Assay Detail
Functional
CHEMBL5584492
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Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KARPAS-422 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.72 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598486 | — | — | 1 | 9.01 |
| CHEMBL5596736 | — | — | 1 | 8.75 |
| CHEMBL5598282 | — | — | 1 | 8.74 |
| CHEMBL5596732 | — | — | 1 | 8.72 |
| CHEMBL5598381 | — | — | 1 | 8.66 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 8.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598486 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5596736 | — | IC50 | = | 1.79 | nM | 8.75 |
| CHEMBL5598282 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5596732 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5598381 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 3.86 | nM | 8.41 |