Assay Detail
Binding
CHEMBL3418015
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L 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
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Targeting DNA methylation with small molecules: what's next?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.49 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318782 | Dichlon | — | 1 | 6.30 |
| CHEMBL3414630 | — | — | 1 | 4.68 |
| CHEMBL1564869 | — | — | 1 | - |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | - |
| CHEMBL640 | PROCAINAMIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318782 | Dichlon | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3414630 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1564869 | — | IC50 | = | 315000.0 | nM | - |
| CHEMBL44 | GENISTEIN | IC50 | > | 100000.0 | nM | - |
| CHEMBL640 | PROCAINAMIDE | IC50 | > | 300000.0 | nM | - |