Assay Detail
Binding
CHEMBL4835774
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His6-tagged/TEV fused SIRT2 (unknown origin) expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by NAD+ addition and measured after 30 mins by FLucK529Ac based luminescence assay
63
Total Activities
61
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
Discovery of Dihydro-1,4-Benzoxazine Carboxamides as Potent and Highly Selective Inhibitors of Sirtuin-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 63 | 4.84 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420311 | — | — | 1 | 6.30 |
| CHEMBL4868419 | — | — | 1 | 6.28 |
| CHEMBL4861853 | — | — | 1 | 6.22 |
| CHEMBL4876108 | — | — | 1 | 5.75 |
| CHEMBL4876032 | — | — | 1 | 5.38 |
| CHEMBL4858009 | — | — | 1 | 4.97 |
| CHEMBL4846832 | — | — | 1 | 4.95 |
| CHEMBL4876979 | — | — | 1 | 4.91 |
| CHEMBL4861333 | — | — | 1 | 4.81 |
| CHEMBL4874547 | — | — | 1 | 4.78 |
| CHEMBL4847107 | — | — | 1 | 4.65 |
| CHEMBL4846802 | — | — | 1 | 4.64 |
| CHEMBL4874493 | — | — | 1 | 4.60 |
| CHEMBL4862252 | — | — | 1 | 4.58 |
| CHEMBL4874876 | — | — | 1 | 4.50 |
| CHEMBL4871146 | — | — | 1 | 4.49 |
| CHEMBL4855963 | — | — | 3 | 4.47 |
| CHEMBL4863826 | — | — | 1 | 4.47 |
| CHEMBL4866570 | — | — | 1 | 4.46 |
| CHEMBL4862410 | — | — | 1 | 4.45 |
| CHEMBL4856119 | — | — | 1 | 4.44 |
| CHEMBL4855315 | — | — | 1 | 4.38 |
| CHEMBL4863048 | — | — | 1 | 4.38 |
| CHEMBL4863020 | — | — | 1 | 4.24 |
| CHEMBL4860158 | — | — | 1 | - |
| CHEMBL4875920 | — | — | 1 | - |
| CHEMBL4845789 | — | — | 1 | - |
| CHEMBL4850398 | — | — | 1 | - |
| CHEMBL4849744 | — | — | 1 | - |
| CHEMBL4860603 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420311 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4868419 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4861853 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4876108 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL4876032 | — | IC50 | = | 4190.0 | nM | 5.38 |
| CHEMBL4858009 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4846832 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL4876979 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL4861333 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL4874547 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL4847107 | — | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL4846802 | — | IC50 | = | 22800.0 | nM | 4.64 |
| CHEMBL4874493 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4862252 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4874876 | — | IC50 | = | 31800.0 | nM | 4.50 |
| CHEMBL4871146 | — | IC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL4855963 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4863826 | — | IC50 | = | 33600.0 | nM | 4.47 |
| CHEMBL4866570 | — | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL4862410 | — | IC50 | = | 35400.0 | nM | 4.45 |
| CHEMBL4856119 | — | IC50 | = | 36100.0 | nM | 4.44 |
| CHEMBL4855963 | — | IC50 | = | 37700.0 | nM | 4.42 |
| CHEMBL4855315 | — | IC50 | = | 41900.0 | nM | 4.38 |
| CHEMBL4863048 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL4855963 | — | IC50 | = | 47300.0 | nM | 4.33 |
| CHEMBL4863020 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL4853946 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4847736 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4852582 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4858490 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4879347 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4867773 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4870792 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4873507 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4857553 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4872699 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4860536 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4852298 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4875158 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4875507 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4878754 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4865218 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4860158 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4845789 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4873836 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4850398 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4869708 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4849744 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4860603 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4862058 | — | IC50 | > | 60000.0 | nM | - |