Assay Detail
Binding
CHEMBL4432803
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DOTL1 (2 to 416 residues)-mediated methylation of nucleosome preincubated for 30 mins followed by addition of S-[methyl-3H-] adenosyl-L-methionine and nucleosome measured after 180 mins by scintillation proximity assay
10
Total Activities
10
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
Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.55 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4452414 | — | — | 1 | 7.85 |
| CHEMBL4436922 | — | — | 1 | 7.33 |
| CHEMBL4548823 | — | — | 1 | 7.05 |
| CHEMBL4446348 | — | — | 1 | 6.08 |
| CHEMBL4475242 | — | — | 1 | 6.04 |
| CHEMBL4587034 | — | — | 1 | 5.37 |
| CHEMBL4575148 | — | — | 1 | 4.41 |
| CHEMBL4434837 | — | — | 1 | 4.01 |
| CHEMBL4446675 | — | — | 1 | 3.86 |
| CHEMBL1312860 | — | — | 1 | 3.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452414 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4436922 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4548823 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4446348 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4475242 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4587034 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4575148 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4434837 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL4446675 | — | IC50 | = | 139000.0 | nM | 3.86 |
| CHEMBL1312860 | — | IC50 | = | 320000.0 | nM | 3.50 |