Assay Detail
Binding
CHEMBL3129169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal 600 residues-deleted DNMT1 using hemimethylated (GAC)12 as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by liquid scintillation counting analysis 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 | 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 | 6 | 4.49 | 5.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3126646 | — | — | 1 | 5.05 |
| CHEMBL3126651 | — | — | 1 | 4.48 |
| CHEMBL2336409 | — | — | 1 | 4.46 |
| CHEMBL2385821 | — | — | 1 | 4.28 |
| CHEMBL3126652 | — | — | 1 | 4.17 |
| CHEMBL3126645 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3126646 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3126651 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2336409 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2385821 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL3126652 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL3126645 | — | IC50 | = | 265000.0 | nM | - |