Assay Detail
Binding
CHEMBL5503836
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Sirt2 (56 to 356 residues) deacetylation expressed in Escherichia coli BL21 (DE3) using ZMAL as substrate incubated for 4 hrs in presence of NAD+ by fluorescence based microplate reader 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
Structure-Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD<sup>+</sup>-Dependent Lysine Deacylase Sirtuin 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.16 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227437 | — | — | 1 | 6.92 |
| CHEMBL5558057 | — | — | 1 | 6.92 |
| CHEMBL5558796 | — | — | 1 | 6.68 |
| CHEMBL5556332 | — | — | 1 | 6.46 |
| CHEMBL5531984 | — | — | 1 | 6.37 |
| CHEMBL5532186 | — | — | 1 | 6.22 |
| CHEMBL5556968 | — | — | 1 | 6.21 |
| CHEMBL5512474 | — | — | 1 | 6.19 |
| CHEMBL5505814 | — | — | 1 | 6.17 |
| CHEMBL5555774 | — | — | 1 | 6.06 |
| CHEMBL5505752 | — | — | 1 | 6.05 |
| CHEMBL5558824 | — | — | 1 | 5.97 |
| CHEMBL5555401 | — | — | 1 | 5.96 |
| CHEMBL3431191 | — | — | 1 | 5.44 |
| CHEMBL5542182 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227437 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5558057 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5558796 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5556332 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5531984 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5532186 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5556968 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5512474 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5505814 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL5555774 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL5505752 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5558824 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL5555401 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3431191 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5542182 | — | IC50 | = | 17800.0 | nM | 4.75 |