Assay Detail
Binding
CHEMBL1011627
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Inhibition of human PDE4
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 | 6.66 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.52 |
| CHEMBL313439 | — | — | 1 | 7.40 |
| CHEMBL473205 | — | — | 1 | 7.17 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.13 |
| CHEMBL475165 | — | — | 1 | 7.09 |
| CHEMBL474556 | — | — | 1 | 6.92 |
| CHEMBL474557 | — | — | 1 | 6.92 |
| CHEMBL472963 | — | — | 1 | 6.89 |
| CHEMBL514339 | — | — | 1 | 6.66 |
| CHEMBL88475 | — | — | 1 | 6.66 |
| CHEMBL475164 | — | — | 1 | 6.58 |
| CHEMBL315529 | — | — | 1 | 6.47 |
| CHEMBL515728 | — | — | 1 | 6.47 |
| CHEMBL473204 | — | — | 1 | 6.21 |
| CHEMBL508838 | — | — | 1 | 6.16 |
| CHEMBL516063 | — | — | 1 | 6.15 |
| CHEMBL515398 | — | — | 1 | 6.09 |
| CHEMBL88153 | CDC-801 | 2.0 | 1 | 5.96 |
| CHEMBL473983 | — | — | 1 | 5.89 |
| CHEMBL90345 | — | — | 1 | 5.80 |
| CHEMBL419135 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL313439 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL473205 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL514800 | APREMILAST | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL475165 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL474556 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL474557 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL472963 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL514339 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL88475 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL475164 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL315529 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL515728 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL473204 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL508838 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL516063 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL515398 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL88153 | CDC-801 | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL473983 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL90345 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL419135 | — | IC50 | = | 1900.0 | nM | 5.72 |