Assay Detail
Binding
CHEMBL3111908
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Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assay
16
Total Activities
16
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 EHMT2 (CHEMBL6032) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.91 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3109639 | — | — | 1 | 9.05 |
| CHEMBL3109631 | — | — | 1 | 9.00 |
| CHEMBL3109630 | — | — | 1 | 8.48 |
| CHEMBL3109637 | — | — | 1 | 8.43 |
| CHEMBL3109634 | — | — | 1 | 8.32 |
| CHEMBL3109632 | — | — | 1 | 8.30 |
| CHEMBL3109638 | — | — | 1 | 7.75 |
| CHEMBL3109633 | — | — | 1 | 6.82 |
| CHEMBL3109625 | — | — | 1 | 6.82 |
| CHEMBL3109636 | — | — | 1 | 6.12 |
| CHEMBL3109635 | — | — | 1 | 5.87 |
| CHEMBL3109626 | — | — | 1 | 5.61 |
| CHEMBL3109627 | — | — | 1 | 5.45 |
| CHEMBL3109640 | — | — | 1 | 4.89 |
| CHEMBL3109629 | — | — | 1 | 4.84 |
| CHEMBL3109628 | — | — | 1 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3109639 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3109631 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3109630 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3109637 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3109634 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3109632 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3109638 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3109633 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3109625 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3109636 | — | IC50 | = | 754.0 | nM | 6.12 |
| CHEMBL3109635 | — | IC50 | = | 1342.0 | nM | 5.87 |
| CHEMBL3109626 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL3109627 | — | IC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL3109640 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL3109629 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL3109628 | — | IC50 | = | 18200.0 | nM | 4.74 |