Assay Detail
Binding
CHEMBL1036445
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Inhibition of human recombinant DNMT3b2
21
Total Activities
21
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
Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.09 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.70 |
| CHEMBL555257 | — | — | 1 | 6.58 |
| CHEMBL557902 | — | — | 1 | 6.52 |
| CHEMBL559283 | — | — | 1 | 6.04 |
| CHEMBL550440 | — | — | 1 | 5.82 |
| CHEMBL560106 | — | — | 1 | 5.72 |
| CHEMBL558883 | — | — | 1 | 4.96 |
| CHEMBL564052 | — | — | 1 | 4.92 |
| CHEMBL538693 | — | — | 1 | 4.77 |
| CHEMBL562689 | — | — | 1 | 4.68 |
| CHEMBL551100 | — | — | 1 | 4.58 |
| CHEMBL560768 | — | — | 1 | 4.57 |
| CHEMBL551174 | — | — | 1 | 4.48 |
| CHEMBL551787 | — | — | 1 | 4.41 |
| CHEMBL563938 | — | — | 1 | 4.39 |
| CHEMBL563230 | — | — | 1 | 4.27 |
| CHEMBL559281 | — | — | 1 | 4.18 |
| CHEMBL563782 | — | — | 1 | 4.00 |
| CHEMBL539449 | — | — | 1 | - |
| CHEMBL563888 | — | — | 1 | - |
| CHEMBL538627 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL555257 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL557902 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL559283 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL550440 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL560106 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL558883 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL564052 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL538693 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL562689 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL551100 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL560768 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL551174 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL551787 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL563938 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL563230 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL559281 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL563782 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL539449 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL563888 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL538627 | — | IC50 | > | 45000.0 | nM | - |