Assay Detail
Binding
CHEMBL3783355
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST-tagged human SIRT1 using 0.3 mM H2N-HK-[N(epsilon)-acetyl-lysine]-LM-COOH as substrate measured after 10 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-1 (CHEMBL4506) ↗| 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 | 7.40 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3781397 | — | — | 1 | 8.64 |
| CHEMBL3781129 | — | — | 1 | 7.43 |
| CHEMBL3781226 | — | — | 1 | 7.41 |
| CHEMBL3780405 | — | — | 1 | 7.25 |
| CHEMBL3780552 | — | — | 1 | 7.20 |
| CHEMBL3781485 | — | — | 1 | 7.12 |
| CHEMBL3781645 | — | — | 1 | 6.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3781397 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3781129 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL3781226 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL3780405 | — | IC50 | = | 56.8 | nM | 7.25 |
| CHEMBL3780552 | — | IC50 | = | 63.5 | nM | 7.20 |
| CHEMBL3781485 | — | IC50 | = | 75.2 | nM | 7.12 |
| CHEMBL3781645 | — | IC50 | = | 165.1 | nM | 6.78 |