Assay Detail
Binding
CHEMBL1067345
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Inhibition of human full length SIRT1 expressed in DE3 cells by fluorimetric 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-1 (CHEMBL4506) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and characterization of novel sirtuin inhibitor scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.19 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446446 | — | — | 1 | 6.75 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 6.22 |
| CHEMBL611953 | — | — | 1 | 6.19 |
| CHEMBL595128 | — | — | 1 | 5.22 |
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | — | 1 | 4.60 |
| CHEMBL594863 | — | — | 1 | 4.47 |
| CHEMBL82949 | — | — | 1 | 4.10 |
| CHEMBL595354 | — | — | 1 | 4.00 |
| CHEMBL592963 | — | — | 1 | - |
| CHEMBL1140 | NIACINAMIDE | 4.0 | 1 | - |
| CHEMBL380797 | SIRTINOL | — | 1 | - |
| CHEMBL611614 | — | — | 1 | - |
| CHEMBL86537 | SPLITOMICIN | — | 1 | - |
| CHEMBL491960 | CAMBINOL | — | 1 | - |
| CHEMBL508272 | SURFACTIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446446 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL265502 | SURAMIN | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL611953 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL595128 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL594863 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL82949 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL595354 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL592963 | — | IC50 | = | 570000.0 | nM | - |
| CHEMBL1140 | NIACINAMIDE | IC50 | = | 250000.0 | nM | - |
| CHEMBL380797 | SIRTINOL | IC50 | = | 120000.0 | nM | - |
| CHEMBL611614 | — | IC50 | - | — | - | |
| CHEMBL86537 | SPLITOMICIN | IC50 | > | 500000.0 | nM | - |
| CHEMBL491960 | CAMBINOL | IC50 | > | 600000.0 | nM | - |
| CHEMBL508272 | SURFACTIN | IC50 | > | 600000.0 | nM | - |