Assay Detail
Binding
CHEMBL1799832
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant SIRT1 expressed in Escherichia coli incubated at 37 degC for 2 hrs by Fluor de Lys fluorescence assay
8
Total Activities
8
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
Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.61 | 5.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL596657 | — | — | 1 | 5.08 |
| CHEMBL1797739 | — | — | 1 | 4.91 |
| CHEMBL1797748 | — | — | 1 | 4.76 |
| CHEMBL491960 | CAMBINOL | — | 1 | 4.24 |
| CHEMBL490905 | — | — | 1 | 4.05 |
| CHEMBL1797725 | — | — | 1 | - |
| CHEMBL1797726 | — | — | 1 | - |
| CHEMBL1797737 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL596657 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL1797739 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL1797748 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL491960 | CAMBINOL | IC50 | = | 57900.0 | nM | 4.24 |
| CHEMBL490905 | — | IC50 | = | 89800.0 | nM | 4.05 |
| CHEMBL1797725 | — | IC50 | - | — | - | |
| CHEMBL1797726 | — | IC50 | - | — | - | |
| CHEMBL1797737 | — | IC50 | = | 112000.0 | nM | - |