Assay Detail
Binding
CHEMBL1036444
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Inhibition of human recombinant DNMT1
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
DNA (cytosine-5)-methyltransferase 1 (CHEMBL1993) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.10 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.10 |
| CHEMBL560106 | — | — | 1 | 6.09 |
| CHEMBL557902 | — | — | 1 | 5.96 |
| CHEMBL559283 | — | — | 1 | 5.60 |
| CHEMBL555257 | — | — | 1 | 5.43 |
| CHEMBL551578 | — | — | 1 | 5.40 |
| CHEMBL551167 | — | — | 1 | 5.35 |
| CHEMBL564052 | — | — | 1 | 5.32 |
| CHEMBL560768 | — | — | 1 | 5.30 |
| CHEMBL555352 | — | — | 1 | 5.27 |
| CHEMBL550440 | — | — | 1 | 5.10 |
| CHEMBL551174 | — | — | 1 | 4.82 |
| CHEMBL563938 | — | — | 1 | 4.75 |
| CHEMBL563782 | — | — | 1 | 4.72 |
| CHEMBL562689 | — | — | 1 | 4.51 |
| CHEMBL538627 | — | — | 1 | 4.44 |
| CHEMBL551100 | — | — | 1 | 4.36 |
| CHEMBL539449 | — | — | 1 | 4.36 |
| CHEMBL559281 | — | — | 1 | 4.03 |
| CHEMBL564490 | — | — | 1 | - |
| CHEMBL538693 | — | — | 1 | - |
| CHEMBL558883 | — | — | 1 | - |
| CHEMBL563888 | — | — | 1 | - |
| CHEMBL551787 | — | — | 1 | - |
| CHEMBL563230 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL560106 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL557902 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL559283 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL555257 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL551578 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL551167 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL564052 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL560768 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL555352 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL550440 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL551174 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL563938 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL563782 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL562689 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL538627 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL551100 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL539449 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL559281 | — | IC50 | = | 94000.0 | nM | 4.03 |
| CHEMBL564490 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL538693 | — | IC50 | > | 45000.0 | nM | - |
| CHEMBL558883 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL563888 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL551787 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL563230 | — | IC50 | > | 100000.0 | nM | - |