Assay Detail
Binding
CHEMBL4766049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 Y641F mutant 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 | 8.42 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4781657 | — | — | 1 | 8.77 |
| CHEMBL4779426 | — | — | 1 | 8.77 |
| CHEMBL4799137 | — | — | 1 | 8.60 |
| CHEMBL3605457 | — | — | 1 | 8.55 |
| CHEMBL4297463 | CPI-1205 | 1.0 | 1 | 8.51 |
| CHEMBL4782143 | — | — | 1 | 8.48 |
| CHEMBL4797333 | — | — | 1 | 8.42 |
| CHEMBL4787149 | — | — | 1 | 8.41 |
| CHEMBL4779123 | — | — | 1 | 8.39 |
| CHEMBL4777385 | — | — | 1 | 8.32 |
| CHEMBL4780697 | — | — | 1 | 8.05 |
| CHEMBL4800227 | — | — | 1 | 7.80 |
| CHEMBL4794859 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4781657 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4779426 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4799137 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3605457 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4297463 | CPI-1205 | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4782143 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4797333 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4787149 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4779123 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4777385 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4780697 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4800227 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4794859 | — | IC50 | < | 1.0 | nM | - |