Assay Detail
Binding
CHEMBL2175606
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assay
3
Total Activities
3
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
Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 7.02 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171169 | — | — | 1 | 7.18 |
| CHEMBL2171170 | — | — | 1 | 7.07 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171169 | — | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL2171170 | — | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL418052 | S-ADENOSYLHOMOCYSTEINE | Kd | = | 150.0 | nM | 6.82 |