | 1 | 9.21 |
| CHEMBL5598486 | — | — | 1 | 9.20 |
| CHEMBL5596736 | — | — | 1 | 9.18 |
| CHEMBL5590359 | — | — | 1 | 9.15 |
| CHEMBL5596537 | — | — | 1 | 9.08 |
| CHEMBL5598381 | — | — | 1 | 9.08 |
| CHEMBL5596669 | — | — | 1 | 9.06 |
| CHEMBL5596320 | — | — | 1 | 9.05 |
| CHEMBL5598303 | — | — | 1 | 9.03 |
| CHEMBL5596572 | — | — | 1 | 9.02 |
| CHEMBL5598282 | — | — | 1 | 9.02 |
| CHEMBL5596522 | — | — | 1 | 9.00 |
| CHEMBL5596557 | — | — | 1 | 8.99 |
| CHEMBL5597402 | — | — | 1 | 8.92 |
| CHEMBL5597808 | — | — | 1 | 8.89 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 8.80 |
| CHEMBL3770000 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5596528 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL5597893 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5596732 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5598486 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL5596736 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL5590359 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5596537 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL5598381 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL5596669 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL5596320 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5598303 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5596572 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5598282 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5596522 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL5596557 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL5597402 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL5597808 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3770000 | — | IC50 | = | 11.0 | nM | 7.96 |