Assay Detail
Binding
CHEMBL5536077
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Binding affinity N-terminal his tagged wild type human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry
4
Total Activities
4
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 SETDB1 (CHEMBL2321646) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SETDB1 as a cancer target: challenges and perspectives in drug design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 6.24 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5569118 | — | — | 1 | 7.10 |
| CHEMBL4449143 | — | — | 1 | 6.68 |
| CHEMBL4471748 | — | — | 1 | 5.80 |
| CHEMBL4471746 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5569118 | — | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL4449143 | — | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL4471748 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL4471746 | — | Kd | = | 4400.0 | nM | 5.36 |