Assay Detail
Binding
CHEMBL4828520
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of biotinylated H3K27Me3 peptide (19 to 33 residues) binding to His-tagged EED (1 to 441 residues) (unknown origin) preincubated for 15 mins followed by H3K27Me3 addition and measured after 30 mins by alphascreen competition binding assay
35
Total Activities
35
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 |
Publication
Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.76 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4870920 | — | — | 1 | 9.70 |
| CHEMBL4865691 | — | — | 1 | 9.40 |
| CHEMBL4851576 | — | — | 1 | 9.30 |
| CHEMBL4860499 | — | — | 1 | 9.22 |
| CHEMBL4877375 | — | — | 1 | 9.22 |
| CHEMBL4869420 | — | — | 1 | 9.22 |
| CHEMBL4872891 | — | — | 1 | 9.22 |
| CHEMBL4850823 | — | — | 1 | 9.15 |
| CHEMBL4861749 | — | — | 1 | 9.15 |
| CHEMBL4859559 | — | — | 1 | 9.15 |
| CHEMBL4873268 | — | — | 1 | 9.15 |
| CHEMBL4856280 | — | — | 1 | 9.10 |
| CHEMBL4862163 | — | — | 1 | 9.10 |
| CHEMBL4878932 | — | — | 1 | 9.10 |
| CHEMBL4856160 | — | — | 1 | 9.00 |
| CHEMBL4854206 | — | — | 1 | 9.00 |
| CHEMBL4850847 | — | — | 1 | 8.96 |
| CHEMBL4847943 | — | — | 1 | 8.92 |
| CHEMBL4861394 | — | — | 1 | 8.85 |
| CHEMBL4871261 | — | — | 1 | 8.82 |
| CHEMBL4849266 | — | — | 1 | 8.80 |
| CHEMBL4858089 | — | — | 1 | 8.80 |
| CHEMBL4854800 | — | — | 1 | 8.80 |
| CHEMBL4858561 | — | — | 1 | 8.74 |
| CHEMBL4857414 | — | — | 1 | 8.49 |
| CHEMBL4855616 | — | — | 1 | 8.44 |
| CHEMBL4869720 | — | — | 1 | 8.39 |
| CHEMBL4104741 | — | — | 1 | 8.32 |
| CHEMBL4869748 | — | — | 1 | 8.04 |
| CHEMBL4877695 | — | — | 1 | 7.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4870920 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4865691 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4851576 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4860499 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4877375 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4869420 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4872891 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4850823 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4861749 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4859559 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4873268 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4856280 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4862163 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4878932 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4854206 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4856160 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4850847 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4847943 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4861394 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4871261 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4849266 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4858089 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4854800 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4858561 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4857414 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4855616 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4869720 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4104741 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4869748 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4877695 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4065484 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL4847397 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4858622 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4869208 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL4861770 | — | IC50 | = | 19.5 | nM | 7.71 |