Assay Detail
Binding
CHEMBL846289
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Affinity for rolipram binding site of phosphodiesterase type IV (PDE4)
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Orally active indole N-oxide PDE4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.16 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 9.40 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.35 |
| CHEMBL102635 | — | — | 1 | 7.92 |
| CHEMBL102503 | — | — | 1 | 7.52 |
| CHEMBL101479 | — | — | 1 | 7.52 |
| CHEMBL102310 | — | — | 1 | 7.42 |
| CHEMBL323069 | — | — | 1 | 7.29 |
| CHEMBL102741 | — | — | 1 | 7.22 |
| CHEMBL322837 | — | — | 1 | 7.19 |
| CHEMBL414417 | — | — | 1 | 7.17 |
| CHEMBL323132 | — | — | 1 | 7.17 |
| CHEMBL103007 | — | — | 1 | 7.15 |
| CHEMBL318586 | — | — | 1 | 7.07 |
| CHEMBL102758 | — | — | 1 | 7.07 |
| CHEMBL102876 | — | — | 1 | 6.94 |
| CHEMBL299332 | — | — | 1 | 6.92 |
| CHEMBL262269 | — | — | 1 | 6.87 |
| CHEMBL301201 | — | — | 1 | 6.87 |
| CHEMBL104780 | — | — | 1 | 6.65 |
| CHEMBL321760 | — | — | 1 | 6.41 |
| CHEMBL101368 | — | — | 1 | 5.95 |
| CHEMBL102020 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL63 | ROLIPRAM | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL102635 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL102503 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL101479 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL102310 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL323069 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL102741 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL322837 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL414417 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL323132 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL103007 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL318586 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL102758 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL102876 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL299332 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL262269 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL301201 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL104780 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL321760 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL101368 | — | Ki | = | 1124.0 | nM | 5.95 |
| CHEMBL102020 | — | Ki | = | 3184.0 | nM | 5.50 |