Assay Detail
Binding
CHEMBL4305697
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Inhibition of recombinant human SIRT2 deacylation activity using Fluor de Lys Sirt2 as substrate measured at 5 mins interval for 30 mins in presence of NAD+ by fluorescence assay
20
Total Activities
20
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-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 | 6.38 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4458848 | — | — | 1 | 7.17 |
| CHEMBL4446458 | — | — | 1 | 6.96 |
| CHEMBL4438193 | — | — | 1 | 6.96 |
| CHEMBL4529328 | — | — | 1 | 6.96 |
| CHEMBL4553811 | — | — | 1 | 6.92 |
| CHEMBL4129995 | — | — | 1 | 6.85 |
| CHEMBL4457496 | — | — | 1 | 6.77 |
| CHEMBL4447813 | — | — | 1 | 6.75 |
| CHEMBL4457681 | — | — | 1 | 6.72 |
| CHEMBL4465910 | — | — | 1 | 6.72 |
| CHEMBL4461872 | — | — | 1 | 6.58 |
| CHEMBL4464941 | — | — | 1 | 6.40 |
| CHEMBL4445565 | — | — | 1 | 6.24 |
| CHEMBL3770903 | — | — | 1 | 6.16 |
| CHEMBL4449389 | — | — | 1 | 5.96 |
| CHEMBL4574491 | — | — | 1 | 5.92 |
| CHEMBL4448993 | — | — | 1 | 5.80 |
| CHEMBL4590449 | — | — | 1 | 5.05 |
| CHEMBL1140 | NIACINAMIDE | 4.0 | 1 | 4.42 |
| CHEMBL4439944 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4458848 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4446458 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4438193 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4529328 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4553811 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4129995 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4457496 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4447813 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4457681 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4465910 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4461872 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4464941 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4445565 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3770903 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4449389 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4574491 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4448993 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4590449 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL1140 | NIACINAMIDE | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4439944 | — | IC50 | > | 1000.0 | nM | - |