Assay Detail
Binding
CHEMBL4048166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged DOT1L (2 to 416 residues) expressed in Escherichia coli assessed as reduction in histone H3 lysine-N-methyltransferase activity using nucleosomes after 3 hrs in presence of SAM by AlphLisa assay
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
Histone-lysine N-methyltransferase, H3 lysine-79 specific (CHEMBL1795117) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Preparation of 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives and their activity against DOT1L.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.00 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075482 | — | — | 1 | 8.20 |
| CHEMBL3414626 | PINOMETOSTAT | 2.0 | 1 | 8.11 |
| CHEMBL4079133 | — | — | 1 | 8.00 |
| CHEMBL2171169 | — | — | 1 | 7.00 |
| CHEMBL4095543 | — | — | 1 | 6.16 |
| CHEMBL4082140 | — | — | 1 | 5.84 |
| CHEMBL4100144 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075482 | — | IC50 | = | 6.34 | nM | 8.20 |
| CHEMBL3414626 | PINOMETOSTAT | IC50 | = | 7.81 | nM | 8.11 |
| CHEMBL4079133 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2171169 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4095543 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4082140 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4100144 | — | IC50 | = | 2160.0 | nM | 5.67 |