Assay Detail
Binding
CHEMBL5353190
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-tagged human DNMT3B (564 to 853 residues)/N-terminal GST-tagged human DNMT3L (160 to 387 residues) co-expressed in baculovirus infected Sf9 cells assessed as DNA methylation using DNA oligonucleotide IDT-01 as substrate preincubated for 15 mins followed by substrate addition in presence of [3H]-SAM and measured after 4 hrs by radioactive methylation assay
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
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.19 | 4.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5428173 | — | — | 1 | 4.19 |
| CHEMBL5414585 | — | — | 1 | - |
| CHEMBL5425605 | — | — | 1 | - |
| CHEMBL5415008 | — | — | 1 | - |
| CHEMBL5404240 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5428173 | — | IC50 | = | 64700.0 | nM | 4.19 |
| CHEMBL5414585 | — | IC50 | = | 220000.0 | nM | - |
| CHEMBL5425605 | — | IC50 | = | 105000.0 | nM | - |
| CHEMBL5415008 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5404240 | — | IC50 | = | 120000.0 | nM | - |