Assay Detail
Binding
CHEMBL4833634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay
28
Total Activities
28
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
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.34 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4852135 | — | — | 1 | 8.00 |
| CHEMBL3414621 | TAZEMETOSTAT | 4.0 | 1 | 7.96 |
| CHEMBL4847202 | — | — | 1 | 7.93 |
| CHEMBL4863309 | — | — | 1 | 7.92 |
| CHEMBL3287735 | GSK2816126 | 1.0 | 1 | 7.89 |
| CHEMBL4855107 | — | — | 1 | 7.82 |
| CHEMBL4861991 | — | — | 1 | 7.80 |
| CHEMBL4856680 | — | — | 1 | 7.78 |
| CHEMBL4872040 | — | — | 1 | 7.78 |
| CHEMBL4854228 | — | — | 1 | 7.72 |
| CHEMBL4845841 | — | — | 1 | 7.60 |
| CHEMBL4858611 | — | — | 1 | 7.60 |
| CHEMBL4862681 | — | — | 1 | 7.58 |
| CHEMBL4867934 | — | — | 1 | 7.47 |
| CHEMBL4855553 | — | — | 1 | 7.47 |
| CHEMBL4877191 | — | — | 1 | 7.42 |
| CHEMBL4867160 | — | — | 1 | 7.39 |
| CHEMBL4875650 | — | — | 1 | 7.33 |
| CHEMBL4871035 | — | — | 1 | 7.32 |
| CHEMBL4878548 | — | — | 1 | 7.29 |
| CHEMBL4856249 | — | — | 1 | 6.76 |
| CHEMBL4876399 | — | — | 1 | 6.74 |
| CHEMBL4875376 | — | — | 1 | 6.70 |
| CHEMBL4858107 | — | — | 1 | 6.62 |
| CHEMBL4857521 | — | — | 1 | 6.43 |
| CHEMBL4875308 | — | — | 1 | 6.40 |
| CHEMBL4851199 | — | — | 1 | 6.40 |
| CHEMBL4852631 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4852135 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL3414621 | TAZEMETOSTAT | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4847202 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4863309 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3287735 | GSK2816126 | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL4855107 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL4861991 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4856680 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL4872040 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL4854228 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4845841 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL4858611 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL4862681 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL4867934 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL4855553 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL4877191 | — | IC50 | = | 37.6 | nM | 7.42 |
| CHEMBL4867160 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL4875650 | — | IC50 | = | 47.3 | nM | 7.33 |
| CHEMBL4871035 | — | IC50 | = | 47.7 | nM | 7.32 |
| CHEMBL4878548 | — | IC50 | = | 51.7 | nM | 7.29 |
| CHEMBL4856249 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL4876399 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4875376 | — | IC50 | = | 198.7 | nM | 6.70 |
| CHEMBL4858107 | — | IC50 | = | 238.1 | nM | 6.62 |
| CHEMBL4857521 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL4875308 | — | IC50 | = | 394.2 | nM | 6.40 |
| CHEMBL4851199 | — | IC50 | = | 396.4 | nM | 6.40 |
| CHEMBL4852631 | — | IC50 | = | 404.2 | nM | 6.39 |