Assay Detail
Binding
CHEMBL4305698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal His6-tagged SIRT1 (Met1 to Ser747 residues) defatty-acylase activity expressed in Escherichia coli using SFP3 as substrate measured at 5 mins interval for 60 mins in presence of NAD+ by fluorescence 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
Development of Peptide-Based Sirtuin Defatty-Acylase Inhibitors Identified by the Fluorescence Probe, SFP3, That Can Efficiently Measure Defatty-Acylase Activity of Sirtuin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.19 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447813 | — | — | 1 | 7.32 |
| CHEMBL4446458 | — | — | 1 | 6.92 |
| CHEMBL4529328 | — | — | 1 | 6.57 |
| CHEMBL4438193 | — | — | 1 | 6.48 |
| CHEMBL4457496 | — | — | 1 | 6.40 |
| CHEMBL4461872 | — | — | 1 | 5.96 |
| CHEMBL4553811 | — | — | 1 | 5.85 |
| CHEMBL4449389 | — | — | 1 | 5.77 |
| CHEMBL1140 | NIACINAMIDE | 4.0 | 1 | 4.48 |
| CHEMBL4458848 | — | — | 1 | - |
| CHEMBL4448993 | — | — | 1 | - |
| CHEMBL4574491 | — | — | 1 | - |
| CHEMBL4445565 | — | — | 1 | - |
| CHEMBL4464941 | — | — | 1 | - |
| CHEMBL3770903 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447813 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4446458 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4529328 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4438193 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4457496 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4461872 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4553811 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4449389 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1140 | NIACINAMIDE | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4458848 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4448993 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4574491 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4445565 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4464941 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3770903 | — | IC50 | > | 10000.0 | nM | - |