Assay Detail
Binding
CHEMBL5138233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DOT1L (unknown origin)
15
Total Activities
15
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
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.87 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5188291 | — | — | 1 | 9.52 |
| CHEMBL4590355 | — | — | 1 | 9.40 |
| CHEMBL5174254 | — | — | 1 | 7.89 |
| CHEMBL5197586 | — | — | 1 | 7.42 |
| CHEMBL5205286 | — | — | 1 | 7.11 |
| CHEMBL5201124 | — | — | 1 | 6.92 |
| CHEMBL5194873 | — | — | 1 | 6.00 |
| CHEMBL5172325 | — | — | 1 | 5.82 |
| CHEMBL4541986 | — | — | 1 | 5.82 |
| CHEMBL4095429 | — | — | 1 | 5.05 |
| CHEMBL5184605 | — | — | 1 | 4.58 |
| CHEMBL4534250 | — | — | 1 | - |
| CHEMBL1312860 | — | — | 1 | - |
| CHEMBL4452414 | — | — | 1 | - |
| CHEMBL5173349 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5188291 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4590355 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5174254 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5197586 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5205286 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5201124 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5194873 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5172325 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4541986 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4095429 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL5184605 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4534250 | — | IC50 | = | 1400.0 | nM | - |
| CHEMBL1312860 | — | IC50 | = | 320000.0 | nM | - |
| CHEMBL4452414 | — | IC50 | = | 14000.0 | nM | - |
| CHEMBL5173349 | — | IC50 | < | 100.0 | nM | - |