Assay Detail
Binding
CHEMBL1640792
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Inhibition of human TACE by fluorescent spectroscopy
14
Total Activities
14
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
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure based optimization of chromen-based TNF-α converting enzyme (TACE) inhibitors on S1' pocket and their quantitative structure-activity relationship (QSAR) study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 9.08 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1630098 | — | — | 1 | 10.00 |
| CHEMBL1630106 | — | — | 1 | 9.57 |
| CHEMBL1630091 | — | — | 1 | 9.55 |
| CHEMBL1630100 | — | — | 1 | 9.52 |
| CHEMBL1630090 | — | — | 1 | 9.34 |
| CHEMBL402030 | — | — | 1 | 9.30 |
| CHEMBL1630089 | — | — | 1 | 9.28 |
| CHEMBL1630088 | — | — | 1 | 9.18 |
| CHEMBL1630104 | — | — | 1 | 9.05 |
| CHEMBL1630103 | — | — | 1 | 8.98 |
| CHEMBL1630102 | — | — | 1 | 8.97 |
| CHEMBL1630105 | — | — | 1 | 8.97 |
| CHEMBL1630101 | — | — | 1 | 7.96 |
| CHEMBL1630099 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1630098 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1630106 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL1630091 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL1630100 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1630090 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL402030 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1630089 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL1630088 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL1630104 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1630103 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL1630102 | — | IC50 | = | 1.07 | nM | 8.97 |
| CHEMBL1630105 | — | IC50 | = | 1.07 | nM | 8.97 |
| CHEMBL1630101 | — | IC50 | = | 10.94 | nM | 7.96 |
| CHEMBL1630099 | — | IC50 | = | 32.82 | nM | 7.48 |