Assay Detail
Binding
CHEMBL4305684
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Inhibition of recombinant human SIRT2 defatty-acylase activity using SFP3 as substrate measured at 5 mins interval for 60 mins in presence of NAD+ by fluorescence assay
21
Total Activities
21
Compounds Tested
2
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
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 | 20 | 6.83 | 7.72 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447813 | — | — | 1 | 7.72 |
| CHEMBL4446458 | — | — | 1 | 7.72 |
| CHEMBL4438193 | — | — | 1 | 7.66 |
| CHEMBL4457496 | — | — | 1 | 7.44 |
| CHEMBL4529328 | — | — | 1 | 7.20 |
| CHEMBL4461872 | — | — | 1 | 7.17 |
| CHEMBL4553811 | — | — | 1 | 6.92 |
| CHEMBL4449389 | — | — | 1 | 6.52 |
| CHEMBL4458848 | — | — | 1 | 6.50 |
| CHEMBL4448993 | — | — | 1 | 6.37 |
| CHEMBL4445565 | — | — | 1 | 5.82 |
| CHEMBL1140 | NIACINAMIDE | 4.0 | 1 | 4.96 |
| CHEMBL4559310 | — | — | 1 | - |
| CHEMBL3770903 | — | — | 1 | - |
| CHEMBL4590449 | — | — | 1 | - |
| CHEMBL4129995 | — | — | 1 | - |
| CHEMBL4439944 | — | — | 1 | - |
| CHEMBL4464941 | — | — | 1 | - |
| CHEMBL4465910 | — | — | 1 | - |
| CHEMBL4457681 | — | — | 1 | - |
| CHEMBL4574491 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447813 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4446458 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4438193 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4457496 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4529328 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4461872 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4553811 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4449389 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4458848 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4448993 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4445565 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1140 | NIACINAMIDE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4559310 | — | Inhibition | - | % | - | |
| CHEMBL3770903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4590449 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4129995 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4439944 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4464941 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4465910 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4457681 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4574491 | — | IC50 | > | 2000.0 | nM | - |