Assay Detail
Binding
CHEMBL5709279
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wildtype full length human SETD7 (1 to 366 residues) expressed in Escherichia coli BL21 (DE3) V2R-pRARE using biotinylated H3 (1-25) peptide as substrate incubated for 1 hrs in presence of 3H-SAM by radioactivity based assay
3
Total Activities
3
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 SETD7 (CHEMBL5523) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.22 | 8.70 |
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 |
|---|---|---|---|---|
| CHEMBL3414622 | — | — | 1 | 8.70 |
| CHEMBL5712041 | — | — | 1 | 6.96 |
| CHEMBL5712060 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414622 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5712041 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5712060 | — | IC50 | = | 1000.0 | nM | 6.00 |