Assay Detail
Functional
CHEMBL1011629
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TNFalpha production in LPS-stimulated human whole blood preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay
20
Total Activities
20
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 (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.85 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 6.96 |
| CHEMBL475165 | — | — | 1 | 6.36 |
| CHEMBL313439 | — | — | 1 | 6.31 |
| CHEMBL474557 | — | — | 1 | 5.85 |
| CHEMBL472963 | — | — | 1 | 5.80 |
| CHEMBL474556 | — | — | 1 | 5.66 |
| CHEMBL473205 | — | — | 1 | 5.62 |
| CHEMBL514339 | — | — | 1 | 5.60 |
| CHEMBL88475 | — | — | 1 | 5.40 |
| CHEMBL419135 | — | — | 1 | 4.98 |
| CHEMBL473983 | — | — | 1 | - |
| CHEMBL516063 | — | — | 1 | - |
| CHEMBL515728 | — | — | 1 | - |
| CHEMBL508838 | — | — | 1 | - |
| CHEMBL515398 | — | — | 1 | - |
| CHEMBL473204 | — | — | 1 | - |
| CHEMBL90345 | — | — | 1 | - |
| CHEMBL475164 | — | — | 1 | - |
| CHEMBL315529 | — | — | 1 | - |
| CHEMBL88153 | CDC-801 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL514800 | APREMILAST | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL475165 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL313439 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL474557 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL472963 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL474556 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL473205 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL514339 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL88475 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL419135 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL473983 | — | IC50 | - | — | - | |
| CHEMBL516063 | — | IC50 | - | — | - | |
| CHEMBL515728 | — | IC50 | - | — | - | |
| CHEMBL508838 | — | IC50 | - | — | - | |
| CHEMBL515398 | — | IC50 | - | — | - | |
| CHEMBL473204 | — | IC50 | - | — | - | |
| CHEMBL90345 | — | IC50 | - | — | - | |
| CHEMBL475164 | — | IC50 | - | — | - | |
| CHEMBL315529 | — | IC50 | - | — | - | |
| CHEMBL88153 | CDC-801 | IC50 | - | — | - |