Assay Detail
Binding
CHEMBL2350651
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of human recombinant DOT1L (1 to 472 amino acid residues) expressed in Escherichia coli BL21 (DE3) using [3H]-SAM assessed as inhibition of nucleosome methylation incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis
2
Total Activities
2
Compounds Tested
2
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
Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 1 | 6.52 | 6.52 |
| IC50 | 1 | 6.22 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171174 | — | — | 1 | 6.52 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171174 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 600.0 | nM | 6.22 |