Assay Detail
Binding
CHEMBL4618934
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
24
Total Activities
24
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
Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 8.22 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639913 | — | — | 1 | 9.15 |
| CHEMBL4639983 | — | — | 1 | 8.74 |
| CHEMBL4638754 | — | — | 1 | 8.74 |
| CHEMBL4637958 | — | — | 1 | 8.74 |
| CHEMBL4640994 | — | — | 1 | 8.70 |
| CHEMBL4649131 | — | — | 1 | 8.62 |
| CHEMBL4639616 | — | — | 1 | 8.60 |
| CHEMBL4637572 | — | — | 1 | 8.47 |
| CHEMBL4635102 | — | — | 1 | 8.46 |
| CHEMBL4635863 | — | — | 1 | 8.46 |
| CHEMBL4633932 | — | — | 1 | 8.29 |
| CHEMBL4639569 | — | — | 1 | 8.23 |
| CHEMBL4633923 | — | — | 1 | 8.20 |
| CHEMBL4634677 | — | — | 1 | 8.17 |
| CHEMBL4635809 | — | — | 1 | 7.58 |
| CHEMBL4297463 | CPI-1205 | 1.0 | 1 | 7.55 |
| CHEMBL4639975 | — | — | 1 | 7.34 |
| CHEMBL4634390 | — | — | 1 | 7.31 |
| CHEMBL4638163 | — | — | 1 | 6.74 |
| CHEMBL4634535 | — | — | 1 | - |
| CHEMBL4633598 | — | — | 1 | - |
| CHEMBL4633053 | — | — | 1 | - |
| CHEMBL4644363 | — | — | 1 | - |
| CHEMBL4632988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639913 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4639983 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4638754 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4637958 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4640994 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4649131 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4639616 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4637572 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4635102 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4635863 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4633932 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4639569 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4633923 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4634677 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4635809 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4297463 | CPI-1205 | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4639975 | — | EC50 | = | 45.3 | nM | 7.34 |
| CHEMBL4634390 | — | EC50 | = | 48.5 | nM | 7.31 |
| CHEMBL4638163 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4634535 | — | EC50 | > | 304.0 | nM | - |
| CHEMBL4633598 | — | EC50 | > | 304.0 | nM | - |
| CHEMBL4633053 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4644363 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4632988 | — | EC50 | < | 100.0 | nM | - |