Assay Detail
Binding
CHEMBL1007511
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TACE catalytic domain expressed in CHO cells by FRET assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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
Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.15 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL498032 | — | — | 1 | 9.00 |
| CHEMBL502796 | — | — | 1 | 9.00 |
| CHEMBL212481 | — | — | 1 | 9.00 |
| CHEMBL385821 | — | — | 1 | 9.00 |
| CHEMBL496619 | — | — | 1 | 8.92 |
| CHEMBL495831 | — | — | 1 | 8.70 |
| CHEMBL380049 | — | — | 1 | 8.70 |
| CHEMBL497838 | — | — | 1 | 8.70 |
| CHEMBL503067 | — | — | 1 | 8.70 |
| CHEMBL497012 | — | — | 1 | 8.70 |
| CHEMBL236572 | — | — | 1 | 8.70 |
| CHEMBL499854 | — | — | 1 | 8.52 |
| CHEMBL524533 | — | — | 1 | 8.05 |
| CHEMBL496423 | — | — | 1 | 8.00 |
| CHEMBL495795 | — | — | 1 | 7.96 |
| CHEMBL495621 | — | — | 1 | 7.48 |
| CHEMBL524281 | — | — | 1 | 7.33 |
| CHEMBL447275 | — | — | 1 | 7.19 |
| CHEMBL526646 | — | — | 1 | 7.14 |
| CHEMBL497413 | — | — | 1 | 6.87 |
| CHEMBL496618 | — | — | 1 | 6.83 |
| CHEMBL495629 | — | — | 1 | 6.70 |
| CHEMBL499313 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL498032 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL502796 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL212481 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL385821 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL496619 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL495831 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL380049 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL497838 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL503067 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL497012 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL236572 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL499854 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL524533 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL496423 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL495795 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL495621 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL524281 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL447275 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL526646 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL497413 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL496618 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL495629 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL499313 | — | IC50 | < | 1.0 | nM | - |