Assay Detail
Binding
CHEMBL3418013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
DNA (cytosine-5)-methyltransferase 3A (CHEMBL1992) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting DNA methylation with small molecules: what's next?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.84 | 5.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3126646 | — | — | 1 | 5.55 |
| CHEMBL2336409 | — | — | 1 | 5.10 |
| CHEMBL3414633 | — | — | 1 | 4.42 |
| CHEMBL3414632 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3126646 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2336409 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3414633 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL3414632 | — | IC50 | = | 50000.0 | nM | 4.30 |