Assay Detail
Functional
CHEMBL699331
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Inhibition of TNF-alpha release in LPS-stimulated human whole blood assay(WBA)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.69 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431680 | — | — | 1 | 7.22 |
| CHEMBL91636 | — | — | 1 | 7.17 |
| CHEMBL325163 | — | — | 1 | 7.16 |
| CHEMBL325421 | — | — | 1 | 6.92 |
| CHEMBL115263 | — | — | 1 | 6.75 |
| CHEMBL114878 | — | — | 1 | 6.75 |
| CHEMBL324550 | — | — | 1 | 6.64 |
| CHEMBL323929 | — | — | 1 | 6.42 |
| CHEMBL324549 | — | — | 1 | 6.39 |
| CHEMBL432990 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431680 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL91636 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL325163 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL325421 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL115263 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL114878 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL324550 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL323929 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL324549 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL432990 | — | IC50 | = | 3700.0 | nM | 5.43 |