Assay Detail
Binding
CHEMBL4479552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DOT1L (1 to 420 amino acids) expressed in Escherichia coli
2
Total Activities
2
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 |
|---|---|---|---|
| IC50 | 2 | 7.28 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588797 | — | — | 1 | 7.89 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588797 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | IC50 | = | 220.0 | nM | 6.66 |