Assay Detail
Binding
CHEMBL4137467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay
39
Total Activities
39
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 1 (CHEMBL1993) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.17 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201129 | DECITABINE | 4.0 | 1 | 7.52 |
| CHEMBL4163329 | — | — | 1 | 6.86 |
| CHEMBL4159597 | — | — | 1 | 6.64 |
| CHEMBL4171233 | — | — | 1 | 6.64 |
| CHEMBL4170225 | — | — | 1 | 6.63 |
| CHEMBL4160008 | — | — | 1 | 6.63 |
| CHEMBL4176464 | — | — | 1 | 6.56 |
| CHEMBL4173626 | — | — | 1 | 6.55 |
| CHEMBL1489 | AZACITIDINE | 4.0 | 1 | 6.52 |
| CHEMBL4170114 | — | — | 1 | 6.42 |
| CHEMBL4162911 | — | — | 1 | 6.38 |
| CHEMBL4173668 | — | — | 1 | 6.31 |
| CHEMBL4159604 | — | — | 1 | 6.30 |
| CHEMBL4175132 | — | — | 1 | 6.24 |
| CHEMBL4159955 | — | — | 1 | 6.21 |
| CHEMBL4162206 | — | — | 1 | 6.21 |
| CHEMBL4175084 | — | — | 1 | 6.12 |
| CHEMBL4162967 | — | — | 1 | 6.03 |
| CHEMBL4163369 | — | — | 1 | 6.03 |
| CHEMBL4177036 | — | — | 1 | 6.02 |
| CHEMBL4161915 | — | — | 1 | 6.01 |
| CHEMBL4173662 | — | — | 1 | 6.01 |
| CHEMBL4174724 | — | — | 1 | 5.98 |
| CHEMBL4166777 | — | — | 1 | 5.98 |
| CHEMBL4174677 | — | — | 1 | 5.97 |
| CHEMBL4162957 | — | — | 1 | 5.90 |
| CHEMBL4167876 | — | — | 1 | 5.90 |
| CHEMBL4166410 | — | — | 1 | 5.86 |
| CHEMBL4164497 | — | — | 1 | 5.85 |
| CHEMBL4164446 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201129 | DECITABINE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4163329 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4171233 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4159597 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4170225 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL4160008 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL4176464 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4173626 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL1489 | AZACITIDINE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4170114 | — | IC50 | = | 382.0 | nM | 6.42 |
| CHEMBL4162911 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL4173668 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL4159604 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL4175132 | — | IC50 | = | 582.0 | nM | 6.24 |
| CHEMBL4162206 | — | IC50 | = | 619.0 | nM | 6.21 |
| CHEMBL4159955 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL4175084 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL4162967 | — | IC50 | = | 945.0 | nM | 6.03 |
| CHEMBL4163369 | — | IC50 | = | 929.0 | nM | 6.03 |
| CHEMBL4177036 | — | IC50 | = | 957.0 | nM | 6.02 |
| CHEMBL4173662 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL4161915 | — | IC50 | = | 969.0 | nM | 6.01 |
| CHEMBL4174724 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL4166777 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL4174677 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4162957 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4167876 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4166410 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4164497 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4164446 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1231795 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL4170228 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL4171275 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL2336409 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL4167925 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL4166822 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2441082 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4169833 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL569864 | — | IC50 | > | 10000.0 | nM | - |