Assay Detail
Binding
CHEMBL3129170
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Inhibition of human N-terminal 600 residues-deleted DNMT1 using poly(dI-dC) as substrate in presence of AdoMet
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
DNA (cytosine-5)-methyltransferase 1 (CHEMBL1993) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 12 | 5.50 | 6.92 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3126646 | — | — | 1 | 6.92 |
| CHEMBL2385821 | — | — | 1 | 6.43 |
| CHEMBL3126651 | — | — | 1 | 6.19 |
| CHEMBL2336409 | — | — | 1 | 6.07 |
| CHEMBL3126652 | — | — | 1 | 5.65 |
| CHEMBL3126645 | — | — | 1 | 5.39 |
| CHEMBL3126648 | — | — | 1 | 4.91 |
| CHEMBL3126653 | — | — | 1 | 4.55 |
| CHEMBL3126644 | — | — | 1 | 4.46 |
| CHEMBL3126649 | — | — | 1 | 4.41 |
| CHEMBL3126654 | — | — | 1 | - |
| CHEMBL3126650 | — | — | 1 | - |
| CHEMBL3126647 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3126646 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2385821 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3126651 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2336409 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL3126652 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL3126645 | — | IC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL3126648 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL3126653 | — | IC50 | = | 27900.0 | nM | 4.55 |
| CHEMBL3126644 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL3126649 | — | IC50 | = | 38600.0 | nM | 4.41 |
| CHEMBL3126654 | — | IC50 | = | 173000.0 | nM | - |
| CHEMBL3126650 | — | Inhibition | - | % | - | |
| CHEMBL3126647 | — | IC50 | = | 174000.0 | nM | - |