Assay Detail
Binding
CHEMBL3375362
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged human recombinant SIRT2 (34 to 356 residues) expressed in Escherichia coli BL21 using Fluor de Lys-SIRT as substrate incubated for 60 mins prior to substrate addition measured after 45 mins by fluorimetric analysis
14
Total Activities
14
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
Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.13 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3358391 | — | — | 1 | 6.22 |
| CHEMBL3358386 | — | — | 1 | 6.05 |
| CHEMBL224864 | — | — | 1 | 5.52 |
| CHEMBL3358382 | — | — | 1 | 5.48 |
| CHEMBL3358375 | — | — | 1 | 5.28 |
| CHEMBL3358384 | — | — | 1 | 5.21 |
| CHEMBL3358387 | — | — | 1 | 5.20 |
| CHEMBL3358377 | — | — | 1 | 4.96 |
| CHEMBL3358390 | — | — | 1 | 4.92 |
| CHEMBL3358385 | — | — | 1 | 4.89 |
| CHEMBL3358383 | — | — | 1 | 4.80 |
| CHEMBL3358381 | — | — | 1 | 4.66 |
| CHEMBL3358388 | — | — | 1 | 4.38 |
| CHEMBL3358389 | — | — | 1 | 4.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3358391 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3358386 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL224864 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3358382 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3358375 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3358384 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3358387 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3358377 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3358390 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3358385 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3358383 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3358381 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3358388 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL3358389 | — | IC50 | = | 57000.0 | nM | 4.24 |