Assay Detail
Binding
CHEMBL4185153
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human APE1 preincubated for 15 mins followed by substrate addition by HTS assay
8
Total Activities
8
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
DNA repair nuclease/redox regulator APEX1 (CHEMBL5619) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibitors of nuclease and redox activity of apurinic/apyrimidinic endonuclease 1/redox effector factor 1 (APE1/Ref-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.48 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275938 | AURINTRICARBOXYLIC ACID | — | 1 | 7.26 |
| CHEMBL109037 | — | — | 1 | 6.96 |
| CHEMBL1365553 | — | — | 1 | 6.60 |
| CHEMBL56393 | — | — | 1 | 6.55 |
| CHEMBL164 | MYRICETIN | — | 1 | 6.50 |
| CHEMBL1256623 | — | — | 1 | 6.30 |
| CHEMBL399043 | THIOLACTOMYCIN | — | 1 | 6.00 |
| CHEMBL1417019 | MITOXANTRONE HYDROCHLORIDE | 4.0 | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275938 | AURINTRICARBOXYLIC ACID | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL109037 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1365553 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL56393 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL164 | MYRICETIN | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1256623 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL399043 | THIOLACTOMYCIN | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1417019 | MITOXANTRONE HYDROCHLORIDE | IC50 | = | 2000.0 | nM | 5.70 |