Assay Detail
Functional
CHEMBL835217
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effect on TNF-Alpha release in LPS-stimulated human whole blood assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.58 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183791 | — | — | 1 | 7.70 |
| CHEMBL184782 | — | — | 1 | 7.12 |
| CHEMBL184553 | — | — | 1 | 7.11 |
| CHEMBL185279 | — | — | 1 | 7.08 |
| CHEMBL185587 | — | — | 1 | 6.99 |
| CHEMBL434348 | — | — | 1 | 6.96 |
| CHEMBL184975 | — | — | 1 | 6.91 |
| CHEMBL185159 | — | — | 1 | 6.80 |
| CHEMBL359569 | — | — | 1 | 6.79 |
| CHEMBL363968 | — | — | 1 | 6.75 |
| CHEMBL184885 | — | — | 1 | 6.75 |
| CHEMBL184265 | — | — | 1 | 6.72 |
| CHEMBL365031 | — | — | 1 | 6.68 |
| CHEMBL364875 | — | — | 1 | 6.65 |
| CHEMBL181807 | — | — | 1 | 6.64 |
| CHEMBL184062 | — | — | 1 | 6.62 |
| CHEMBL426434 | — | — | 1 | 6.60 |
| CHEMBL183431 | — | — | 1 | 6.60 |
| CHEMBL185397 | — | — | 1 | 6.59 |
| CHEMBL364589 | — | — | 1 | 6.39 |
| CHEMBL184302 | — | — | 1 | 6.38 |
| CHEMBL363732 | — | — | 1 | 6.38 |
| CHEMBL184266 | — | — | 1 | 6.30 |
| CHEMBL359625 | — | — | 1 | 6.29 |
| CHEMBL361376 | — | — | 1 | 6.22 |
| CHEMBL185321 | — | — | 1 | 6.20 |
| CHEMBL365905 | — | — | 1 | 6.06 |
| CHEMBL363451 | — | — | 1 | 6.05 |
| CHEMBL183868 | — | — | 1 | 6.04 |
| CHEMBL184942 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183791 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL184782 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL184553 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL185279 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL185587 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL434348 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL184975 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL185159 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL359569 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL363968 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL184885 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL184265 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL365031 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL364875 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL181807 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL184062 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL183431 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL426434 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL185397 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL364589 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL184302 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL363732 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL184266 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL359625 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL361376 | — | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL185321 | — | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL365905 | — | IC50 | = | 867.0 | nM | 6.06 |
| CHEMBL363451 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL183868 | — | IC50 | = | 913.0 | nM | 6.04 |
| CHEMBL184942 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL183828 | — | IC50 | = | 2503.0 | nM | 5.60 |
| CHEMBL362100 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL185521 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL184200 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL182730 | — | IC50 | > | 3000.0 | nM | - |