Assay Detail
Binding
CHEMBL3134897
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containing
6
Total Activities
6
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
Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.38 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171169 | — | — | 1 | 9.14 |
| CHEMBL3087503 | — | — | 1 | 8.96 |
| CHEMBL3087502 | — | — | 1 | 8.89 |
| CHEMBL2171174 | — | — | 1 | 6.54 |
| CHEMBL3087501 | — | — | 1 | - |
| CHEMBL2169919 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171169 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL3087503 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3087502 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2171174 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL3087501 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL2169919 | — | Ki | = | 0.3 | nM | - |