Assay Detail
Binding
CHEMBL5654527
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Binding affinity to recombinant N-terminal DOT1L (1 to 420 residues) (unknown origin) expressed in Escherichia coli (DE3) assessed as dissociation constant by surface plasmon resonance assay
5
Total Activities
5
Compounds Tested
1
Activity Types
2
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
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 8.91 | 10.22 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3087498 | — | — | 1 | 10.22 |
| CHEMBL2169919 | — | — | 1 | 9.60 |
| CHEMBL2171169 | — | — | 1 | 8.70 |
| CHEMBL5661857 | — | — | 1 | 8.47 |
| CHEMBL5661898 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3087498 | — | Kd | = | 0.06 | nM | 10.22 |
| CHEMBL2169919 | — | Kd | = | 0.25 | nM | 9.60 |
| CHEMBL2171169 | — | Kd | = | 1.99 | nM | 8.70 |
| CHEMBL5661857 | — | Kd | = | 3.35 | nM | 8.47 |
| CHEMBL5661898 | — | Kd | = | 26.9 | nM | 7.57 |