Assay Detail
Binding
CHEMBL4479463
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EZH1 histone methyltransferase activity of EZH1/EED/SUZ12/RBBP4/AEBP2 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 EZH1 (CHEMBL2189116) ↗| 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 | 6.64 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4594174 | — | — | 1 | 7.22 |
| CHEMBL3414619 | — | — | 1 | 7.16 |
| CHEMBL4567859 | — | — | 1 | 7.07 |
| CHEMBL4557033 | — | — | 1 | 7.06 |
| CHEMBL4559875 | — | — | 1 | 6.97 |
| CHEMBL4545986 | — | — | 1 | 6.90 |
| CHEMBL4539055 | — | — | 1 | 6.90 |
| CHEMBL4554286 | — | — | 1 | 6.80 |
| CHEMBL4551319 | — | — | 1 | 6.68 |
| CHEMBL4521710 | — | — | 1 | 6.50 |
| CHEMBL4559801 | — | — | 1 | 6.50 |
| CHEMBL4529085 | — | — | 1 | 6.41 |
| CHEMBL4569399 | — | — | 1 | 6.21 |
| CHEMBL4542135 | — | — | 1 | 6.17 |
| CHEMBL4593352 | — | — | 1 | 6.11 |
| CHEMBL4544978 | — | — | 1 | 6.09 |
| CHEMBL4575460 | — | — | 1 | 6.06 |
| CHEMBL4554500 | — | — | 1 | - |
| CHEMBL4535507 | — | — | 1 | - |
| CHEMBL4566302 | — | — | 1 | - |
| CHEMBL4520484 | — | — | 1 | - |
| CHEMBL4577352 | — | — | 1 | - |
| CHEMBL4527307 | — | — | 1 | - |
| CHEMBL4572342 | — | — | 1 | - |
| CHEMBL4561884 | — | — | 1 | - |
| CHEMBL4568471 | — | — | 1 | - |
| CHEMBL4521620 | — | — | 1 | - |
| CHEMBL4535050 | — | — | 1 | - |
| CHEMBL4533229 | — | — | 1 | - |
| CHEMBL4535178 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4594174 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3414619 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4567859 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4557033 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4559875 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4545986 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4539055 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4554286 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4551319 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4521710 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL4559801 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4529085 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL4569399 | — | IC50 | = | 613.0 | nM | 6.21 |
| CHEMBL4542135 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL4593352 | — | IC50 | = | 773.0 | nM | 6.11 |
| CHEMBL4544978 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4575460 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4518847 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4524767 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4521009 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4542936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4593180 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4590919 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4539350 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4542524 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4532360 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4538520 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4525296 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4549862 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4515987 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4591568 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4563038 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4534613 | — | IC50 | > | 1250.0 | nM | - |
| CHEMBL4568471 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4554500 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4535507 | — | IC50 | > | 1250.0 | nM | - |
| CHEMBL4566302 | — | IC50 | > | 1250.0 | nM | - |
| CHEMBL4520484 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4577352 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4527307 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4572342 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4561884 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4483642 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4521620 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4535050 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4533229 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4535178 | — | IC50 | > | 1250.0 | nM | - |
| CHEMBL4532174 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4584071 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4581179 | — | IC50 | > | 10000.0 | nM | - |