Assay Detail
Binding
CHEMBL5582725
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Inhibition of human SIRT2 preincubated for 15 mins followed by H3K9Ac (KQTARK(Ac)STGGWW) peptide addition and measured after 5 mins
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
A Mitochondria-Targeting SIRT3 Inhibitor with Activity against Diffuse Large B Cell Lymphoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.22 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5594203 | — | — | 1 | 7.92 |
| CHEMBL5556672 | — | — | 1 | 7.85 |
| CHEMBL5595847 | — | — | 1 | 7.75 |
| CHEMBL5592172 | — | — | 1 | 7.70 |
| CHEMBL5592160 | — | — | 1 | 7.60 |
| CHEMBL5590798 | — | — | 1 | 7.57 |
| CHEMBL5592898 | — | — | 1 | 7.52 |
| CHEMBL5593038 | — | — | 1 | 7.42 |
| CHEMBL5584049 | — | — | 1 | 7.40 |
| CHEMBL5590784 | — | — | 1 | 7.36 |
| CHEMBL5593399 | — | — | 1 | 7.35 |
| CHEMBL5595303 | — | — | 1 | 7.30 |
| CHEMBL5594477 | — | — | 1 | 7.30 |
| CHEMBL5593798 | — | — | 1 | 7.14 |
| CHEMBL5592509 | — | — | 1 | 7.09 |
| CHEMBL5595757 | — | — | 1 | 7.06 |
| CHEMBL5595804 | — | — | 1 | 6.92 |
| CHEMBL5594582 | — | — | 1 | 6.89 |
| CHEMBL5594018 | — | — | 1 | 6.05 |
| CHEMBL5594863 | — | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5594203 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5556672 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5595847 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5592172 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5592160 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5590798 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5592898 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5593038 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5584049 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5590784 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5593399 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5595303 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5594477 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5593798 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5592509 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5595757 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5595804 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5594582 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5594018 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5594863 | — | IC50 | = | 7650.0 | nM | 5.12 |