Assay Detail
Binding
CHEMBL3772956
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Inhibition of methyltransferase activity of human EZH2 using chicken oligonucleotide as substrate by pull down assay
48
Total Activities
48
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
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 6.29 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770000 | — | — | 1 | 8.00 |
| CHEMBL3769571 | — | — | 1 | 8.00 |
| CHEMBL3771372 | — | — | 1 | 8.00 |
| CHEMBL3770184 | — | — | 1 | 7.70 |
| CHEMBL3770820 | — | — | 1 | 7.52 |
| CHEMBL3771083 | — | — | 1 | 7.52 |
| CHEMBL3770973 | — | — | 1 | 7.52 |
| CHEMBL3771013 | — | — | 1 | 7.52 |
| CHEMBL3771343 | — | — | 1 | 7.30 |
| CHEMBL3769652 | — | — | 1 | 7.30 |
| CHEMBL3770438 | — | — | 1 | 7.10 |
| CHEMBL3771269 | — | — | 1 | 7.00 |
| CHEMBL3770154 | — | — | 1 | 7.00 |
| CHEMBL3769624 | — | — | 1 | 6.70 |
| CHEMBL3771135 | — | — | 1 | 6.70 |
| CHEMBL3770109 | — | — | 1 | 6.70 |
| CHEMBL3770788 | — | — | 1 | 6.70 |
| CHEMBL3770239 | — | — | 1 | 6.70 |
| CHEMBL3770922 | — | — | 1 | 6.52 |
| CHEMBL3769849 | — | — | 1 | 6.40 |
| CHEMBL3770619 | — | — | 1 | 6.30 |
| CHEMBL3414618 | — | — | 1 | 6.30 |
| CHEMBL3770626 | — | — | 1 | 6.16 |
| CHEMBL3770418 | — | — | 1 | 6.05 |
| CHEMBL3769599 | — | — | 1 | 6.05 |
| CHEMBL3771291 | — | — | 1 | 5.96 |
| CHEMBL3769631 | — | — | 1 | 5.80 |
| CHEMBL3771140 | — | — | 1 | 5.77 |
| CHEMBL3770059 | — | — | 1 | 5.66 |
| CHEMBL3771177 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770000 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3771372 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3769571 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3770184 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3770820 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3771083 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3770973 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3771013 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3771343 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3769652 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3770438 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3771269 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3770154 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3770239 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3771135 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3770109 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3769624 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3770788 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3770922 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3769849 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3770619 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3414618 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3770626 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3769599 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3770418 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3771291 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3769631 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3771140 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3770059 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3771177 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3770249 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3770845 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3769797 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3771043 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3771120 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3769574 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3769963 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3770081 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3769498 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3770104 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3769788 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3770929 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3769806 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3769561 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3769731 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3770275 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3769778 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3770192 | — | IC50 | > | 50000.0 | nM | - |