Assay Detail
Binding
CHEMBL1046740
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Inhibition of G9a by Alpha screen assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase EHMT2 (CHEMBL6032) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.91 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572373 | — | — | 1 | 6.70 |
| CHEMBL578227 | — | — | 1 | 6.64 |
| CHEMBL569864 | — | — | 1 | 6.54 |
| CHEMBL570120 | — | — | 1 | 6.29 |
| CHEMBL571717 | — | — | 1 | 6.09 |
| CHEMBL576260 | — | — | 1 | 6.05 |
| CHEMBL568964 | — | — | 1 | 5.29 |
| CHEMBL570799 | — | — | 1 | 5.24 |
| CHEMBL585180 | — | — | 1 | 5.19 |
| CHEMBL571951 | — | — | 1 | 5.04 |
| CHEMBL570119 | — | — | 1 | - |
| CHEMBL583046 | — | — | 1 | - |
| CHEMBL568963 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572373 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL578227 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL569864 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL570120 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL571717 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL576260 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL568964 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL570799 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL585180 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL571951 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL570119 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL583046 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL568963 | — | IC50 | > | 10000.0 | nM | - |