Assay Detail
Binding
CHEMBL4480254
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged human SETD8 (191 to 352 residues) expressed in Escherichia coli Rosseta-2(DE3) cells using histone peptide substrate preincubated for 10 mins followed by substrate addition in presence of [3H-Me]SAM by liquid scintillation counting method
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 |
Publication
Design, synthesis, and protein methyltransferase activity of a unique set of constrained amine containing compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.38 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337173 | — | — | 1 | 6.68 |
| CHEMBL3414625 | — | — | 1 | 6.30 |
| CHEMBL580421 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337173 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3414625 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL580421 | — | IC50 | = | 700.0 | nM | 6.16 |