Assay Detail
Binding
CHEMBL4479560
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human DOT1L (1 to 472 residues) preincubated for 10 mins prior addition of [3H]SAM measured after 30 mins by Beckman LS-6500 scintillation counter method
1
Total Activities
1
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
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 1 | 6.54 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171174 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171174 | — | Ki | = | 290.0 | nM | 6.54 |