Assay Detail
Functional
CHEMBL867739
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of LPS-stimulated TNF production in THP cells at 1 uM
27
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP |
| 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 |
|---|---|---|---|
| Inhibition | 26 | - | - |
| IC50 | 1 | 6.85 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206815 | APRATASTAT | 2.0 | 2 | 6.85 |
| CHEMBL207729 | — | — | 1 | - |
| CHEMBL205998 | — | — | 1 | - |
| CHEMBL381554 | — | — | 1 | - |
| CHEMBL206481 | — | — | 1 | - |
| CHEMBL204100 | — | — | 1 | - |
| CHEMBL206739 | — | — | 1 | - |
| CHEMBL381163 | — | — | 1 | - |
| CHEMBL203886 | — | — | 1 | - |
| CHEMBL383028 | — | — | 1 | - |
| CHEMBL202899 | — | — | 1 | - |
| CHEMBL202839 | — | — | 1 | - |
| CHEMBL381505 | — | — | 1 | - |
| CHEMBL206155 | — | — | 1 | - |
| CHEMBL437499 | — | — | 1 | - |
| CHEMBL382585 | — | — | 1 | - |
| CHEMBL206144 | — | — | 1 | - |
| CHEMBL202806 | — | — | 1 | - |
| CHEMBL440945 | — | — | 1 | - |
| CHEMBL206298 | — | — | 1 | - |
| CHEMBL380439 | — | — | 1 | - |
| CHEMBL383079 | — | — | 1 | - |
| CHEMBL441177 | — | — | 1 | - |
| CHEMBL206688 | — | — | 1 | - |
| CHEMBL207776 | — | — | 1 | - |
| CHEMBL380343 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206815 | APRATASTAT | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL437499 | — | Inhibition | = | 53.0 | % | - |
| CHEMBL205998 | — | Inhibition | = | 67.0 | % | - |
| CHEMBL381554 | — | Inhibition | = | 74.0 | % | - |
| CHEMBL206481 | — | Inhibition | = | 81.0 | % | - |
| CHEMBL204100 | — | Inhibition | = | 78.0 | % | - |
| CHEMBL206739 | — | Inhibition | = | 76.0 | % | - |
| CHEMBL381163 | — | Inhibition | = | 73.0 | % | - |
| CHEMBL203886 | — | Inhibition | = | 13.0 | % | - |
| CHEMBL383028 | — | Inhibition | = | - | % | - |
| CHEMBL202899 | — | Inhibition | = | - | % | - |
| CHEMBL202839 | — | Inhibition | = | 10.0 | % | - |
| CHEMBL381505 | — | Inhibition | = | 40.0 | % | - |
| CHEMBL206155 | — | Inhibition | = | 5.0 | % | - |
| CHEMBL207729 | — | Inhibition | = | 87.0 | % | - |
| CHEMBL382585 | — | Inhibition | = | 52.0 | % | - |
| CHEMBL206144 | — | Inhibition | = | 19.0 | % | - |
| CHEMBL202806 | — | Inhibition | = | 25.0 | % | - |
| CHEMBL206815 | APRATASTAT | Inhibition | = | 89.0 | % | - |
| CHEMBL440945 | — | Inhibition | = | 62.0 | % | - |
| CHEMBL206298 | — | Inhibition | = | 48.0 | % | - |
| CHEMBL380439 | — | Inhibition | = | 11.0 | % | - |
| CHEMBL383079 | — | Inhibition | = | 50.0 | % | - |
| CHEMBL441177 | — | Inhibition | = | 16.0 | % | - |
| CHEMBL206688 | — | Inhibition | = | 36.0 | % | - |
| CHEMBL207776 | — | Inhibition | = | 76.0 | % | - |
| CHEMBL380343 | — | Inhibition | = | 14.0 | % | - |