Assay Detail
Binding
CHEMBL1103427
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Inhibition of human recombinant ADAM17 by fluorometric assay
17
Total Activities
17
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
Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.28 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1089843 | — | — | 1 | 9.15 |
| CHEMBL1089842 | — | — | 1 | 8.80 |
| CHEMBL1088878 | — | — | 1 | 7.23 |
| CHEMBL1093690 | — | — | 1 | 6.96 |
| CHEMBL514138 | CGS-27023A | — | 1 | 6.80 |
| CHEMBL1092104 | — | — | 1 | 6.68 |
| CHEMBL1090647 | — | — | 1 | 6.52 |
| CHEMBL1090284 | — | — | 1 | 5.96 |
| CHEMBL83508 | — | — | 1 | 5.75 |
| CHEMBL311932 | — | — | 1 | 5.64 |
| CHEMBL550148 | — | — | 1 | 5.62 |
| CHEMBL1090283 | — | — | 1 | 5.41 |
| CHEMBL1090035 | — | — | 1 | 5.00 |
| CHEMBL1093689 | — | — | 1 | 4.36 |
| CHEMBL561625 | — | — | 1 | 4.28 |
| CHEMBL181244 | — | — | 1 | - |
| CHEMBL226439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1089843 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1089842 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1088878 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1093690 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL514138 | CGS-27023A | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1092104 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1090647 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1090284 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL83508 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL311932 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL550148 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1090283 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1090035 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1093689 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL561625 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL181244 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL226439 | — | IC50 | = | 180000.0 | nM | - |