Assay Detail
Functional
CHEMBL1011628
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Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| 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 | 21 | 6.26 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 10.70 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.11 |
| CHEMBL472963 | — | — | 1 | 6.92 |
| CHEMBL475165 | — | — | 1 | 6.72 |
| CHEMBL474557 | — | — | 1 | 6.66 |
| CHEMBL313439 | — | — | 1 | 6.62 |
| CHEMBL473205 | — | — | 1 | 6.57 |
| CHEMBL508838 | — | — | 1 | 6.47 |
| CHEMBL473204 | — | — | 1 | 6.43 |
| CHEMBL474556 | — | — | 1 | 6.43 |
| CHEMBL88475 | — | — | 1 | 6.16 |
| CHEMBL514339 | — | — | 1 | 5.89 |
| CHEMBL515398 | — | — | 1 | 5.83 |
| CHEMBL475164 | — | — | 1 | 5.82 |
| CHEMBL315529 | — | — | 1 | 5.80 |
| CHEMBL90345 | — | — | 1 | 5.77 |
| CHEMBL88153 | CDC-801 | 2.0 | 1 | 5.60 |
| CHEMBL419135 | — | — | 1 | 5.57 |
| CHEMBL516063 | — | — | 1 | 5.52 |
| CHEMBL473983 | — | — | 1 | 4.46 |
| CHEMBL515728 | — | — | 1 | 4.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL514800 | APREMILAST | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL472963 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL475165 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL474557 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL313439 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL473205 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL508838 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL473204 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL474556 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL88475 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL514339 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL515398 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL475164 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL315529 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL90345 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL88153 | CDC-801 | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL419135 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL516063 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL473983 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL515728 | — | IC50 | = | 36000.0 | nM | 4.44 |