Assay Detail
Binding
CHEMBL3418012
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His6-tagged human recombinant DNMT1 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
13
Total Activities
13
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 1 (CHEMBL1993) ↗| 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 | 13 | 5.18 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | 3.0 | 1 | 6.30 |
| CHEMBL318782 | Dichlon | — | 1 | 5.80 |
| CHEMBL3414630 | — | — | 1 | 5.40 |
| CHEMBL2336409 | — | — | 1 | 5.22 |
| CHEMBL3126646 | — | — | 1 | 5.05 |
| CHEMBL3414633 | — | — | 1 | 4.92 |
| CHEMBL3414632 | — | — | 1 | 4.72 |
| CHEMBL3414631 | — | — | 1 | 4.70 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 4.52 |
| CHEMBL1564869 | — | — | 1 | - |
| CHEMBL1916517 | — | — | 1 | - |
| CHEMBL403716 | — | — | 1 | - |
| CHEMBL640 | PROCAINAMIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL318782 | Dichlon | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3414630 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2336409 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3126646 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3414633 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3414632 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3414631 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL44 | GENISTEIN | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1564869 | — | IC50 | = | 390000.0 | nM | - |
| CHEMBL1916517 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL403716 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL640 | PROCAINAMIDE | IC50 | > | 500000.0 | nM | - |