Assay Detail
Binding
CHEMBL4628254
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Inhibition of human SET7 overexpressed in Escherichia coli BL21 (DE3) cells preincubated for 15 mins followed by addition of SAM as substrate and biotinylated Histone H3 (1-50) peptide measured after 30 mins by AlphaLISA assay relative to control
8
Total Activities
8
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 SETD7 (CHEMBL5523) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.21 | 5.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55415 | SCUTELLAREIN | — | 1 | 5.71 |
| CHEMBL28626 | MORIN | — | 1 | 5.22 |
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 5.22 |
| CHEMBL9470 | SHIKONIN | — | 1 | 4.67 |
| CHEMBL8996 | ERIODICTYOL | — | 1 | - |
| CHEMBL40919 | KAEMPFERIDE | — | 1 | - |
| CHEMBL309490 | GALANGIN | — | 1 | - |
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55415 | SCUTELLAREIN | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL28626 | MORIN | IC50 | = | 6020.0 | nM | 5.22 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL9470 | SHIKONIN | IC50 | = | 21620.0 | nM | 4.67 |
| CHEMBL8996 | ERIODICTYOL | IC50 | > | 200000.0 | nM | - |
| CHEMBL40919 | KAEMPFERIDE | IC50 | > | 200000.0 | nM | - |
| CHEMBL309490 | GALANGIN | IC50 | > | 200000.0 | nM | - |
| CHEMBL150 | KAEMPFEROL | IC50 | > | 200000.0 | nM | - |