Assay Detail
Binding
CHEMBL3383626
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BL21-DE3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
NAD-dependent protein deacetylase sirtuin-2 (CHEMBL4462) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent and selective sirtuin 2 (SIRT2) inhibitors using a fragment-based approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.84 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3343652 | — | — | 1 | 7.32 |
| CHEMBL3343653 | — | — | 1 | 7.11 |
| CHEMBL3343654 | — | — | 1 | 6.36 |
| CHEMBL3343533 | — | — | 1 | 6.36 |
| CHEMBL3343534 | — | — | 1 | 6.31 |
| CHEMBL3343656 | — | — | 1 | 6.25 |
| CHEMBL3343535 | — | — | 1 | 6.09 |
| CHEMBL3343532 | — | — | 1 | 6.06 |
| CHEMBL3343655 | — | — | 1 | 6.02 |
| CHEMBL3343651 | — | — | 1 | 6.01 |
| CHEMBL224864 | — | — | 1 | 5.81 |
| CHEMBL420311 | — | — | 1 | 5.71 |
| CHEMBL3343523 | — | — | 1 | 5.37 |
| CHEMBL3343525 | — | — | 1 | 5.20 |
| CHEMBL3343530 | — | — | 1 | 5.12 |
| CHEMBL3343531 | — | — | 1 | 5.01 |
| CHEMBL3343528 | — | — | 1 | 5.01 |
| CHEMBL1140 | NIACINAMIDE | 4.0 | 1 | 4.98 |
| CHEMBL3343526 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3343652 | — | IC50 | = | 48.3 | nM | 7.32 |
| CHEMBL3343653 | — | IC50 | = | 77.4 | nM | 7.11 |
| CHEMBL3343654 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL3343533 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL3343534 | — | IC50 | = | 489.0 | nM | 6.31 |
| CHEMBL3343656 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL3343535 | — | IC50 | = | 811.0 | nM | 6.09 |
| CHEMBL3343532 | — | IC50 | = | 869.0 | nM | 6.06 |
| CHEMBL3343655 | — | IC50 | = | 955.0 | nM | 6.02 |
| CHEMBL3343651 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL224864 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL420311 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL3343523 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3343525 | — | IC50 | = | 6290.0 | nM | 5.20 |
| CHEMBL3343530 | — | IC50 | = | 7570.0 | nM | 5.12 |
| CHEMBL3343531 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3343528 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL1140 | NIACINAMIDE | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL3343526 | — | IC50 | = | 12100.0 | nM | 4.92 |