Assay Detail
Functional
CHEMBL1008312
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Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 1 hrs before LPS challenge measured after 4 hrs by ELISA
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | RAW264.7 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.55 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495831 | — | — | 1 | 7.17 |
| CHEMBL495795 | — | — | 1 | 6.90 |
| CHEMBL503067 | — | — | 1 | 6.64 |
| CHEMBL497012 | — | — | 1 | 6.62 |
| CHEMBL495621 | — | — | 1 | 6.48 |
| CHEMBL496619 | — | — | 1 | 6.46 |
| CHEMBL498032 | — | — | 1 | 6.42 |
| CHEMBL524533 | — | — | 1 | 6.42 |
| CHEMBL212481 | — | — | 1 | 6.40 |
| CHEMBL380049 | — | — | 1 | 6.31 |
| CHEMBL236572 | — | — | 1 | 6.21 |
| CHEMBL496423 | — | — | 1 | - |
| CHEMBL447275 | — | — | 1 | - |
| CHEMBL499854 | — | — | 1 | - |
| CHEMBL499313 | — | — | 1 | - |
| CHEMBL502796 | — | — | 1 | - |
| CHEMBL497838 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495831 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL495795 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL503067 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL497012 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL495621 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL496619 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL498032 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL524533 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL212481 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL380049 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL236572 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL496423 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL447275 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL499854 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL499313 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL502796 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL497838 | — | IC50 | > | 1000.0 | nM | - |