Assay Detail
Binding
CHEMBL5138548
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal domain DNMT3b catalytic domain (568 to 853 residues) expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inhibition of methylated dI-dC formation using poly dI-dC and [Me-3H]SAM as substrate incubated for 45 mins in presence of DNMT3L by liquid scintillation counting analysis
7
Total Activities
7
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 3B (CHEMBL6095) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and Characterization of Transition-State Analogue Inhibitors against Human DNA Methyltransferase 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.61 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178532 | — | — | 1 | 6.52 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.16 |
| CHEMBL4170114 | — | — | 1 | 5.92 |
| CHEMBL5189142 | — | — | 1 | 5.89 |
| CHEMBL5191050 | — | — | 1 | 5.18 |
| CHEMBL5187655 | — | — | 1 | 4.89 |
| CHEMBL5192832 | — | — | 1 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178532 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4170114 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5189142 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5191050 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5187655 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL5192832 | — | IC50 | = | 18200.0 | nM | 4.74 |