Assay Detail
Binding
CHEMBL4480299
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| 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
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.72 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4590355 | — | — | 1 | 7.80 |
| CHEMBL4534250 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4590355 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4534250 | — | IC50 | = | 23.0 | nM | 7.64 |