Assay Detail
Binding
CHEMBL4766048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type EZH2 in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins followed by addition of [3H]-SAM measured after 2 hrs by Topcount scintillation proximity assay
13
Total Activities
13
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
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 |
|---|---|---|---|
| IC50 | 13 | 8.66 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4782143 | — | — | 1 | 8.80 |
| CHEMBL4797333 | — | — | 1 | 8.74 |
| CHEMBL4787149 | — | — | 1 | 8.70 |
| CHEMBL4297463 | CPI-1205 | 1.0 | 1 | 8.66 |
| CHEMBL4777385 | — | — | 1 | 8.64 |
| CHEMBL4800227 | — | — | 1 | 8.60 |
| CHEMBL4780697 | — | — | 1 | 8.48 |
| CHEMBL3605457 | — | — | 1 | - |
| CHEMBL4781657 | — | — | 1 | - |
| CHEMBL4779123 | — | — | 1 | - |
| CHEMBL4779426 | — | — | 1 | - |
| CHEMBL4799137 | — | — | 1 | - |
| CHEMBL4794859 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4782143 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4797333 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4787149 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4297463 | CPI-1205 | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4777385 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4800227 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4780697 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3605457 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4781657 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4779123 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4779426 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4799137 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4794859 | — | IC50 | < | 1.0 | nM | - |