Assay Detail
Binding
CHEMBL4479672
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Inhibition of full-length recombinant human 6His-tagged SENP1 expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by addition of SUMO1-AMC as substrate measured after 1 hr by fluorescence analysis
5
Total Activities
5
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 |
Publication
Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.60 | 5.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012938 | VIALININ A | — | 1 | 5.79 |
| CHEMBL4587307 | — | — | 1 | 5.61 |
| CHEMBL2012939 | — | — | 1 | 5.57 |
| CHEMBL4593579 | — | — | 1 | 5.42 |
| CHEMBL2013072 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012938 | VIALININ A | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL4587307 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL2012939 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL4593579 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL2013072 | — | IC50 | > | 50000.0 | nM | - |