Assay Detail
Binding
CHEMBL4054428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-tagged recombinant human SIRT-1 expressed in Escherichia coli using Fluor-de-Lys-SIRT1 as substrate after 15 mins by fluorescence assay
12
Total Activities
12
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 and Characterization of R/S-N-3-Cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.94 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420311 | — | — | 1 | 7.00 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 5.55 |
| CHEMBL4102380 | — | — | 1 | 5.21 |
| CHEMBL4074207 | — | — | 1 | 4.49 |
| CHEMBL4059756 | — | — | 1 | 4.26 |
| CHEMBL380797 | SIRTINOL | — | 1 | 4.08 |
| CHEMBL224864 | — | — | 1 | 4.01 |
| CHEMBL4090805 | — | — | 1 | - |
| CHEMBL4084417 | — | — | 1 | - |
| CHEMBL4092171 | — | — | 1 | - |
| CHEMBL4104634 | — | — | 1 | - |
| CHEMBL608379 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420311 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL265502 | SURAMIN | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4102380 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4074207 | — | IC50 | = | 32100.0 | nM | 4.49 |
| CHEMBL4059756 | — | IC50 | = | 54800.0 | nM | 4.26 |
| CHEMBL380797 | SIRTINOL | IC50 | = | 82500.0 | nM | 4.08 |
| CHEMBL224864 | — | IC50 | = | 98100.0 | nM | 4.01 |
| CHEMBL4090805 | — | IC50 | = | 108700.0 | nM | - |
| CHEMBL4084417 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4092171 | — | IC50 | = | 121200.0 | nM | - |
| CHEMBL4104634 | — | IC50 | = | 109900.0 | nM | - |
| CHEMBL608379 | — | IC50 | > | 200000.0 | nM | - |