Assay Detail
Binding
CHEMBL1017160
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Inhibition of recombinant SIRT1 preincubated for 5 mins before addition of substrate measured after 1 hr by fluorescence-based assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
NAD-dependent protein deacetylase sirtuin-1 (CHEMBL4506) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N(epsilon)-thioacetyl-lysine-containing tri-, tetra-, and pentapeptides as SIRT1 and SIRT2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.86 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL505399 | — | — | 1 | 6.75 |
| CHEMBL504310 | — | — | 1 | 6.75 |
| CHEMBL492925 | — | — | 1 | 6.66 |
| CHEMBL510904 | — | — | 1 | 6.64 |
| CHEMBL420311 | — | — | 1 | 6.55 |
| CHEMBL447677 | — | — | 1 | 6.48 |
| CHEMBL521807 | — | — | 1 | 6.48 |
| CHEMBL504711 | — | — | 1 | 6.42 |
| CHEMBL492308 | — | — | 1 | 6.32 |
| CHEMBL453807 | — | — | 1 | 6.26 |
| CHEMBL492309 | — | — | 1 | 6.24 |
| CHEMBL449883 | — | — | 1 | 6.05 |
| CHEMBL492710 | — | — | 1 | 5.85 |
| CHEMBL523676 | — | — | 1 | 5.50 |
| CHEMBL452893 | — | — | 1 | 5.37 |
| CHEMBL493160 | — | — | 1 | 5.35 |
| CHEMBL507676 | — | — | 1 | 5.30 |
| CHEMBL523498 | — | — | 1 | 5.17 |
| CHEMBL492521 | — | — | 1 | 5.06 |
| CHEMBL447852 | — | — | 1 | 4.97 |
| CHEMBL493159 | — | — | 1 | 4.96 |
| CHEMBL493355 | — | — | 1 | 4.92 |
| CHEMBL503595 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL505399 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL504310 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL492925 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL510904 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL420311 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL447677 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL521807 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL504711 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL492308 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL453807 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL492309 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL449883 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL492710 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL523676 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL452893 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL493160 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL507676 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL523498 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL492521 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL447852 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL493159 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL493355 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL503595 | — | IC50 | = | 23200.0 | nM | 4.63 |