Assay Detail
Binding
CHEMBL3129168
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Inhibition of human DNMT3A2/3L using unmethylated DNA as substrate in presence of [methyl-3H]-AdoMet
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.82 | 5.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3126646 | — | — | 1 | 5.55 |
| CHEMBL2336409 | — | — | 1 | 5.00 |
| CHEMBL3126652 | — | — | 1 | 4.75 |
| CHEMBL2385821 | — | — | 1 | 4.68 |
| CHEMBL3126651 | — | — | 1 | 4.57 |
| CHEMBL3126645 | — | — | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3126646 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2336409 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3126652 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2385821 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3126651 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3126645 | — | IC50 | = | 42000.0 | nM | 4.38 |