Assay Detail
Binding
CHEMBL4479462
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH2 histone methyltransferase activity of EZH2/EED/SUZ12 protein complex (unknown origin) using histone H3 peptide as substrate (21 to 44 residues) in presence of [3H]-S-adenosylmethionine after 2 hrs by scintillation proximity assay
54
Total Activities
54
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
Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 7.13 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4569399 | — | — | 1 | 7.96 |
| CHEMBL4532174 | — | — | 1 | 7.92 |
| CHEMBL4544978 | — | — | 1 | 7.92 |
| CHEMBL4575460 | — | — | 1 | 7.77 |
| CHEMBL4593352 | — | — | 1 | 7.66 |
| CHEMBL4542135 | — | — | 1 | 7.62 |
| CHEMBL4529085 | — | — | 1 | 7.60 |
| CHEMBL4535178 | — | — | 1 | 7.58 |
| CHEMBL4532360 | — | — | 1 | 7.50 |
| CHEMBL4534613 | — | — | 1 | 7.50 |
| CHEMBL4584071 | — | — | 1 | 7.46 |
| CHEMBL4535507 | — | — | 1 | 7.39 |
| CHEMBL4533229 | — | — | 1 | 7.38 |
| CHEMBL4554500 | — | — | 1 | 7.32 |
| CHEMBL4521620 | — | — | 1 | 7.24 |
| CHEMBL4520484 | — | — | 1 | 7.19 |
| CHEMBL4566302 | — | — | 1 | 7.18 |
| CHEMBL4483642 | — | — | 1 | 7.14 |
| CHEMBL4535050 | — | — | 1 | 6.93 |
| CHEMBL4568471 | — | — | 1 | 6.83 |
| CHEMBL4539350 | — | — | 1 | 6.72 |
| CHEMBL4572342 | — | — | 1 | 6.55 |
| CHEMBL4525296 | — | — | 1 | 6.48 |
| CHEMBL4521009 | — | — | 1 | 6.42 |
| CHEMBL4521826 | — | — | 1 | 6.27 |
| CHEMBL4561884 | — | — | 1 | 6.16 |
| CHEMBL4549862 | — | — | 1 | 5.99 |
| CHEMBL4527307 | — | — | 1 | 5.95 |
| CHEMBL4594174 | — | — | 1 | - |
| CHEMBL4557033 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4569399 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4532174 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4544978 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4575460 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4593352 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4542135 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4529085 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4535178 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4532360 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4534613 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4584071 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4535507 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4533229 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4554500 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4521620 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4520484 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4566302 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4483642 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4535050 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4568471 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4539350 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4572342 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4525296 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4521009 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL4521826 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4561884 | — | IC50 | = | 697.0 | nM | 6.16 |
| CHEMBL4549862 | — | IC50 | = | 1016.0 | nM | 5.99 |
| CHEMBL4527307 | — | IC50 | = | 1111.0 | nM | 5.95 |
| CHEMBL4538395 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4588784 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4518847 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4524767 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4542936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4559801 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4590919 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4581179 | — | IC50 | > | 2300.0 | nM | - |
| CHEMBL4542524 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4538520 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4515987 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4591568 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4563038 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4551319 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4567859 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4593180 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4521710 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3414619 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4554286 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4577352 | — | IC50 | > | 1250.0 | nM | - |
| CHEMBL4557033 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4594174 | — | IC50 | < | 10.0 | nM | - |