Assay Detail
Binding
CHEMBL3783357
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant His6 tagged human SIRT3 using 0.105 mM H2N-HK-[N(epsilon)-acetyl-lysine]-LM-COOH as substrate measured after 10 mins HPLC analysis in presence of 3.5 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-3, mitochondrial (CHEMBL4461) ↗| 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 | 7.10 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3781397 | — | — | 1 | 7.37 |
| CHEMBL3781226 | — | — | 1 | 7.28 |
| CHEMBL3781129 | — | — | 1 | 7.24 |
| CHEMBL3780552 | — | — | 1 | 7.15 |
| CHEMBL3781485 | — | — | 1 | 7.08 |
| CHEMBL3780405 | — | — | 1 | 6.99 |
| CHEMBL3781645 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3781397 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL3781226 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL3781129 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL3780552 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3781485 | — | IC50 | = | 82.9 | nM | 7.08 |
| CHEMBL3780405 | — | IC50 | = | 102.6 | nM | 6.99 |
| CHEMBL3781645 | — | IC50 | = | 269.5 | nM | 6.57 |