Assay Detail
Functional
CHEMBL934155
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Inhibition of LPS-induced TNFalpha release in human whole blood
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.82 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404019 | — | — | 1 | 7.28 |
| CHEMBL429674 | — | — | 1 | 7.19 |
| CHEMBL271450 | — | — | 1 | 7.13 |
| CHEMBL403777 | — | — | 1 | 7.13 |
| CHEMBL255418 | — | — | 1 | 7.12 |
| CHEMBL403539 | — | — | 1 | 6.97 |
| CHEMBL272512 | — | — | 1 | 6.95 |
| CHEMBL403778 | — | — | 1 | 6.91 |
| CHEMBL270817 | — | — | 1 | 6.82 |
| CHEMBL272102 | — | — | 1 | 6.79 |
| CHEMBL258055 | — | — | 1 | 6.78 |
| CHEMBL402393 | — | — | 1 | 6.77 |
| CHEMBL402636 | — | — | 1 | 6.66 |
| CHEMBL255160 | — | — | 1 | 6.58 |
| CHEMBL271938 | — | — | 1 | 6.20 |
| CHEMBL402118 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404019 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL429674 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL271450 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL403777 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL255418 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL403539 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL272512 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL403778 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL270817 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL272102 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL258055 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL402393 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL402636 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL255160 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL271938 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL402118 | — | IC50 | = | 1230.0 | nM | 5.91 |