Assay Detail
Binding
CHEMBL2176207
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant SIRT2 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay
15
Total Activities
15
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
Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.69 | 5.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224864 | — | — | 1 | 5.26 |
| CHEMBL2171194 | — | — | 1 | 4.97 |
| CHEMBL2171191 | — | — | 1 | 4.95 |
| CHEMBL596657 | — | — | 1 | 4.91 |
| CHEMBL2171193 | — | — | 1 | 4.90 |
| CHEMBL2171197 | — | — | 1 | 4.80 |
| CHEMBL2171195 | — | — | 1 | 4.77 |
| CHEMBL2171199 | — | — | 1 | 4.65 |
| CHEMBL2171198 | — | — | 1 | 4.61 |
| CHEMBL2171200 | — | — | 1 | 4.52 |
| CHEMBL2171192 | — | — | 1 | 4.52 |
| CHEMBL2171201 | — | — | 1 | 4.51 |
| CHEMBL491960 | CAMBINOL | — | 1 | 4.38 |
| CHEMBL420311 | — | — | 1 | 4.31 |
| CHEMBL2171196 | — | — | 1 | 4.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224864 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2171194 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL2171191 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL596657 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL2171193 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL2171197 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL2171195 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL2171199 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL2171198 | — | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL2171200 | — | IC50 | = | 29900.0 | nM | 4.52 |
| CHEMBL2171192 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2171201 | — | IC50 | = | 30800.0 | nM | 4.51 |
| CHEMBL491960 | CAMBINOL | IC50 | = | 42100.0 | nM | 4.38 |
| CHEMBL420311 | — | IC50 | = | 48500.0 | nM | 4.31 |
| CHEMBL2171196 | — | IC50 | = | 58500.0 | nM | 4.23 |