Assay Detail
Functional
CHEMBL927612
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Inhibition of LPS-stimulated TNFalpha release in human whole blood
15
Total Activities
15
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
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.51 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134908 | — | — | 1 | 7.70 |
| CHEMBL252891 | — | — | 1 | 7.36 |
| CHEMBL252892 | — | — | 1 | 7.26 |
| CHEMBL252893 | — | — | 1 | 6.89 |
| CHEMBL402992 | — | — | 1 | 6.73 |
| CHEMBL253088 | — | — | 1 | 6.54 |
| CHEMBL437791 | — | — | 1 | 6.41 |
| CHEMBL537229 | — | — | 1 | 6.32 |
| CHEMBL403684 | — | — | 1 | 6.21 |
| CHEMBL402746 | — | — | 1 | 6.18 |
| CHEMBL254108 | — | — | 1 | 6.05 |
| CHEMBL254307 | — | — | 1 | 5.54 |
| CHEMBL404083 | — | — | 1 | 5.39 |
| CHEMBL254107 | — | — | 1 | - |
| CHEMBL253909 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134908 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL252891 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL252892 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL252893 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL402992 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL253088 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL437791 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL537229 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL403684 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL402746 | — | IC50 | = | 662.0 | nM | 6.18 |
| CHEMBL254108 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL254307 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL404083 | — | IC50 | = | 4114.0 | nM | 5.39 |
| CHEMBL254107 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL253909 | — | IC50 | > | 3000.0 | nM | - |