Assay Detail
Binding
CHEMBL4015670
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DNMT3A catalytic domain using AdoMet assessed as reduction of methylation in 5'-biotin/3' 6-carboxyfluorescein labeled DNA duplex at CpG site after 1 hr by fluorescence assay
11
Total Activities
11
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 3A (CHEMBL1992) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.72 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4091463 | — | — | 1 | 6.52 |
| CHEMBL4070517 | — | — | 1 | 6.00 |
| CHEMBL4099197 | — | — | 1 | 5.96 |
| CHEMBL4097685 | — | — | 1 | 5.92 |
| CHEMBL4076088 | — | — | 1 | 5.85 |
| CHEMBL4070549 | — | — | 1 | 5.72 |
| CHEMBL4096869 | — | — | 1 | 5.68 |
| CHEMBL4096752 | — | — | 1 | 5.47 |
| CHEMBL4096360 | — | — | 1 | 5.36 |
| CHEMBL4084601 | — | — | 1 | 5.31 |
| CHEMBL4100095 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4091463 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4070517 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4099197 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4097685 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4076088 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4070549 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4096869 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4096752 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4096360 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4084601 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4100095 | — | EC50 | = | 6800.0 | nM | 5.17 |