Assay Detail
Binding
CHEMBL2340697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged SIRT3 (102 to 399) expressed in Escherichia coli BL21(DE3) assessed as inhibition of deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after 30 mins by mass spectrophotometric analysis
34
Total Activities
34
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-3, mitochondrial (CHEMBL4461) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.08 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2332041 | — | — | 1 | 8.49 |
| CHEMBL2332039 | — | — | 1 | 8.40 |
| CHEMBL2332037 | — | — | 1 | 8.31 |
| CHEMBL2338810 | — | — | 1 | 8.14 |
| CHEMBL2332043 | — | — | 1 | 8.12 |
| CHEMBL2332042 | — | — | 1 | 7.89 |
| CHEMBL2332040 | — | — | 1 | 7.64 |
| CHEMBL2332038 | — | — | 1 | 7.62 |
| CHEMBL2338813 | — | — | 1 | 7.55 |
| CHEMBL2332044 | — | — | 1 | 7.54 |
| CHEMBL2338814 | — | — | 1 | 7.52 |
| CHEMBL2332055 | — | — | 1 | 7.48 |
| CHEMBL2332052 | — | — | 1 | 7.41 |
| CHEMBL2332045 | — | — | 1 | 7.25 |
| CHEMBL2338812 | — | — | 1 | 7.21 |
| CHEMBL2338808 | — | — | 1 | 7.17 |
| CHEMBL2338809 | — | — | 1 | 7.04 |
| CHEMBL2338816 | — | — | 1 | 6.96 |
| CHEMBL2338818 | — | — | 1 | 6.82 |
| CHEMBL2332053 | — | — | 1 | 6.55 |
| CHEMBL2332046 | — | — | 1 | 6.52 |
| CHEMBL2338811 | — | — | 1 | 6.43 |
| CHEMBL2332054 | — | — | 1 | 6.19 |
| CHEMBL2332051 | — | — | 1 | 6.11 |
| CHEMBL2338815 | — | — | 1 | 5.89 |
| CHEMBL2338817 | — | — | 1 | 5.68 |
| CHEMBL2332050 | — | — | 1 | 5.36 |
| CHEMBL2332047 | — | — | 1 | 5.07 |
| CHEMBL2332049 | — | — | 1 | - |
| CHEMBL2332048 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2332041 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL2332039 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2332037 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL2338810 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2332043 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL2332042 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2332040 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2332038 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2338813 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2332044 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2338814 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2332055 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2332052 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2332045 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2338812 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2338808 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2338809 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2338816 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2338818 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2332053 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2332046 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2338811 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2332054 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2332051 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2338815 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2338817 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2332050 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2332047 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2332049 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2332048 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL420311 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2338819 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2338820 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2338821 | — | IC50 | > | 50000.0 | nM | - |