Assay Detail
Binding
CHEMBL4015669
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length His-tagged human DNMT1 using SAM/[methyl-3H]SAM assessed as reduction of methylation in biotinylated hemimethylated DNA duplex after 1 hr by scintillation counting method
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 1 (CHEMBL1993) ↗| 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 | 4.48 | 4.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4070549 | — | — | 1 | 4.80 |
| CHEMBL4091463 | — | — | 1 | 4.70 |
| CHEMBL4096869 | — | — | 1 | 4.62 |
| CHEMBL4097685 | — | — | 1 | 4.58 |
| CHEMBL4096752 | — | — | 1 | 4.57 |
| CHEMBL4076088 | — | — | 1 | 4.52 |
| CHEMBL4084601 | — | — | 1 | 4.50 |
| CHEMBL4096360 | — | — | 1 | 4.34 |
| CHEMBL4100095 | — | — | 1 | 4.14 |
| CHEMBL4099197 | — | — | 1 | 4.00 |
| CHEMBL4070517 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4070549 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4091463 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4096869 | — | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4097685 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4096752 | — | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4076088 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4084601 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4096360 | — | EC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL4100095 | — | EC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL4099197 | — | EC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4070517 | — | EC50 | - | — | - |