Assay Detail
Binding
CHEMBL4353604
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His-tagged SIRT2 expressed in Escherichia coli using p53 (Gln-Pro-Lys-Lys(Ac)) (317 to 320 residues) as substrate incubated for 3 hrs measured up to 30 mins by fluorescence assay
6
Total Activities
6
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
Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD<sup>+</sup>-Binding Site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.23 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770903 | — | — | 1 | 6.52 |
| CHEMBL4465620 | — | — | 1 | 6.51 |
| CHEMBL4471909 | — | — | 1 | 6.43 |
| CHEMBL4516553 | — | — | 1 | 6.22 |
| CHEMBL4589851 | — | — | 1 | 5.93 |
| CHEMBL2152613 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770903 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4465620 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4471909 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4516553 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4589851 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL2152613 | — | IC50 | = | 1740.0 | nM | 5.76 |