Assay Detail
Binding
CHEMBL2209121
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Inhibition of PRC2 complex of FLAG-EZH2, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 30 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.01 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204997 | — | — | 1 | 9.22 |
| CHEMBL2204995 | — | — | 1 | 8.92 |
| CHEMBL2204998 | — | — | 1 | 8.10 |
| CHEMBL2204996 | — | — | 1 | 7.85 |
| CHEMBL2204999 | — | — | 1 | 7.13 |
| CHEMBL1608462 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204997 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2204995 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2204998 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL2204996 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2204999 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL1608462 | — | Ki | = | 149.0 | nM | 6.83 |