Assay Detail
Binding
CHEMBL4618933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPATGGVKKP-NTPEGBiot peptide as substrate preincubated with [3H]SAM for 4 to 5 hrs followed by substrate addition and measured after 20 hrs by Topcount reader analysis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 |
|---|---|---|---|
| IC50 | 25 | 9.65 | 10.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639983 | — | — | 1 | 10.24 |
| CHEMBL4640994 | — | — | 1 | 10.23 |
| CHEMBL4638754 | — | — | 1 | 10.22 |
| CHEMBL4637572 | — | — | 1 | 10.20 |
| CHEMBL4635809 | — | — | 1 | 10.17 |
| CHEMBL4635863 | — | — | 1 | 10.14 |
| CHEMBL4635102 | — | — | 1 | 10.04 |
| CHEMBL4633923 | — | — | 1 | 10.00 |
| CHEMBL4639913 | — | — | 1 | 10.00 |
| CHEMBL4633932 | — | — | 1 | 9.92 |
| CHEMBL4634677 | — | — | 1 | 9.89 |
| CHEMBL4637958 | — | — | 1 | 9.85 |
| CHEMBL4649131 | — | — | 1 | 9.80 |
| CHEMBL4639569 | — | — | 1 | 9.74 |
| CHEMBL4639616 | — | — | 1 | 9.74 |
| CHEMBL4632988 | — | — | 1 | 9.70 |
| CHEMBL4633053 | — | — | 1 | 9.70 |
| CHEMBL4644363 | — | — | 1 | 9.70 |
| CHEMBL4641325 | — | — | 1 | 9.70 |
| CHEMBL4634390 | — | — | 1 | 9.31 |
| CHEMBL4638163 | — | — | 1 | 9.21 |
| CHEMBL4639975 | — | — | 1 | 9.14 |
| CHEMBL4638720 | — | — | 1 | 8.42 |
| CHEMBL4634535 | — | — | 1 | 8.39 |
| CHEMBL4633598 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639983 | — | IC50 | = | 0.057 | nM | 10.24 |
| CHEMBL4640994 | — | IC50 | = | 0.059 | nM | 10.23 |
| CHEMBL4638754 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL4637572 | — | IC50 | = | 0.063 | nM | 10.20 |
| CHEMBL4635809 | — | IC50 | = | 0.067 | nM | 10.17 |
| CHEMBL4635863 | — | IC50 | = | 0.072 | nM | 10.14 |
| CHEMBL4635102 | — | IC50 | = | 0.092 | nM | 10.04 |
| CHEMBL4633923 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4639913 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4633932 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4634677 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4637958 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4649131 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4639569 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4639616 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4632988 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4633053 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4644363 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4641325 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4634390 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL4638163 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4639975 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4638720 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4634535 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4633598 | — | IC50 | = | 19.0 | nM | 7.72 |