Assay Detail
Binding
CHEMBL867735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TACE
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.37 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207729 | — | — | 1 | 8.10 |
| CHEMBL206481 | — | — | 1 | 7.96 |
| CHEMBL381554 | — | — | 1 | 7.82 |
| CHEMBL207776 | — | — | 1 | 7.72 |
| CHEMBL206815 | APRATASTAT | 2.0 | 1 | 7.70 |
| CHEMBL381163 | — | — | 1 | 7.70 |
| CHEMBL206298 | — | — | 1 | 7.64 |
| CHEMBL383028 | — | — | 1 | 7.55 |
| CHEMBL206688 | — | — | 1 | 7.50 |
| CHEMBL383079 | — | — | 1 | 7.46 |
| CHEMBL441177 | — | — | 1 | 7.40 |
| CHEMBL206144 | — | — | 1 | 7.40 |
| CHEMBL203886 | — | — | 1 | 7.40 |
| CHEMBL206739 | — | — | 1 | 7.38 |
| CHEMBL380439 | — | — | 1 | 7.38 |
| CHEMBL440945 | — | — | 1 | 7.38 |
| CHEMBL382585 | — | — | 1 | 7.28 |
| CHEMBL204100 | — | — | 1 | 7.24 |
| CHEMBL202806 | — | — | 1 | 7.21 |
| CHEMBL202839 | — | — | 1 | 7.17 |
| CHEMBL437499 | — | — | 1 | 7.13 |
| CHEMBL380343 | — | — | 1 | 6.95 |
| CHEMBL202899 | — | — | 1 | 6.86 |
| CHEMBL205998 | — | — | 1 | 6.84 |
| CHEMBL206155 | — | — | 1 | 6.82 |
| CHEMBL381505 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207729 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL206481 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL381554 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL207776 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL206815 | APRATASTAT | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL381163 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL206298 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL383028 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL206688 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL383079 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL441177 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL206144 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL203886 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL206739 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL380439 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL440945 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL382585 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL204100 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL202806 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL202839 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL437499 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL380343 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL202899 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL205998 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL206155 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL381505 | — | IC50 | = | 199.0 | nM | 6.70 |