Assay Detail
Binding
CHEMBL3783356
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant His6 tagged human SIRT2 using 0.39 mM H2N-HK-[N(epsilon)-acetyl-lysine]-LM-COOH as substrate measured after 12 mins HPLC analysis in presence of 0.5 mM beta-NAD+
7
Total Activities
7
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
NAD-dependent protein deacetylase sirtuin-2 (CHEMBL4462) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Simple N(ε)-thioacetyl-lysine-containing cyclic peptides exhibiting highly potent sirtuin inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.01 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3781485 | — | — | 1 | 8.00 |
| CHEMBL3781226 | — | — | 1 | 7.28 |
| CHEMBL3780405 | — | — | 1 | 7.23 |
| CHEMBL3780552 | — | — | 1 | 6.87 |
| CHEMBL3781397 | — | — | 1 | 6.84 |
| CHEMBL3781645 | — | — | 1 | 6.48 |
| CHEMBL3781129 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3781485 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL3781226 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL3780405 | — | IC50 | = | 58.9 | nM | 7.23 |
| CHEMBL3780552 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL3781397 | — | IC50 | = | 143.6 | nM | 6.84 |
| CHEMBL3781645 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL3781129 | — | IC50 | = | 404.3 | nM | 6.39 |