Assay Detail
Binding
CHEMBL4835780
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Uncompetitive inhibition of His6-tagged SIRT1 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant measured every 2 mins for 30 mins in presence of NAD+ and ATP by FLucK549Ac based Michaelis-Menten analysis
3
Total Activities
3
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
Discovery of Dihydro-1,4-Benzoxazine Carboxamides as Potent and Highly Selective Inhibitors of Sirtuin-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 6.63 | 6.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420311 | — | — | 1 | 6.94 |
| CHEMBL4858009 | — | — | 1 | 6.54 |
| CHEMBL4855963 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420311 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL4858009 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL4855963 | — | Ki | = | 400.0 | nM | 6.40 |