Assay Detail
Binding
CHEMBL5138538
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full-length DNMT1 expressed in Sf9 cells assessed as inhibition of methylated dI-dC formation using poly dI-dC and [Me-3H]SAM as substrate incubated for 2 hrs by liquid scintillation counting analysis
18
Total Activities
18
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
Synthesis and Characterization of Transition-State Analogue Inhibitors against Human DNA Methyltransferase 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.54 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5187655 | — | — | 1 | 6.40 |
| CHEMBL4170114 | — | — | 1 | 6.40 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.16 |
| CHEMBL5189142 | — | — | 1 | 6.05 |
| CHEMBL5178532 | — | — | 1 | 5.96 |
| CHEMBL5191050 | — | — | 1 | 5.92 |
| CHEMBL5188258 | — | — | 1 | 5.57 |
| CHEMBL5193031 | — | — | 1 | 5.54 |
| CHEMBL5187336 | — | — | 1 | 5.44 |
| CHEMBL5173333 | — | — | 1 | 5.14 |
| CHEMBL5192832 | — | — | 1 | 5.07 |
| CHEMBL5200086 | — | — | 1 | 4.99 |
| CHEMBL5174871 | — | — | 1 | 4.99 |
| CHEMBL5207209 | — | — | 1 | 4.76 |
| CHEMBL5188584 | — | — | 1 | 4.71 |
| CHEMBL5189315 | — | — | 1 | - |
| CHEMBL5170757 | — | — | 1 | - |
| CHEMBL5172874 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5187655 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4170114 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5189142 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5178532 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5191050 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5188258 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5193031 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5187336 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5173333 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL5192832 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL5200086 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL5174871 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL5207209 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL5188584 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL5189315 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5170757 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5172874 | — | IC50 | > | 100000.0 | nM | - |