Assay Detail
Binding
CHEMBL4766050
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 in human HeLa cells assessed as inhibition of trimethylation of H3K27 after 72 hrs by AlphaLISA assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 6.83 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4794859 | — | — | 1 | 7.70 |
| CHEMBL4297463 | CPI-1205 | 1.0 | 1 | 7.50 |
| CHEMBL4782143 | — | — | 1 | 7.42 |
| CHEMBL4797333 | — | — | 1 | 7.41 |
| CHEMBL3605457 | — | — | 1 | 7.10 |
| CHEMBL4779123 | — | — | 1 | 6.96 |
| CHEMBL4779426 | — | — | 1 | 6.82 |
| CHEMBL4799137 | — | — | 1 | 6.58 |
| CHEMBL4777385 | — | — | 1 | 6.54 |
| CHEMBL4800227 | — | — | 1 | 6.38 |
| CHEMBL4781657 | — | — | 1 | 6.33 |
| CHEMBL4780697 | — | — | 1 | 6.03 |
| CHEMBL4787149 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4794859 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4297463 | CPI-1205 | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4782143 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4797333 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3605457 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4779123 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4779426 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4799137 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4777385 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4800227 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4781657 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4780697 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4787149 | — | EC50 | = | 1100.0 | nM | 5.96 |